Chloroquine is an antimalarial drug that was originally synthesized in Germany in 1934. It works by accumulating in the food vacuoles of parasitic protozoa, such as Plasmodium falciparum, the parasite that causes malaria. Chloroquine disrupts the parasite's ability to digest hemoglobin, leading to its death. Chloroquine has been used to treat malaria for decades and is considered a safe and effective drug. However, resistance to chloroquine has emerged in some areas, making it less effective in those regions. Chloroquine has also been investigated for its potential to treat other conditions, such as rheumatoid arthritis, lupus, and some types of cancer. It has been studied for its potential to inhibit the growth of cancer cells and to modulate the immune system. In recent years, chloroquine has been investigated for its potential to treat COVID-19. While early studies showed some promise, further research is needed to determine its efficacy and safety for this purpose. Chloroquine's ability to inhibit lysosomal function and modulate the immune system makes it a subject of ongoing research for various medical applications. '
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 2719 |
| CHEMBL ID | 76 |
| CHEBI ID | 3638 |
| SCHEMBL ID | 8933 |
| MeSH ID | M0004182 |
| Synonym |
|---|
| AB00053436-05 |
| BRD-A91699651-065-01-1 |
| reumachlor |
| benaquin |
| rp 3377 |
| resochen |
| amokin |
| nsc187208 |
| quinagamine |
| chloroquinium |
| avlochlor |
| arthrochin |
| roquine |
| heliopar |
| malaren |
| bemasulph |
| malarex |
| quinagamin |
| chloraquine |
| wln: t66 bnj emy1&3n2&2 ig |
| quinoscan |
| iroquine |
| chlorquin |
| sn 6718 |
| chlorochin |
| pfizerquine |
| gontochin |
| quinilon |
| sn 7618 |
| nivachine |
| quinachlor |
| trochin |
| sopaquin |
| 7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline |
| mesylith |
| quinercyl |
| lapaquin |
| chloroquina |
| quinoline, 7-chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]- |
| win 244 |
| silbesan |
| siragan |
| clorochina |
| aralen |
| tresochin |
| n(sup4)-(7-chloro-4-quinolinyl)-n(sup1),4-pentanediamine |
| klorokin |
| elestol |
| cidanchin |
| reumaquin |
| 1, n4-(7-chloro-4-quinolinyl)-n1,n1-diethyl- |
| bipiquin |
| neochin |
| dichinalex |
| imagon |
| artrichin |
| malaquin |
| resoquina |
| nsc-187208 |
| cocartrit |
| solprina |
| bemaco |
| w 7618 |
| KBIO1_000404 |
| DIVK1C_000404 |
| n(sup 4)-(7-chloro-4-quinolinyl)-n(sup 1),n(sup 1)-diethyl-1,4-pentanediamine |
| quinoline, 7-chloro-4-((4-(diethylamino)-1-methylbutyl)amino)- |
| st 21 (pharmaceutical) |
| cloroquina [inn-spanish] |
| hsdb 3029 |
| ronaquine |
| 7-chloro-4-((4-(diethylamino)-1-methylbutyl)amino)quinoline |
| brn 0482809 |
| st 21 |
| 1,4-pentanediamine, n(4)-(7-chloro-4-quinolinyl)-n(1),n(1)-diethyl- |
| n4-(7-chloro-4-quinolinyl)-n1,n1-diethyl-1,4-pentanediamine |
| chloroquine (van) |
| 1,4-pentanediamine, n(sup 4)-(7-chloro-4-quinolinyl)-n(sup 1),n(sup 1)-diethyl- |
| chlorochinum |
| clorochina [dcit] |
| ccris 3439 |
| nsc 187208 |
| chloroquinum [inn-latin] |
| einecs 200-191-2 |
| bdbm22985 |
| {4-[(7-chloroquinolin-4-yl)amino]pentyl}diethylamine |
| chembl76 , |
| chloroquine, 17 |
| SPECTRUM_000132 |
| BSPBIO_000595 |
| delagil |
| khingamin |
| ipsen 225 |
| tanakene |
| cq |
| chloroin |
| chingamin |
| nsc14050 |
| 3377 rp |
| nivaquine b |
| rivoquine |
| arolen |
| sanoquin |
| resoquine |
| chemochin |
| miniquine |
| gontochin phosphate |
| quingamine |
| bemaphate |
| PRESTWICK3_000548 |
| SMP2_000034 |
| LOPAC0_000296 |
| PRESTWICK2_000548 |
| BPBIO1_000655 |
| BSPBIO_002001 |
| quinoline, 7-chloro-4-(4-diethylamino-1-methyl-butylamino)- |
| chloroquin |
| capquin |
| rp-3377 |
| 1,4-pentanediamine, n4-(7-chloro-4-quinolinyl)-n1,n1-diethyl- |
| malaquin (*diphosphate*) |
| AB00053436 |
| C07625 |
| chloroquine |
| 54-05-7 |
| DB00608 |
| D02366 |
| chloroquine (usp/inn) |
| n(4)-(7-chloroquinolin-4-yl)-n(1),n(1)-diethylpentane-1,4-diamine |
| chloroquinum |
| n(4)-(7-chloro-4-quinolinyl)-n(1),n(1)-diethyl-1,4-pentanediamine |
| CHEBI:3638 , |
| cloroquina |
| KBIOGR_000778 |
| KBIO2_000592 |
| KBIOSS_000592 |
| KBIO2_003160 |
| MOLMAP_000009 |
| KBIO2_005728 |
| NCI60_000894 |
| KBIO3_001221 |
| SPECTRUM3_000341 |
| PRESTWICK0_000548 |
| SPBIO_000174 |
| SPECTRUM2_000127 |
| NINDS_000404 |
| PRESTWICK1_000548 |
| SPBIO_002516 |
| SPECTRUM4_000279 |
| IDI1_000404 |
| CU-01000012392-2 , |
| SPECTRUM5_000707 |
| NCGC00162120-01 |
| n4-(7-chloroquinolin-4-yl)-n1,n1-diethylpentane-1,4-diamine |
| 4-n-(7-chloroquinolin-4-yl)-1-n,1-n-diethylpentane-1,4-diamine |
| HMS2090O03 |
| NCGC00015256-04 |
| chlorochine |
| GNF-PF-4216 |
| MLS-0466768.0001 |
| CCG-204391 |
| AKOS015935106 |
| NCGC00015256-10 |
| NCGC00015256-02 |
| NCGC00015256-09 |
| NCGC00015256-03 |
| NCGC00015256-05 |
| NCGC00015256-07 |
| NCGC00015256-08 |
| NCGC00015256-06 |
| 3377 rp opalate |
| chloroquine + proveblue |
| unii-886u3h6uff |
| (+-)-chloroquine |
| 886u3h6uff , |
| chloroquine [usp:inn:ban] |
| FT-0623612 |
| NCGC00015256-13 |
| EPITOPE ID:131785 |
| S6999 |
| n'-(7-chloroquinolin-4-yl)-n,n-diethylpentane-1,4-diamine |
| gtpl5535 |
| chloroquine [hsdb] |
| chloroquine [mart.] |
| chloroquine [mi] |
| chloroquine [usp monograph] |
| chloroquine [who-dd] |
| 1,4-pentanediamine, n(sup 4)-(7-chloro-4-quinolinyl)-n(sup 1),n (sup 1)-diethyl- |
| chloroquine [vandf] |
| chloroquine [inn] |
| chloroquine [usp impurity] |
| n4-(7-chloro-4-quinolyl)-n1,n1-diethyl-pentane-1,4-diamine |
| SCHEMBL8933 |
| KH-0005 |
| delagil (salt/mix) |
| n(sup4)-(7-chloro-4-quinolinyl)-n(sup1),n(sup1)-diethyl-1,4-pentanediamine |
| (.+/-.)-chloroquine |
| tanakan (salt/mix) |
| cloroquine |
| arechin (salt/mix) |
| resoquine (salt/mix) |
| bemaphate (salt/mix) |
| AB00053436_06 |
| AB00053436_07 |
| DTXSID2040446 , |
| mfcd00024009 |
| CS-W004760 |
| SBI-0050284.P004 |
| NCGC00015256-17 |
| Q422438 |
| CS-0021871 |
| 4,7-dichloroquine |
| chloroquine; chloroquine sulphate; 4-n-(7-chloroquinolin-4-yl)-1-n,1-n-diethylpentane-1,4-diamine |
| HY-17589A |
| 117399-83-4 |
| BRD-A91699651-316-06-7 |
| SDCCGSBI-0050284.P005 |
| NCGC00015256-28 |
| SB73098 |
| SY086904 |
| 7-chloro-n-[5-(diethylamino)pentan-2-yl]quinolin-4-amine |
| EN300-120683 |
| C3730 |
| cloroquina (inn-spanish) |
| chloroquine (usp:inn:ban) |
| p01ba01 |
| chloroquine (usp impurity) |
| chloroquine (usp monograph) |
| (7-chloro-4-(4-diethylamino-1-methylbutylamino)-quinoline |
| chloroquinum (inn-latin) |
| dtxcid0020446 |
| chloroquine (mart.) |
| n~4~-(7-chloroquinolin-4-yl)-n~1~,n~1~-diethylpentane-1,4-diamine |
Chloroquine (CQ) is a low-cost antimalarial used worldwide for the treatment of Plasmodium vivax malaria. It has been found to exhibit anti-ZIKV activity at concentrations around 10 μM.
Chloroquine (CQ) has a broad spectrum of pharmacological activities including anticancer and anti-inflammatory, in addition to its well-known antimalarial activity. It has a major impact on the vision-related health status of affected patients, emphasizing the need for its anticipation. Chlorquine has a parallel inhibitory effect on DNA replication in human lymphocytes.
Chloroquine resistance has been genetically linked to mutations in a parasite protein (PfCRT) that might confer resistance by inhibiting chloroquine accumulation in infected erythrocytes. The drug has been used worldwide for about 75 years and is listed by the WHO as an essential medicine to treat malaria.
Chloroquine can cause muscle problems, loss of appetite, and diarrhea as a side effect. It can inhibit the cell proliferation, reduce ATP level and induce apoptosis in HepG2 cells.
Pretreatment with chloroquine for 3 h, resulted in a 2-2.5 fold increase in 125i-labeled very low density lipoprotein recovered in the liver 45 min after injection of the homologous and heterologous lipoproteins. A treatment with chlorquine is indicated in cases with contraindications again glucocorticoids and azathioprine.
Chloroquine diphosphate does not seem to induce hearing impairment as measured by pure tone audiometry, reinforcing its safe use during pregnancy of lupus patients. The most serious side-effect of chloroquine is retinopathy.
The plasma half-life of chloroquine was significantly higher in renal patients than in controls. Chloroquine is extensively distributed with an enormous total apparent volume of distribution (Vd) more than 100 L/kg. The developed population-based pharmacokinetic model could be applied for future prediction of optimal dosage regimen.
The activity of chloroquine and quinine, alone and in combination with desferrioxamine (7 mumol/liter), was evaluated in vitro against susceptible and resistant clones of Plasmodium falciparum by a semimicroassay system. Chloroquine combined with primaquine was evaluated for the same results.
The effect of rice-based meals on chloroquine bioavailability was assessed in six healthy adult male volunteers. Chloroquine is well absorbed and distributes extensively resulting in a large volume of distribution with an apparent and terminal half-life of 1.
Chloroquine decreased the action of native insulin on glycogen synthesis, but did not affect the dose-response characteristics of encapsulated insulin. We conclude that simple alterations in dosage and frequency of administration can give chloroquine an acceptable therapeutic ratio.
| Excerpt | Relevance | Reference |
|---|---|---|
| " Guidelines for cholorquine or quinine dosage in severe disease are proposed; each drug is given at a dose of 5 to 10 mg/kg in 10 ml/kg of fluid as an intravenous infusion in four hours at a frequency of dosing every 12 to 24 hours." | ( The treatment of severe falciparum malaria. Hall, AP, 1977) | 0.26 |
| " Therefore it is better to combine glucocorticoids and azathioprine in some cases, especially in those with a high dosed glucocorticoid therapy." | ( [Therapy of chronic hepatitis (author's transl)]. Siede, W, 1979) | 0.26 |
| " The dosage was subsequently adjusted to keep the parasitemia below 5%." | ( Plasmodium berghei--infected mice. Focal glomerulonephritis in hyperimmune state. Bhamarapravati, N; Boonpucknavig, S; Boonpucknavig, V, 1979) | 0.26 |
| " The accumulation of a nontoxic drug in the eye is not necessarily of clinical significance, but ocular damage can occur in patients on long-term tricyclic agents when the amount, duration, and frequency of dosage are sufficiently high." | ( Ocular accumulation and toxicity of certain systemically administered drugs. Mason, CG, 1977) | 0.26 |
| " Macular changes were found in about 25% of the patients, regardless of age in the lowest dosage group." | ( Chloroquine retinopathy in patients with rheumatoid arthritis. Elman, A; Gullberg, R; Nilsson, E; Rendahl, I; Wachtmeister, L, 1976) | 1.7 |
| " Combination therapy with full-dose quinine and clindamycin for three days cured all four patients so treated who were followed up, and with half dosage three out of five patients were cured." | ( Falciparum malaria semi-resistant to clindamycin. Doberstyn, EB; Hall, AP; Nanokorn, A; Sonkom, P, 1975) | 0.25 |
| " If, however, chloroquine is administered, the necessity of exakt dosage and periodic ophthalmologic controls has to be stressed." | ( [Complications in chloroquin therapy]. Siegmeth, W, 1975) | 0.62 |
| " After treatment with Resochin in an erroneously high dosage (1." | ( [Accident in treatment of porphyria cutanea tarda by chloroquine (Resochin) (author's transl)]. Eichenauer, MG; Goerz, G; Krieg, T, 1976) | 0.51 |
| " The mean dosage of chloroquine for complete inhibition of schizont formation declined from 10." | ( [Alteration in resistance of Plasmodium falciparum to chloroquine after cessation of chloroquine medication for twelve years]. Cai, XZ; Gao, DQ; Liang, AH; Ling, CF; Liu, DQ; Liu, RJ; Qiu, CP; Ren, DX; Tang, Y; Zhang, CY, 1992) | 0.86 |
| " In six patients, the concentrations were followed during a one day dosage interval." | ( Chloroquine levels in blood during chronic treatment of patients with rheumatoid arthritis. Augustijns, P; Geusens, P; Verbeke, N, 1992) | 1.73 |
| " In 5 patients it was demonstrated that the amount of uptake of chloroquine into the hair varied proportionally with the dosage (from 500 mg/week to 10 g single dose) and with the time of administration." | ( Sequential concentration of chloroquine in human hair correlates with ingested dose and duration of therapy. Ochsendorf, FR; Raudonat, HW; Runne, U; Schmidt, K, 1992) | 0.82 |
| " Mefloquine prophylaxis has required a change in its dosing regimen." | ( Trends and controversies in the prophylaxis and treatment of malaria. Bia, FJ, 1992) | 0.28 |
| " In nine of 13 patients who received prophylaxis, there was inadequate dosing or poor compliance." | ( Imported malaria in the Bronx: review of 51 cases recorded from 1986 to 1991. Froude, JR; Tanowitz, HB; Weiss, LM; Wittner, M, 1992) | 0.28 |
| " The authors consider it appropriate in this region to continue treating malaria in children with chloroquine (in a dosage of 25 mg/kg) and to use a second-line treatment in the event of the recurrence of malaria symptoms within the next two weeks." | ( [Stability of P. Falciparum resistance to chloroquine between 1987 and 1989 in Mounana, Gabon]. Guéret, D; Le Bras, J; Migot, F; Ringwald, P; Thibaut, P, 1992) | 0.76 |
| " The radiopotentiation factor, which is similar to the dose modification factor, was determined from dose-response curves by relating the reciprocal of the slope (D0) of the reference survival curve to that of the survival curve of cells receiving the combined postirradiation treatment with chloroquine and mild hyperthermia." | ( Potentiation of radiation lethality in HeLa cells by combined mild hyperthermia and chloroquine. Austin, JP; Djordjevic, B; Lange, CS; Rotman, M, 1992) | 0.68 |
| " A dosage of chloroquine base (25 mg/kg of body weight) was given to women over a 3-day period, followed by 5 mg/kg doses administered weekly for 4 weeks." | ( Malaria and pregnancy in Cameroonian women. Effect of pregnancy on Plasmodium falciparum parasitemia and the response to chloroquine. Campbell, CC; James, MA; Mvondo, JL, 1992) | 0.86 |
| " falciparum cases within seventh day in Purulia and Jalpaiguri districts respectively, with a dosage of 25 mg per kg body weight, spread over three days in divided doses." | ( Changing response of Plasmodium falciparum to chloroquine in West Bengal during 1980-1988. Barkakaty, BN; Narasimham, MV; Pandya, AP, 1991) | 0.54 |
| " The antihistamine was more frequently given 30 min before chloroquine, but this had no advantage over the concomitant administration of the two drugs, which may therefore be presented in one dosage form for a better treatment compliance." | ( Responsiveness of chloroquine-induced pruritus to antihistamine therapy--a clinical survey. Okor, RS, 1990) | 0.86 |
| " With a judiciously determined daily dosage and regular 6-month ophthalmologic follow-up examinations, the risk of developing retinopathy can be avoided, because the daily dosage rate rather than total dose accumulation determines the development of chloroquine-induced retinopathy." | ( Treatment of cutaneous sarcoidosis with chloroquine. Review of the literature. Arzubiaga, C; Horowitz, DH; King, LE; Zic, JA, 1991) | 0.73 |
| " 36% of 642 women had urine chloroquine metabolite levels compatible with regular compliance to the weekly chloroquine dosage schedule." | ( Antenatal chloroquine chemoprophylaxis in Malawi: chloroquine resistance, compliance, protective efficacy and cost. Campbell, CC; Heymann, DL; Khoromana, CO; McFarland, DA; Steketee, RW; Wirima, JJ, ) | 0.83 |
| " Taken together, these data suggest that more effective dosage regimens will be possible when therapeutic concentration ranges are properly established." | ( Antimalarials in rheumatic diseases. Cutler, D; Day, R; Tett, S, 1990) | 0.28 |
| " The increase dosage in comparison with the WHO recommendations (25 mg/kg), lead to no advantages for chloroquine treatment (50% failure), in contrast with amodiaquine (4% failure)." | ( [Uncomplicated malaria attack in an area with high chloroquine resistance. 2. Evaluation of first-choice therapeutic scheme]. Arrive, A; Eberlé, F; Gazin, P; Hengy, C; Jambou, R; Kouka-Bemba, D, 1990) | 0.75 |
| " Chloroquine has a constant rate of efficiency, whatever dosage and duration of treatment be and should be saved for home presumptive treatment of malaria fever." | ( [Evaluation of the efficacy of amino 4-quinolones in a chemoresistant zone. Proposals for new therapeutic schemes]. Eberle, F; Gazin, P; Hengy, C; Jambou, R; Louis, JP, ) | 1.04 |
| " Validation studies with artemisinin demonstrated the need for revising the protocol for the production of the dosing solutions." | ( In vitro sensitivity of multiresistant Plasmodium falciparum to new candidate antimalarial drugs in western Thailand. Rooney, W; Schildbach, S; Suebsaeng, L; Wernsdorfer, WH, 1990) | 0.28 |
| " Blocking the acetylcholine receptor shifted the dose-response relation for PGE-induced fusion to higher concentrations." | ( The control of chick myoblast fusion by ion channels operated by prostaglandins and acetylcholine. Bevan, S; Entwistle, A; Warner, AE; Zalin, RJ, 1988) | 0.27 |
| " Dose-response studies showed, however, that the State 2 pathway was more sensitive to leupeptin or monensin than the State 1 pathway." | ( Differential effects of leupeptin, monensin and colchicine on ligand degradation mediated by the two asialoglycoprotein receptor pathways in isolated rat hepatocytes. Clarke, BL; Weigel, PH, 1989) | 0.28 |
| " Based on children's weights and treatment histories provided by their mothers, the median total dosage of chloroquine given at home was 12." | ( Home treatment of febrile children with antimalarial drugs in Togo. Deming, MS; Gayibor, A; Jones, TS; Karsa, T; Murphy, K, 1989) | 0.49 |
| " A dose-response study showed saturation of remnant uptake at 180 micrograms of remnant protein/10(7) cells." | ( Chylomicron-remnant uptake by freshly isolated hepatocytes. Effect of heparin and of hepatic triacylglycerol lipase. Griglio, S; Lagrange, D; Le Liepvre, X; Sultan, F, 1989) | 0.28 |
| " A stepwise multiple regression analysis was used to evaluate the dose-response relationship between the registered data on one hand and solvent exposure, employment on chemical tankers, age, alcohol and chloroquine phosphate consumption on the other." | ( Seamen exposed to organic solvents. A cross-sectional study with special reference to the nervous system. Fossan, GO; Moen, BE; Riise, T; Todnem, K, 1988) | 0.46 |
| " The lysosomotropic agent chloroquine induced suppression of LPS-stimulated proliferation and Ig production with a dose-response profile similar to that of DA." | ( Opposite effects of the catecholamines dopamine and norepinephrine on murine polyclonal B-cell activation. Boukhris, W; Kouassi, E; Li, YS; Millet, I; Revillard, JP, ) | 0.43 |
| " Nineteen patients had ocular manifestations of giant cell arteritis always from the onset, except for a fall in visual acuity; 26 relapses were observed in 18 patients, either during reduction of steroid dosage (21 cases) or after withdrawal (5 cases)." | ( [Prognosis of treated temporal arteritis. Retrospective study of 87 cases]. Alcalay, M; Becq-Giraudon, B; Boissonnot, L; Bontoux, D; Gil, R; Gouet, D; Le Berre, D; Lefevre, JP; Maréchaud, R; Risse, JF, 1986) | 0.27 |
| " During gradual reduction of the steroid dosage osteocalcin returned to pretreatment values." | ( Serum osteocalcin in rheumatoid arthritis and other inflammatory arthritides: relation between inflammatory activity and the effect of glucocorticoids and remission inducing drugs. Ekenstam, EA; Hällgren, R; Ljunghall, S, 1986) | 0.27 |
| " The drugs were given as a combined dosage and separately to different groups via stomach gavage tube." | ( Pigmentary changes in rat oral mucosa following antimalarial therapy. Adkins, KF; Barber, MT; Savage, NW, 1986) | 0.27 |
| "With the test in vivo and the bleeding dosage of chloroquine, authors report the rate of resistance of chloroquine to Plasmodium falciparum." | ( [Chemoresistance of Plasmodium falciparum in Kinshasha. In vivo tests and chloroquine absorption]. Elenga, E; Kaba, S; Kadima, N; Lokombe, B; Makengo, N; Mbanzulu, PN; Miankanina, B; Ngangoue, C; Ngbege, T; Ngimbi, NP, 1988) | 0.76 |
| "Oral mepacrine dihydrochloride, 200 mg (158 mg of the base) six-hourly for five doses followed by 100 mg (79 mg of the base) eight-hourly for six days (half dosage for those less than or equal to 50 kg) was given to 21 patients with high-grade chloroquine-resistant falciparum malaria in eastern Thailand." | ( Mepacrine accumulation during treatment of chloroquine-resistant falciparum malaria. Chanthavanich, P; Edwards, G; Looareesuwan, S; Phillips, RE; Rodick, CL; Supanaranond, W; Warrell, DA, 1988) | 0.72 |
| " The blood concentration of chloroquine was dosed before, during and after treatment by a sensitive method." | ( [Low levels of chloroquine resistance of Plasmodium falciparum in the province of Zou in Benin]. Danis, M; Djivoh, C; Fayomi, EB; Gay, F; Massougbodji, A; Turk, P, 1988) | 0.92 |
| " We conclude that simple alterations in dosage and frequency of administration can give parenteral chloroquine an acceptable therapeutic ratio and reinstate it as the treatment of choice for severe malaria in areas where chloroquine resistance is not a major problem." | ( Chloroquine treatment of severe malaria in children. Pharmacokinetics, toxicity, and new dosage recommendations. Berry, C; Brown, J; Churchill, FC; Greenwood, BM; Miller, KD; White, NJ; Williams, SB, 1988) | 1.93 |
| " No nonlinear elimination or distribution processes appeared to be operating at the doses of hydroxychloroquine used in this study, supporting the hypothesis that in the therapeutic dosing range the pharmacokinetics of hydroxychloroquine are linear." | ( A dose-ranging study of the pharmacokinetics of hydroxy-chloroquine following intravenous administration to healthy volunteers. Brown, KF; Cutler, DJ; Day, RO; Tett, SE, 1988) | 0.74 |
| " Information about dosage and date of therapy was not recalled by most of the interviewed parents." | ( Further observations on chemoprophylaxis and prevalence of malaria using questionnaire data in urban and rural areas of Burkina Faso. Bosman, A; Lamizana, L; Sabatinelli, G, ) | 0.13 |
| " The dosage of trans(E)-clopenthixol was optimized through a pharmacokinetic study, and the suppression of the growth of Plasmodium berghei in vivo was tested in mice, with chloroquine acting as the positive and saline as the negative control." | ( Effect of trans(E)-clopenthixol on Plasmodium berghei in vivo. Andersen, BJ; Jepsen, S; Kristiansen, JE; Kurtzhals, JA, 1988) | 0.47 |
| " The dosage of chloroquine recommended roughly 40 years ago for regular long-term prophylaxis should therefore not be changed." | ( Chloroquine and desethylchloroquine concentrations during regular long-term malaria prophylaxis. Bergqvist, Y; Hellgren, U; Rombo, L, 1987) | 2.07 |
| " The dose-response curve for the enhancement of fluid-phase endocytosis by insulin was identical with that for the stimulation of hexose transport, as measured by the uptake of 2-deoxyglucose." | ( Insulin stimulates fluid-phase endocytosis and exocytosis in 3T3-L1 adipocytes. Appleman, JR; Frost, SC; Gibbs, EM; Lane, MD; Lienhard, GE, 1986) | 0.27 |
| " Complete clearance of Plasmodium falciparum trophozoites (TC) by day 7 was achieved by a dosage of 9-12 mg kg-1." | ( In vivo response of Plasmodium falciparum to different doses of chloroquine in semi-immune children in Liberia, West Africa. Bengtsson, E; Björkman, A; Hanson, AP; Rombo, L; Willcox, M, 1986) | 0.51 |
| " For prophylaxis, it has been suggested that the dosage of 10 mg/kg/wk should be spread over the week (3." | ( [Pharmacokinetics of antimalarials: quinine and mefloquine, halofantrine, qinghaosu, amino-4-quinolines]. Blayo, MC; Pussard, E; Verdier, F, ) | 0.13 |
| " Dose-response curves were established by measuring the acetylcholine-triggered Ca2+ mobilization in cell suspensions by means of a fluorometric assay with chlorotetracycline." | ( Chloroquine is a muscarinic antagonist. Binding and dose-response studies with chick embryo cells. Oettling, G; Schmidt, H, 1987) | 1.72 |
| " The weekly dosage of the drug was adjusted according to age." | ( The implementation of community participation in the control of malaria in rural Tanjung Pinang, Indonesia. Muzaham, F; Pribadi, W; Rasidi, R; Rukmono, B; Santoso, T, 1986) | 0.27 |
| " The shopkeeper frequently advised which drug to take and the dosage as well as selling the drugs." | ( Changes in sources of treatment occurring after inception of a community-based malaria control programme in Saradidi, Kenya. Kaseje, DC; Mburu, FM; Spencer, HC, 1987) | 0.27 |
| " With increasing dosage of monensin, secreted and intracellular ASB activity increased for both OA and normal cells." | ( Monensin stimulation of arylsulfatase B activity in human chondrocytes. Colofiore, JR; Schwartz, ER, 1986) | 0.27 |
| " We studied the efficacy of chloroquine in two patients with sarcoidosis who were unable to tolerate the dosage of corticosteroids required to control hypercalciuria and prevent the formation of renal stones." | ( The effects of chloroquine on serum 1,25-dihydroxyvitamin D and calcium metabolism in sarcoidosis. Cohanim, M; Jones, G; Lohnes, D; O'Leary, TJ; Yendt, ER; Yip, A, 1986) | 0.92 |
| " The mode of action of chloroquine and the possible consequences of the findings for dosage of chloroquine when used for malaria prophylaxis is discussed." | ( Effect of chloroquine on human lymphocyte proliferation. Bygbjerg, IC; Flachs, H, 1986) | 0.98 |
| " To reduce the physiological alterations induced by NSAIDs, short-half-life drugs such as ibuprofen, flurbiprofen or ketoprofen should be used at the maximally tolerable dosage interval." | ( Antirheumatic medication in pregnancy. Brooks, PM; Needs, CJ, 1985) | 0.27 |
| "For the past 300 years antimalarial dosage regimens have not been based on pharmacokinetic information." | ( Clinical pharmacokinetics of antimalarial drugs. White, NJ, ) | 0.13 |
| " In groups 1, 2, and 3 the dosages of chloroquine base administered alone were adjusted to body weight, surface area of subject, and age; in group 4 a combination of chloroquine diphosphate and pyrimethamine was given at a standard dosage related to age." | ( Effect of four different types of single-dose treatment with chloroquine and with chloroquine and pyrimethamine on Plasmodium falciparum infections in a semi-immune population in northern Nigeria. Kusnecov, R; Lietaert, P; Storey, J, 1972) | 0.76 |
| " Preliminary results seem to indicate, that the dosage used may be reduced slowly and therapy finally stopped after 3-4 years of treatment in most patients." | ( [Therapy of chronic hepatitis (author's transl)]. Arnold, W; Meyer zum Büschenfelde, KH, 1981) | 0.26 |
| " The dose-response curve was steep, nearly all incorporation being inhibited by 2 x IC50." | ( Inhibition of lymphocyte transformation by mepacrine and chloroquine. Trist, DG; Weatherall, M, 1981) | 0.51 |
| " Group II: 26 children were treated with quinine at the dosage adjusted to the body surface area based on an adult dose of 500 mg base eight hourly for 14 days." | ( In vivo and in vitro sensitivity of Falciparum malaria to quinine in Thai children. Attanath, P; Chongsuphajaisiddhi, T; Sabcharoen, A, 1981) | 0.26 |
| " The dose-response curves of inhibition of mitogen-induced lymphocyte activation for chloroquine and methylamine are very steep and are similar to the dose-response curves obtained with dimaprit and nordimaprit, but very different from the flat dose-response curves previously described for histamine." | ( A comparison of dimaprit, nordimaprit, methylamine and chloroquine as inhibitors of mitogen-induced lymphocyte activation. Dale, MM; Ladd, R, 1984) | 0.74 |
| " The clinical and parasitological responses were satisfactory with all three dosage regimens." | ( A phase II clinical trial of mefloquine in patients with chloroquine-resistant falciparum malaria in Thailand. Bunnag, D; Harinasuta, T; Wernsdorfer, WH, 1983) | 0.51 |
| " The KZ1 isolate from East Africa had an intermediate level of chloroquine resistance and a flat dose-response curve and each of its clones had a similar dose-response curve, indicating that the intermediate level of chloroquine resistance did not result from the KZ1 isolate's being a mixture of clones with high and low sensitivity." | ( Drug sensitivity and isoenzyme type in cloned lines of Plasmodium falciparum. Carter, R; Graves, PM; Keystone, JS; Seeley, DC, 1984) | 0.51 |
| " falciparum infections during the year died, and (v) increasing the dosage of chloroquine base from 15 to 25 to 37." | ( Absence of malaria mortality in villagers with chloroquine-resistant Plasmodium falciparum treated with chloroquine. Campbell, JR; Harun, S; Hoffman, SL; Hussein, PR; Marwoto, HA; Masbar, S; Smrkovski, L; Soewarta, A; Wiady, I, 1984) | 0.75 |
| "The clindamycin dose-response curves observed with both chloroquine-resistant and chloroquine-susceptible strains of Plasmodium falciparum in vitro demonstrated a plateau region that extended from 10(-2) to 10(1) micrograms/ml of drug (22 nM to 22 microM)." | ( Clindamycin activity against chloroquine-resistant Plasmodium falciparum. Brodasky, TF; Gluzman, IY; Krogstad, DJ; Parquette, AR; Phillips, GW; Seaberg, LS, 1984) | 0.81 |
| " The higher dosage of chloroquine caused no exacerbations." | ( Effect of antimalarial drugs on psoriasis. Kuflik, EG, 1980) | 0.58 |
| " Reappraisal of quinine therapy has led to important modifications in dosage recommendations and recognition of a major complication of severe malaria associated with its use--hypoglycaemia." | ( Management of Plasmodium falciparum malaria. Phillips, RE, 1984) | 0.27 |
| " Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines." | ( Pharmacologic actions of 4-aminoquinoline compounds. Mackenzie, AH, 1983) | 0.27 |
| " Currently recommended dosage schedules appear to be too high in certain cases." | ( Steady state disposition of chloroquine in patients with rheumatoid disease. Bergqvist, Y; Domeij-Nyberg, B; Frisk-Holmberg, M, 1983) | 0.56 |
| " The present knowledge of CQ kinetics could provide a basis for revision of current dosage regimens in malaria suppression and rheumatoid disease to ensure efficacious and safe therapy." | ( The single dose kinetics of chloroquine and its major metabolite desethylchloroquine in healthy subjects. Bergqvist, Y; Domeij-Nyberg, B; Frisk-Holmberg, M; Termond, E, 1984) | 0.56 |
| " Chloroquine rapidly crossed the placenta, resulting in equivalent fetal and maternal blood concentrations 15-30 min after dosing the mother." | ( Placental transfer of chloroquine in pregnant rabbits. Akintonwa, A; Meyer, MC; Yau, MK, 1983) | 1.49 |
| " We treated rats with chloroquine in a dosage schedule sufficient to cause a 35% increase in liver phospholipid content." | ( Chloroquine treatment does not cause phospholipid storage by depleting rat liver lysosomes of acid phospholipase A. Hostetler, KY; Reasor, MJ, 1984) | 2.02 |
| ") inhibited AA in the same dosing regimen." | ( [Studies of D-penicillamine (5): effects on rat adjuvant arthritis (author's transl)]. Higuchi, S; Kimura, M; Nakaike, S; Ohzeki, M; Otomo, S; Sasajima, M; Tarumoto, Y, 1981) | 0.26 |
| " These phospholipase A2 inhibitors also inhibited the cellular uptake of 45Ca2+ evoked by carbamylcholine with similar dose-response curves to those for inhibition of catecholamine secretion." | ( Suppression by phospholipase A2 inhibitors of secretion of catecholamines from isolated adrenal medullary cells by suppression of cellular calcium uptake. Izumi, F; Kobayashi, H; Sakurai, S; Wada, A; Yanagihara, N, 1983) | 0.27 |
| " I therefore consider these dosage rates safe, since they are below the threshold of retinal toxicity." | ( Dose refinements in long-term therapy of rheumatoid arthritis with antimalarials. Mackenzie, AH, 1983) | 0.27 |
| " Documented cases of resistance have been reported from all the countries of the region, and dosage schedules of various antimalarials have to be modified and combination of drugs used when treating such cases." | ( Chemotherapy of malaria. Ponnampalam, JT, 1981) | 0.26 |
| " It was less effective in a single daily dose of 4 mg/kg body-weight for four days, when it cured only five out of nine patients, while a dosage of 4 mg/kg body-weight for seven days cured 23 out of 26 patients." | ( Doxycycline in the treatment of falciparum malaria among aborigine children in West Malaysia. Ponnampalam, JT, 1981) | 0.26 |
| "Responses of parasitemia and fever in vivax malaria to standard doses of chloroquine and different dosage schedules of co-trimoxazole were compared in 165 children." | ( A comparative trial of oral chloroquine and oral co-trimoxazole in vivax malaria in children. Lal, H, 1982) | 0.79 |
| "14 mumol/litre of blood, which is the discriminating dosage for resistance at RI level." | ( Incipient resistance of Plasmodium falciparum to chloroquine among a semi-immune population of the United Republic of Tanzania. 1. Results of in vivo and in vitro studies and of an ophthalmological survey. Almeida Franco, J; Grab, B; Grab, D; Horst, HI; Joia, H; Onori, E; Payne, D, 1982) | 0.52 |
| " Many of these reviews, while generally excellent, have propagated some apparent misconceptions by disregarding or de-emphasizing data suggesting that irreversible retinal toxicity due to antimalarials can be easily avoided by judicious daily dosage and regular ophthalmologic follow-up." | ( Antimalarials and ophthalmologic safety. Olansky, AJ, 1982) | 0.26 |
| " This deminished absorption reflected the fact that chloroquine bioavailability after oral dosing has recently been shown to be decreased by kaolin." | ( Examination of the chloroquine-kaolin drug absorption interaction using the buccal partitioning model. D'Arcy, PF; McElnay, JC; Sidahmed, AM, 1982) | 0.84 |
| " The psychosis disappeared after cessation of the drug, combined with or without the use of low dosage phenothiazines in excited patients." | ( Chloroquine psychosis: a chemical psychosis? Mohan, D; Mohandas, E; Rajat, R, 1981) | 1.71 |
| " The recommended dosage is 0,5 mg/kg body mass of primaquine base." | ( Chemotherapy of Babesia felis infection: efficacy of certain drugs. Potgieter, FT, 1981) | 0.26 |
| " We wounder whether check-ups of these patients remain necessary when dosage of chloroquine or its equivalent is below 75 g per year." | ( Ophthalmological examination of patients taking chloroquine. Graniewski-Wijnands, HS; van Lith, GH; Vijfvinkel-Bruinenga, S, 1980) | 0.74 |
| " Most probably this is due to the low dosage of chloroquine which is used nowadays." | ( Interpretation of the electro-oculogram of patients taking chloroquine. Kok, GA; Reijmer, CN; Tijssen, JG; van Lith, GH, 1980) | 0.76 |
| " A sigmoidal dose-response curve is followed with 50% hemolysis being produced by 4 microM FP." | ( Hemolysis of mouse erythrocytes by ferriprotoporphyrin IX and chloroquine. Chemotherapeutic implications. Chou, AC; Fitch, CD, 1980) | 0.5 |
| " Based on these observations and the fact that authors who have observed an inhibition of the collagen synthesis have used an uncomparibly higher dosage per kilogram of body weight, the authors of this report are so far of the opinion that the dosage they are using (300-600 mg/day) does not significantly influence the speed of wound healing." | ( [D-penicillamine and wound healing in patients with rheumatoid arthritis]. Bamert, W; Stojan, B; Wiedmer, U, ) | 0.13 |
| " Chloroquine decreased the action of native insulin on glycogen synthesis, but did not affect the dose-response characteristics of encapsulated insulin." | ( Biological effects of encapsulated insulin on transfected Chinese hamster ovary cells. Aunis, D; Crémel, G; Hubert, P; Roques, M, 1995) | 1.2 |
| " Dose-response curves were established for (a) the intracellular accumulation of 35S-GAGs and (b) the release of beta-hexosaminidase after exposure (72 hr) to tilorone (1-35 microM)." | ( Tilorone-induced lysosomal storage of sulphated glycosaminoglycans can be separated from tilorone-induced enhancement of lysosomal enzyme secretion. Lüllmann-Rauch, R; Pods, R; Von Witzendorff, B, 1995) | 0.29 |
| " vivax malaria and seven healthy male Thais, after the standard oral dosage regimen of CQ (a total dose of 1500 mg given over 3 days)." | ( The pharmacokinetics of chloroquine in healthy Thai subjects and patients with Plasmodium vivax malaria. Karbwang, J; Limpaibul, L; Na-Bangchang, K; Tan-Ariya, P; Thanavibul, A, 1994) | 0.6 |
| "Patients with active RA diagnosed at age > or = 60 were randomized to receive prednisone (15 mg/day for 1 month, with the dosage tapered as low as possible thereafter) (n = 28) or chloroquine (n = 28)." | ( Prednisone treatment of elderly-onset rheumatoid arthritis. Disease activity and bone mass in comparison with chloroquine treatment. Breedveld, FC; Dijkmans, BA; Han, KH; Papapoulos, S; Pauwels, EK; Valkema, R; van Schaardenburg, D; Zwinderman, AH, 1995) | 0.7 |
| " Although Plasmodium falciparum has developed resistance to many antimalarial drugs, including chloroquine, resistance may be attributed, among other factors, to subclinical dosage of chloroquine from administered pharmaceutical forms." | ( Slow release of chloroquine phosphate from multiple taste-masked W/O/W multiple emulsions. Vaziri, A; Warburton, B, ) | 0.7 |
| " Our results failed to demonstrate an association between a weekly chloroquine dosing regimen and drug-induced retinopathy." | ( No evidence for chloroquine-associated retinopathy among missionaries on long-term malaria chemoprophylaxis. Contoreggi, CS; Frame, JD; Frankenfield, DL; Lange, WR; Moriarty-Sheehan, M, 1994) | 0.87 |
| "In recent years major advances have been made in the clinical pharmacology of many drugs used for the treatment of tropical diseases, particularly in the design and development of dosage regimens for the treatment of severe malaria." | ( Clinical pharmacokinetics in the treatment of tropical diseases. Some applications and limitations. Edwards, G; Ward, SA; Winstanley, PA, 1994) | 0.29 |
| "Various commercial preparations of chloroquine dosage forms have been examined both by thin-layer chromatography (TLC) and liquid chromatography (LC)." | ( Determination of chloroquine and its decomposition products in various brands of different dosage forms by liquid chromatography. Abdelrahman, AN; Ibrahim, KE; Karim, EI, 1994) | 0.91 |
| "01); mean dosage of inhibition dropped 15." | ( [Longitudinal surveillance of chloroquine resistance of Plasmodium falciparum after cessation of medication in south Yunnan]. Che, LG; Chen, WC; Dong, Y; He, H; Liu, DQ; Liu, RJ; Yang, HL; Yang, PF; Zhan, B; Zhang, CY, 1994) | 0.58 |
| " Dosage was 25 mg/kg chloroquine base delivered over three days." | ( Chloroquine resistant Plasmodium falciparum in coastal Tanzania. A challenge to the continued strategy of village based chemotherapy for malaria control. Minjas, JN; Premji, Z; Shiff, CJ, 1994) | 2.05 |
| "500 mg chloroquine base corresponding to the accepted dosage of the drug in malarial chemotherapy." | ( Chloroquine excretion in semen following antimalarial-drug administration. Adeeko, AO; Dada, OA, ) | 2.03 |
| " To reduce the side effects, another test was carried out in 3 monkeys and the dosage regimen was modified to pyronaridine 6 mg/kg-artemether 10 mg/kg-chloroquine 20 mg/kg (PAC-2) once daily for 3 days." | ( [Studies on the establishment of malarial animal model of short-term relapse. III. Combined therapy with pyronaridine-artemether-chloroquine for parasitemia clearance]. Fang, Y; Lin, BY; Pan, YR; Zhang, JX; Zheng, H, 1993) | 0.69 |
| " The investigations undertaken by the Pasteur Institute of Madagascar, by the Institute for Tropical Medicine and Epidemiology in Paris and by the Unit of Epidemiological Surveillance within the Malagasy Ministry of Health raise a number of questions: Taking to account the various causes for imprecision in measurement and in evaluation (variations in parasite density, microscopic detection levels, bio-availability of the drug) of the groups of R I and R II how significant are the variations observed in numbers and proportions of resistance levels R I and R II? How important are the effects of auto-medication? Can they be correctly evaluated by Bergquist's test? How explain the low level of drug resistance in a country close to East Africa, in which chemoprophylaxis has been widely practiced and in which insufficient dosage for treatment is common? The absence of R III resistance in vivo permit for chloroquine to remain the first line treatment for malaria in Madagascar." | ( [Evolution of Plasmodium falciparum drug sensitivity in Madagascar from 1982 to 1993 and operational consequences]. Blanchy, S; Rakotonjanabelo, A; Ranaivoson, G, 1993) | 0.43 |
| " For oxytetracycline, flucloxacillin and amoxycillin, the conventional bioavailability parameters indicated partial equivalence whereas using the te and to parameters, more realistic indications of the possible extent of the performance of a drug from dosage forms were obtained than with the conventional bioequivalence parameters." | ( The application of new bioavailability parameters in the bioequivalence testing of antimicrobial agents. Ellis, SM; Koeleman, HA; Steyn, HS; Wessels, JC, 1993) | 0.29 |
| " With a daily dosage regimen, the divergent pharmacokinetic behaviour of chloroquine enantiomers generates a calculated R:S ratio of blood concentrations amounting to 1:0." | ( Stereoselective pharmacokinetic properties of chloroquine and de-ethyl-chloroquine in humans. Augustijns, P; Verbeke, N, 1993) | 0.78 |
| "The effects of 3-day oral chloroquine phosphate treatment administered at a dosage of 250 mg four times daily on fasting serum levels of lipids, lipoproteins, and apolipoproteins were studied in 20 patients with non-insulin-dependent diabetes mellitus (NIDDM)." | ( Effects of chloroquine on the dyslipidemia of non-insulin-dependent diabetes mellitus. Jones, RH; Powrie, JK; Shojaee-Moradie, F; Smith, GD; Sönksen, PH; Watts, GF, 1993) | 0.98 |
| "In a randomized trial, a high dosage chloroquine monotherapy (45 mg/kg over 3 days) was compared with combination regimens of sulfadoxine/pyrimethamine and chloroquine/clindamycin for treating Gabonese school children with Plasmodium falciparum malaria." | ( Sulfadoxine/pyrimethamine or chloroquine/clindamycin treatment of Gabonese school children infected with chloroquine resistant malaria. Bienzle, U; Graninger, W; Kremsner, PG; Metzger, W; Mordmüller, B, 1995) | 0.86 |
| " It also appears that although the individual enantiomers show minimal embryotoxicity at the dosage used, they potentiate each other's effects in the racemic mixture." | ( Effects of chloroquine and its enantiomers on the development of rat embryos in vitro. Ofori-Adjei, D; Tagoe, CN, 1995) | 0.68 |
| "In 30 patients (20 males and 10 females) wih psoriatic arthritis chloroquine was administered in a dosage of 250 mg daily per os." | ( [Chloroquine in the treatment of psoriatic arthritis]. Grazio, S; Jajić, I; Jajić, Z, 1995) | 1.44 |
| " All drug dosing was performed under supervision by the study team, making this an evaluation of intervention efficacy (excluding the role of patient compliance)." | ( Objectives and methodology in a study of malaria treatment and prevention in pregnancy in rural Malawi: The Mangochi Malaria Research Project. Breman, JG; Heymann, DL; Khoromana, CO; Slutsker, WL; Steketee, RW; Wirima, JJ, 1996) | 0.29 |
| " The dosage parameters associated with retinopathy are still uncertain as well as the best way to screen for it but the dosage/kg body weight appears to be important." | ( Retinopathy and antimalarial drugs--the British experience. Spalton, DJ, 1996) | 0.29 |
| " Thus, the clinical dosing required for these compounds would probably be greater for chloroquine-resistant strains than for chloroquine-susceptible strains." | ( 4-aminoquinoline analogs of chloroquine with shortened side chains retain activity against chloroquine-resistant Plasmodium falciparum. Dorn, A; Girometta, MA; Guenzi, A; Hofheinz, W; Huber, W; Jaquet, C; Jolidon, S; Masciadri, R; Matile, H; Peters, W; Richter, WF; Ridley, RG; Thaithong, S; Urwyler, H, 1996) | 0.81 |
| " Whole blood chloroquine levels on the last day of dosing confirmed normal absorption (range 413-3248, mean 1141, SD 616 ng/mL)." | ( Survey of resistance to chloroquine by Plasmodium vivax in Indonesia. Baird, JK; Basri, H; Dewi, RM; Khairani, M; Leksana, B; Masbar, S; Sustriayu Nalim, MF; Tjitra, E; Wignall, FS, ) | 0.81 |
| "Treatment failure of chloroquine in standard dosage (25 mg/kg)." | ( Risk factors of chloroquine resistance in Plasmodium falciparum malaria. Cowdrey, D; Hess, FI; Iannuzzi, A; Leafasia, J; Löscher, T; Nothdurft, HD; Rieckmann, KH; Von Sonnenburg, F, 1996) | 0.96 |
| " A total dose of 3 mg/kg of WR 238605 given at a dosage of 1 mg/kg/day for three days cleared patent parasites in all eight monkeys but recrudescence of parasitemia occurred 15-25 days after initiation of treatment." | ( WR 238605, chloroquine, and their combinations as blood schizonticides against a chloroquine-resistant strain of Plasmodium vivax in Aotus monkeys. Cooper, RD; Kyle, DE; Nuzum, EO; Obaldia, N; Rieckmann, KH; Rossan, RN; Shanks, GD, 1997) | 0.69 |
| " This malaria parasite was sensitive to standard dosage of either chloroquine or sulphadoxine-pyrimethamine." | ( Malaria in Mvumi, central Tanzania and the in vivo response of Plasmodium falciparum to chloroquine and sulphadoxine pyrimethamine. Mboera, LE; Ndawi, BT; Wakibara, JV, 1997) | 0.76 |
| " The dosage is empirically based." | ( Chloroquine blood concentrations and malaria prophylaxis in Tanzanian women during the second and third trimesters of pregnancy. Aden Abdi, Y; Diwan, VK; Ericsson, O; Gustafsson, LL; Kilewo, C; Massele, AY; Rimoy, G; Tomson, G, 1997) | 1.74 |
| " A high dosage of chloroquine seemed to reduce the OHC loss in albino, but not in black or red guinea pigs." | ( Hair cell loss from acoustic trauma in chloroquine-treated red, black and albino guinea pigs. Barrenäs, ML, ) | 0.73 |
| " Third, internalization of lipase-enriched lipoproteins via syndecan-1 and of clustered IgGs via the chimera showed identical kinetics (t1/2 = 1 h) and identical dose-response sensitivities to cytochalasin B, which disrupts microfilaments, and to genistein, which inhibits tyrosine kinases." | ( The syndecan family of proteoglycans. Novel receptors mediating internalization of atherogenic lipoproteins in vitro. Fisher, EA; Fuki, IV; Iozzo, RV; Kuhn, KM; Lomazov, IR; Rothman, VL; Swenson, TL; Tuszynski, GP; Williams, KJ, 1997) | 0.3 |
| " Probit analysis of log dose-response was used to determine effective concentrations EC50, EC90 and EC99 to the studied drugs." | ( In vivo and in vitro Plasmodium falciparum resistance to chloroquine, amodiaquine and quinine in the Brazilian Amazon. di Santi, SM; Segurado, AA; Shiroma, M, ) | 0.38 |
| " Despite the dosage employed, the frequency and duration of use, and excretion primarily through the bowels as the active parent compound, primaquine appeared to have little or no significant effect against a variety of common intestinal parasites." | ( Intestinal parasite infections after extended use of chloroquine or primaquine for malaria prevention. Basri, H; Fryauff, DJ; Jones, TR; Mouzin, E; Prodjodipuro, P; Subianto, B; Widjaja, H, 1998) | 0.55 |
| " All sanctioned providers limited their first choices of antimalarial drug to those recommended by the national malaria control program and reported using correct dosing regimens." | ( Use of antimalarial drugs in Mali: policy versus reality. Dicko, A; Diop, S; Djimde, A; Doumbo, O; Plowe, CV; Wellems, TE, 1998) | 0.3 |
| "The stability of five drugs commonly prescribed for use in oral liquid dosage forms but not commercially available as such was studied." | ( Stability of alprazolam, chloroquine phosphate, cisapride, enalapril maleate, and hydralazine hydrochloride in extemporaneously compounded oral liquids. Allen, LV; Erickson, MA, 1998) | 0.6 |
| " This study was done to assess the quality of chloroquine dosage forms in Kampala." | ( Quality of oral and parenteral chloroquine in Kampala. Odyek, O; Ogwal-Okeng, JW; Okello, DO, 1998) | 0.84 |
| " Patients should be dosed on the basis of ideal body weight (not actual body weight) to reduce the incidence of macular toxicity." | ( Detection and prevention of maculopathy associated with antimalarial agents. Easterbrook, M, 1999) | 0.3 |
| "Chloroquine diphosphate was administered intraperioneally to two groups of adult male rats at two dosage levels of 5 mg base/kg body weight and 10 mg base/kg body weight." | ( Chloroquine reduces fertilizing capacity of epididyma sperm in rats. Adeeko, AO; Dada, OA, ) | 3.02 |
| " While most patients with tertian malaria were cured with the standard chloroquine and primaquine regimen, a higher dosage was required for one case acquired in Papua New Guinea." | ( Imported malaria: successful treatment of 31 patients in the era of chloroquine resistance. Chang, HL; Chang, SC; Chen, YC; Fang, CT; Hsieh, WC; Hsueh, PR; Hung, CC, 1999) | 0.77 |
| " With prudent dosage and monitoring, these agents can be used safely and effectively in the treatment and management of dermatologic disease." | ( Antimalarials. Piette, WW; Van Beek, MJ, 2001) | 0.31 |
| " Further research is needed to determine the best dosage regimen for antimalarial drugs used for chemoprophylaxis in children." | ( Antimalarial chemoprophylaxis in infants and children. Kramer, MH; Lobel, HO, 2001) | 0.31 |
| " For optimal efficacy, treatment regimens must be adjusted with regard to dosage of primaquine and association with halofantrine, mefloquine or other new antimalarial agents." | ( [Epidemiological and therapeutic aspects of plasmodial infection from Plasmodium vivax]. Granier, H; Klotz, F; Martin, J; Nicolas, X, 2000) | 0.31 |
| " The latter is defined as regular intake of antimalarial drugs in subtherapeutic dosage in order to suppress the development of clinical disease." | ( [Malaria--chemoprophylaxis 2001]. Beck, B; Blum, J; Funk, M; Furrer, H; Genton, B; Hatz, FR; Holzer, B; Loutan, L; Markwalder, K; Raeber, PA; Schlagenhauf, P; Siegl, G; Steffen, R; Stürchler, D; Wyss, R, 2001) | 0.31 |
| "Non-compliance to correct dosing is thought to be one of the main causes of treatment failure of chloroquine in the home management of childhood malaria." | ( Compliance to correct dose of chloroquine in uncomplicated malaria correlates with improvement in the condition of rural Nigerian children. Akpala, CO; Mbah, AU; Nwaiwu, O; Okafor, HU; Okonkwo, PO, ) | 0.64 |
| " The recommended dosage of chloroquine to be administered over three days was 25 mg/kg but the median chloroquine tablet or syrup dosage given over the first three days of treatment was 15 mg/kg." | ( Malaria control in Bungoma District, Kenya: a survey of home treatment of children with fever, bednet use and attendance at antenatal clinics. Deming, MS; Hamel, MJ; Odhacha, A; Roberts, JM, 2001) | 0.61 |
| " The administration of incorrect dosages, which proved common with chloroquine, may occur less frequently with sulfadoxine-pyrimethamine, as its dosage regimen is simpler." | ( Malaria control in Bungoma District, Kenya: a survey of home treatment of children with fever, bednet use and attendance at antenatal clinics. Deming, MS; Hamel, MJ; Odhacha, A; Roberts, JM, 2001) | 0.55 |
| "The cytotoxicity of the selected systemic and intravitreally dosed drugs tamoxifen, toremifene, chloroquine, 5-fluorouracil, gentamicin and ganciclovir was studied in retinal pigment epithelium (RPE) in vitro." | ( Evaluation of the cytotoxicity of selected systemic and intravitreally dosed drugs in the cultures of human retinal pigment epithelial cell line and of pig primary retinal pigment epithelial cells. Diehl, H; Engelke, M; Huhtala, A; Mäenpää, H; Mannerström, M; Mäntylä, E; Mäntylä, M; Marselos, M; Pappas, P; Salminen, L; Tähti, H; Toimela, T; Uusitalo, H; Zorn-Kruppa, M, 2002) | 0.53 |
| " But children did not receive the recommended dosage of chloroquine because of lack of compliance on the parts of providers as well as users of health care." | ( Appropriate treatment of malaria? Use of antimalarial drugs for children's fevers in district medical units, drug shops and homes in eastern Uganda. Kristensen, M; Nshakira, N; Ssali, F; Whyte, SR, 2002) | 0.56 |
| "All cases arose because of failure by physicians to avoid dosing above published safe levels." | ( Hydroxychloroquine and chloroquine retinopathy: screening for drug toxicity. Browning, DJ, 2002) | 0.77 |
| "A dose-response relationship for hydroxychloroquine (HCQ), in terms of the proportion of patients achieving the Paulus 20% criteria for improvement, had previously been observed in patients with rheumatoid arthritis (RA) receiving a 6-week loading regimen of 400, 800, or 1,200 mg HCQ daily." | ( Hydroxychloroquine concentration-response relationships in patients with rheumatoid arthritis. Baethge, BA; Botstein, GR; Caldwell, J; Dietz, F; Ettlinger, R; Furst, DE; Gibbs, JP; Golden, HE; Lindsley, H; McLaughlin, GE; Moreland, LW; Munster, T; Roberts, WN; Rooney, TW; Rothschild, B; Sack, M; Sebba, AI; Shen, D; Weisman, M; Welch, KE; Yocum, D, 2002) | 1.04 |
| " The four drivers had been treated with chloroquine and proguanil but the dosage may have been insufficient with regard to their body weight (average weight = 110 kg)." | ( [A collective malarial infestation during a humanitarian mission in west Africa]. Beytout, J; Caumon, L; Chouaki, M; Cueto, T; Delort, P; Dufraise, S; Monchard, F; Philippe, JM; Rimeize, H, 2002) | 0.58 |
| " Chloroquine was administered on a dosage of 25 mg/kg, spread over three days." | ( [Therapeutic efficacy of chloroquine in the uncomplicated malaria due to Plasmodium falciparum in hospital patients in central Ivory Coast (1997-2000)]. Adou-Bryn, KD; Akoussi, CF; Assoumou, A; Boni, NM; Ehouman, A; Krelo, K; Ouhon, J; Penali, LK; Yapo, GC, 2002) | 1.53 |
| " As a consequence, tests of parasite susceptibility to chloroquine in vitro were repeated using the same protocol except for the replacement of previously used commercially available predosed WHO culture plates by independently dosed plates." | ( Reassessment of the resistance of Plasmodium falciparum to chloroquine in Gabon: implications for the validity of tests in vitro vs. in vivo. Adegnika, AA; Binder, RK; Borrmann, S; Issifou, S; Kremsner, PG; Missinou, MA; Ramharter, M; Wernsdorfer, WH, ) | 0.62 |
| "The patient was given chloroquine by his captain in a dosage regimen appropriate for quinine (2 tablets 3 times daily for 7 d)." | ( Toxicity related to chloroquine treatment of resistant vivax malaria. Barrett, PH; Davis, TM; Ilett, KF; Syed, DA, 2003) | 0.96 |
| " For drugs with a narrow therapeutic index such as chloroquine, recommended dosing regimens should be respected, and adequate information sources must be available where such drugs are dispensed by untrained personnel." | ( Toxicity related to chloroquine treatment of resistant vivax malaria. Barrett, PH; Davis, TM; Ilett, KF; Syed, DA, 2003) | 0.89 |
| "The in vivo use of chloroquine is effective for promoting gene delivery to the liver, but requires multiple dosing and is limited by systemic toxicity." | ( The in vivo use of chloroquine to promote non-viral gene delivery to the liver via the portal vein and bile duct. Collins, L; Dong, X; Fabre, JW; Qiu, Y; Sawyer, GJ; Zhang, X, 2003) | 0.98 |
| "This study was carried out as a follow-up to establish the quality of chloroquine tablet and injection dosage forms in the Ugandan drug market from June - November 2001." | ( Chloroquine in the Ugandan market fails quality test: a pharmacovigilance study. Obua, C; Ogwal-Okeng, JW; Owino, E, 2003) | 2 |
| "Chloroquine tablets and injection dosage forms, randomly purchased from pharmacies and drug shops in the four regions of Uganda, were assayed for content of the active ingredient according to the USP standard, using the HPLC method." | ( Chloroquine in the Ugandan market fails quality test: a pharmacovigilance study. Obua, C; Ogwal-Okeng, JW; Owino, E, 2003) | 3.2 |
| " The weekly dosage of the drugs (300 mg of chloroquine base or 25 mg of pyrimethamine per 50 g of salt) had in each case been adjusted to the average salt consumption." | ( Chloroquine or pyrimethamine in salt as a supressive against sporozoite-induced vivax malaria (Chesson strain). BURGESS, RW; COATNEY, GR; MICKELSEN, O; PIRKLE, CI; YOUNG, MD, 1958) | 1.94 |
| " Less than 10% of cases of childhood 'malaria' had been treated with chloroquine at home, and 69% of those giving home medication did not know the correct dosage for a child." | ( Home treatment of 'malaria' in children in rural Gambia is uncommon. Bøgh, C; Clarke, SE; Lindsay, SW; Rowley, J; Walraven, GE, 2003) | 0.55 |
| "To evaluate the efficacy of two dosing regimens of cotrimoxazole in the treatment of falciparum malaria and compare the efficacy with that of chloroquine, the first-line antimalaria drug in the area of study." | ( Comparative efficacy of chloroquine and cotrimoxazole in the treatment of acute uncomplicated falciparum malaria in Nigerian children. Adedeji, AA; Fehintola, FA; Sowunmi, A, ) | 0.64 |
| "For the majority of chronic asthmatics, symptoms are best controlled using inhaled steroids, but for a small group of asthma sufferers, symptoms cannot be controlled using inhaled steroids and instead continuous use of high dosage oral steroids (corticosteroids) are required." | ( Chloroquine as a steroid sparing agent for asthma. Bara, A; Dean, T; Dewey, A; Lasserson, TJ; Walters, EH, 2003) | 1.76 |
| " Further trials should optimise oral steroid dosage before addition of the steroid-sparing agent." | ( Chloroquine as a steroid sparing agent for asthma. Bara, A; Dean, T; Dewey, A; Lasserson, TJ; Walters, EH, 2003) | 1.76 |
| " A relatively high concentration was still determined in the uveal tract even at 48 weeks after single oral dosing by whole-body autoradiography." | ( Absorption, distribution and excretion of 14C-chloroquine after single oral administration in albino and pigmented rats: binding characteristics of chloroquine-related radioactivity to melanin in-vivo. Ono, C; Tanaka, M; Yamada, M, 2003) | 0.58 |
| " g(-1) at 24 h after dosing and declined slowly with a terminal half-life of 468." | ( Absorption, distribution and excretion of 14C-levofloxacin after single oral administration in albino and pigmented rats: binding characteristics of levofloxacin-related radioactivity to melanin in vivo. Ono, C; Tanaka, M; Yamada, M, 2004) | 0.32 |
| " In view of toxicological importance of CQ metabolites, it is suggested that caution should be exercised in evaluation of higher dosage regimen of CQ in pregnant women." | ( Evidence for increased metabolism of chloroquine during the early third trimester of human pregnancy. Bolaji, OO; Chukwuani, MC; Makinde, ON; Ogunbona, FA; Onyeji, CO, 2004) | 0.6 |
| " The concentration and the extent of accumulation of radioactivity not only in melanin-containing ocular tissues but also in other non-pigmented ocular tissues, such as retina, after chronic oral administration of 14C-levofloxacin once daily for 84 days were much lower than those after multiple dosing with 14C-chloroquine under the same conditions." | ( Comparative assessment of ocular tissue distribution of drug-related radioactivity after chronic oral administration of 14C-levofloxacin and 14C-chloroquine in pigmented rats. Takashina, H; Tanaka, M; Tsutsumi, S, 2004) | 0.7 |
| " Ideal agents would be efficacious, easily dosed and administered, inexpensive, and with few adverse effects." | ( Chloroquine and hydroxychloroquine as inhibitors of human immunodeficiency virus (HIV-1) activity. Hoven, AD; Romanelli, F; Smith, KM, 2004) | 1.77 |
| " These findings demonstrate the need for better education of parents about correct dosage of first-line malaria drugs, and for particular attention in the treatment of very young children." | ( Community effectiveness of chloroquine and traditional remedies in the treatment of young children with falciparum malaria in rural Burkina Faso. Kouyate, B; Mueller, O; Razum, O; Traore, C, 2004) | 0.62 |
| " Antimalarial drug dosage was incorrect in 84% of those who initiated self-treatment." | ( [Self-treatment of fever in the northern district of Dakar, Senegal]. Diedhiou, A; Juergens-Behr, A; Lemort, JP; Ndiaye, P; Tal-Dia, A, 2006) | 0.33 |
| " For patients using chloroquine, the correlation between RNFL measurements and chloroquine dosage was assessed." | ( Retinal nerve fibre layer thickness measurements in patients using chloroquine. Bonanomi, MT; Dantas, NC; Medeiros, FA, 2006) | 0.89 |
| " Multiple chloroquine drug doses were used, revealing the existence of inverted-U dose-response relationships in every strain, allowing us to determine strain-dependent peak scratching behavior over the entire dose range." | ( Influence of genotype, dose and sex on pruritogen-induced scratching behavior in the mouse. Green, AD; Lehto, SG; Mogil, JS; Smith, SB; Young, KK, 2006) | 0.74 |
| " In another experiment, mice infected with 1 x 10(3) and 1x 10(5) pRBC were treated with an oral four-day dosage of 20 mg/kg of CQ base from days 2, 3 or 4 post-infection." | ( Chloroquine efficacy in Plasmodium berghei NK65-infected ICR mice, with reference to the influence of initial parasite load and starting day of drug administration on the outcome of treatment. Ishih, A; Matsui, K; Muregi, FW; Suzuki, T; Terada, M, 2006) | 1.78 |
| "The dose-response curves and effective concentration that resulted in a 50% inhibitory of parasitemia (IC50) of chloroquine, artemisinin, artemether and pyronaridine phosphate against Plasmodium falciparum strain FCC1/HN cultured in vitro were tested by microfluorimetric assay (MFA) and compared with those determined by microscopy-based assay." | ( [The microfluorimetric assay (MFA) in in vitro testing the sensitivity of Plasmodium falciparum to antimalarial drugs]. Hi, YC; Huang, F; Tang, LH; Wang, QM, 2006) | 0.54 |
| " Patients were treated with standard dosage of CQ and followed up for 28 days." | ( Linkage disequilibrium between two distinct loci in chromosomes 5 and 7 of Plasmodium falciparum and in vivo chloroquine resistance in Southwest Nigeria. Bolaji, OM; Fateye, BA; Folarin, OA; Gbotosho, GO; Happi, CT; Kyle, DE; Milhous, W; Oduola, AM; Sowunmi, A; Wirth, DF, 2006) | 0.55 |
| " Different primaquine dosing regimens are in use." | ( Primaquine for preventing relapses in people with Plasmodium vivax malaria. Galappaththy, GN; Omari, AA; Tharyan, P, 2007) | 0.34 |
| " Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
| " falciparum malaria infections were treated with the standard dosage of CQ and followed-up for 28 days." | ( Rapid detection of Pfcrt and Pfmdr1 mutations in Plasmodium falciparum isolates by FRET and in vivo response to chloroquine among children from Osogbo, Nigeria. Fagbenro-Beyioku, AF; Fendel, R; Kremsner, PG; Kun, JF; Ogungbamigbe, TO; Ojurongbe, O, 2007) | 0.55 |
| "A 59-year-old man took a daily dosage of 250 mg chloroquine for his rheumatoid arthritis (up to a total dose of 540 g)." | ( Electrophysiologic findings in chloroquine maculopathy. Halfeld Furtado de Mendonça, R; Maia, OO; Yukihiko Takahashi, W, 2007) | 0.88 |
| " A young patient presenting with toxic maculopathy after 57 g of hydroxychloroquine and a daily dosage of 2 mg/kg body weight prompted us to retrospectively look at our patients examined in this respect over about 1 year." | ( [Chloroquine/hydroxychloroquine: variability of retinotoxic cumulative doses]. Berndt, S; Foerster, J; Rüther, K; Schroeter, J, 2007) | 1.48 |
| " Adverse events observed after treatment with chloroquine or prednisone (chloroquine maculopathy,cataract, glaucoma) are related to dosage and duration of the treatment." | ( [Ocular changes and general condition in lupus erythematosus (SLE)--own observation]. Brydak-Godowska, J, 2007) | 0.6 |
| " Additionally, it was observed that 48% of females admitted a preference for injections over other dosage forms compared to 33." | ( The response of students to malaria and malaria therapy in a university in southwest Nigeria. Babalola, OO; Lamikanra, A, 2007) | 0.34 |
| "5% improvement in the accumulated proportion of patients (1) treated, (2) treated within 24h of illness onset, (3) treated with the recommended antimalarials, (4) treated at an adequate dosage and (5) treated for the correct duration." | ( Home-based management of fever and malaria treatment practices in Uganda. Nsungwa-Sabiiti, J; Ogwal-Okeng, J; Pariyo, G; Peterson, S; Petzold, MG; Tomson, G, 2007) | 0.34 |
| "Hydroxychloroquine was found to be significantly more effective than chloroquine in the treatment of polymorphic light eruption and can be used safely in the dosage studied in such patients with little risk of ocular toxicity." | ( Comparative study of efficacy and safety of hydroxychloroquine and chloroquine in polymorphic light eruption: a randomized, double-blind, multicentric study. Chandurkar, N; Khopkar, U; Naik, GS; Pareek, A; Sacchidanand, S, ) | 0.84 |
| " bolus drug dosing to investigate stage specific CQ effects in detail." | ( Stage independent chloroquine resistance and chloroquine toxicity revealed via spinning disk confocal microscopy. Cooper, RA; Elliott, DA; Gligorijevic, B; Purdy, K; Roepe, PD, 2008) | 0.68 |
| "1%) were the three main molecules which account for antimalarial self-treatment However the use of these molecules was inappropriate regarding the dosage (41." | ( [Self-medication in the treatment of acute malaria: study based on users of private health drug stores in Ouagadougou, Burkina Faso]. Diarra, M; Guissou, IP; Ouédraogo, LT; Somé, IT, 2008) | 0.35 |
| "In recent issues, the efficacy of chloroquine (and the dosage that may be used) in the treatment of acute chikungunya infections was discussed." | ( On chikungunya acute infection and chloroquine treatment. Boisson, V; Charrel, RN; De Lamballerie, X; Enault, S; Flahault, A; Le Grand, R; Reynier, JC; Roques, P, 2008) | 0.9 |
| " We aimed to determine the dosage of chloroquine commonly prescribed, the doses commonly taken, and whether concentration-dependent adverse events occurred in routine practice." | ( Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. Bergqvist, Y; Kofoed, PE; Rodrigues, A; Rombo, L; Ursing, J, 2009) | 2.07 |
| " The findings indicate that there was no agranulocytosis or hepatic toxicity suggesting that AQ may pose no public health risk in its wide therapeutic dosage uses." | ( Biological and haematological safety profile of oral amodiaquine and chloroquine in healthy volunteers with or without Plasmodium falciparum infection in northeast Tanzania. Akida, JA; Bygbjerg, IC; Chile, MM; Kitua, AY; Lemnge, MM; Lusingu, JP; Makunde, R; Malebo, HM; Massaga, JJ; Rønn, AM; Theander, TG, 2008) | 0.58 |
| "4%) respondents knew the correct drug, dosage and timing of IPT." | ( Perception and practice of malaria prophylaxis in pregnancy among primary health care providers in Ibadan, Nigeria. Fawole, AO; Onyeaso, NC, 2008) | 0.35 |
| "A guideline which illustrated the presentation of clinical types of malaria, the appropriate steps to take for each type and the correct dosage schedule of chloroquine (based on the age of the child) for treatment of uncomplicated malaria was developed." | ( The development of a treatment guideline for childhood malaria in rural Southwest Nigeria using participatory approach. Ajayi, IO; Bamgboye, EA; Falade, CO; Kale, O; Oladepo, O, 2009) | 0.55 |
| " Male Wistar rats were intraperitoneally injected with chloroquine diphosphate at a dosage of 50 mg/kg body weight every day." | ( Amyloid-beta accumulation caused by chloroquine injections precedes ER stress and autophagosome formation in rat skeletal muscle. Arahata, H; Fujii, N; Furuya, H; Ikezoe, K; Kira, J; Nakagawa, M; Tateishi, T, 2009) | 0.88 |
| " rhodesiense in vivo, curing three of four infected mice dosed intraperitoneally at 5 mg/kg x 4 days." | ( Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes. Bakunov, SA; Bakunova, SM; Barzcz, T; Brun, R; Chen, H; Jones, SK; Kumar, EV; Patrick, DA; Tidwell, RR; Wenzler, T; Werbovetz, KA, 2009) | 0.35 |
| " The dose-response pattern of ATM kinase activation was concordant with the transition from HRS to IRR." | ( ATM-dependent hyper-radiosensitivity in mammalian cells irradiated by heavy ions. Cao, J; Fan, S; Furusawa, Y; Okayasu, R; Xue, L; Yu, D, 2009) | 0.35 |
| " When the prescriptions were differentiated into the different dosage forms prescribed, the prescriptions containing intramuscular injections only had over 90% of the cost lost to irrational prescribing." | ( Cost implication of irrational prescribing of chloroquine in Lagos State general hospitals. Aina, BA; Taylor, O; Tayo, F, 2008) | 0.6 |
| " Each case in group A received a total dosage of 1 200 mg(base) over a 3-day period (600 mg on the first day then 300 mg daily)." | ( [Sensitivity of Plasmodium vivax to chloroquine in Laza City, Myanmar]. Liang, GL; Sun, XD; Wang, J; Zhang, ZX, 2009) | 0.63 |
| " A higher dosage per kg body mass, long therapy duration, presence of keratopathy and renal or hepatic dysfunction are probably associated with an increased risk to develop a maculopathy/retinopathy." | ( [Retinal damage by (hydroxy)chloroquine intake: published evidence for an efficient ophthalmological follow-up]. Pluta, JP; Rüther, K, 2009) | 0.65 |
| " The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model." | ( Spiroindolones, a potent compound class for the treatment of malaria. Beck, HP; Brun, R; Cohen, SB; Dartois, V; Dharia, NV; Diagana, TT; Fidock, DA; Goh, A; González-Páez, GE; Jegla, T; Keller, TH; Lakshminarayana, SB; Lee, MC; McNamara, C; Nosten, F; Plouffe, DM; Renia, L; Rottmann, M; Russell, B; Schmitt, EK; Seitz, P; Spencer, KR; Suwanarusk, R; Tan, J; Winzeler, EA; Yeung, BK; Zou, B, 2010) | 0.36 |
| " Individual and weight-adapted dosing is especially essential for chloroquine." | ( Evaluation of risk factors for retinal damage due to chloroquine and hydroxychloroquine. Bergholz, R; Rüther, K; Schroeter, J, 2010) | 0.85 |
| " The implementation of this assay to the screening of a highly diverse academic chemical library of 14,300 molecules yielded, after secondary assays and generation of dose-response curves, the identification of two natural product inhibitors, cyanidin and delphinidin." | ( Identification by high-throughput screening of inhibitors of Schistosoma mansoni NAD(+) catabolizing enzyme. Haiech, J; Hibert, M; Kellenberger, E; Kuhn, I; Lobstein, A; Muller-Steffner, H; Rognan, D; Said-Hassane, F; Schuber, F; Villa, P, 2010) | 0.36 |
| " Representative compounds 8e and 9c showed good causal prophylactic activity in Rhesus monkeys dosed 30 mg/kg/day for 3 consecutive days by IM, delayed patency for 19-21 days and 54-86 days, respectively, as compared to the untreated control." | ( New imidazolidinedione derivatives as antimalarial agents. Kozar, MP; Lin, AJ; Luong, T; Melendez, V; Sathunuru, R; Zhang, L, 2011) | 0.37 |
| "The prior recommendation emphasized dosing by weight." | ( Revised recommendations on screening for chloroquine and hydroxychloroquine retinopathy. Kellner, U; Lai, TY; Lyons, JS; Marmor, MF; Mieler, WF, 2011) | 0.64 |
| " We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
| " CQ showed a delayed dose-response relationship in the murine malaria model and additive efficacy when combined with DHA." | ( Pharmacokinetics, pharmacodynamics, and allometric scaling of chloroquine in a murine malaria model. Batty, KT; Ilett, KF; Jago, JD; Moore, BR; Page-Sharp, M; Stoney, JR, 2011) | 0.61 |
| " Each analogue reduced parasitemia by more than 90% after 25 (mg/kg)/day dosing and in some cases provided a cure." | ( Antimalarial activity of natural and synthetic prodiginines. Alhamadsheh, M; Challis, GL; Haynes, SW; Kelly, JX; Papireddy, K; Reynolds, KA; Salem, SM; Smilkstein, M, 2011) | 0.37 |
| "Simplification of dosage regimes, consistency of information provided between different medical briefs and emphasis of the threat from malaria in Belize significantly improved compliance with antimalarial chemoprophylaxis." | ( Improvements in compliance with medical force protection measures by simplification of the anti-malarial chemoprophylaxis regime. Green, AD; Ross, DA; Sellers, EL, 2011) | 0.37 |
| " This results in dosing large number of animals and generating composite PK profile." | ( A modified serial blood sampling technique and utility of dried-blood spot technique in estimation of blood concentration: application in mouse pharmacokinetics. Kurawattimath, V; Mandlekar, S; Mariappan, TT; Pocha, K; Trivedi, RK, 2012) | 0.38 |
| " The identification and dosage of active pharmaceutical ingredients in the tablets, dissolution rate, hardness and the friability of CQ tablets were performed according to the United States Pharmacopeia (USP) and European Pharmacopoeia (Eur." | ( Quality of chloroquine tablets available in Africa. Al-Adhroey, AH; Al-Mekhlafi, HM; Amood Al-Kamarany, M; Bouklouze, A; Cherrah, Y; Elkarbane, M; Sawadogo, CW, 2011) | 0.76 |
| " Cumulative dosage had a statistically significant correlation with anterior keratocyte density, the number of sub-basal nerves and the density of abnormal particles." | ( Chloroquine keratopathy of rheumatoid arthritis patients detected by in vivo confocal microscopy. He, D; He, L; Ma, X; Xu, J, 2012) | 1.82 |
| " By taking a novel functional genomics strategy, which employs a unique combination of genome-wide drug-gene synthetic lethality (DGSL), gene-gene synthetic lethality (GGSL), and dosage suppression (DS) screens in the model organism Saccharomyces cerevisiae and is thus termed SL/DS for simplicity, we found that CQ inhibits the thiamine transporters Thi7, Nrt1, and Thi72 in yeast." | ( Discovering thiamine transporters as targets of chloroquine using a novel functional genomics strategy. Chen, K; Huang, Z; Li, W; Li, Y; Pan, X; Quiocho, FA; Srinivasan, S; Zhang, J, 2012) | 0.63 |
| " The treatment of malaria in young children and the relative benefits of age- and weight-based dosing need further exploration." | ( Monitoring antimalarial drug resistance in India via sentinel sites: outcomes and risk factors for treatment failure, 2009-2010. Anvikar, AR; Arora, U; Bhatt, RM; Das, MK; Dhariwal, AC; Ghosh, SK; Gupta, R; Kaitholia, K; Kumar, A; Mishra, N; Shah, NK; Sharma, SK; Singh, JP; Sonal, GS; Srivastava, B; Valecha, N, 2012) | 0.38 |
| "Rheumatoid arthritis (RA) patients who had taken CQ for at least 6 months and stable CQ dosage for at least 2 months were included." | ( Prevalence and risk factors for chloroquine maculopathy and role of plasma chloroquine and desethylchloroquine concentrations in predicting chloroquine maculopathy. Arromdee, E; Boonprasert, R; Chandranipapongse, W; Chatsiricharoenkul, S; Chiowchanwisawakit, P; Danwiriyakul, W; Katchamart, W; Koolvisoot, A; Nilganuwong, S; Pongnarin, P; Ruangvaravate, N; Srinonprasert, V, 2013) | 0.67 |
| " The study was designed to have a 5% type 1 error and 90% power to show whether tinidazole would produce a relapse rate of less than 20% or greater than 45% through Day 63 of weekly follow-up after initiation of treatment and initial parasite clearance with 3 days of an oral weight based dosing of chloroquine and five days of 2 grams/day of tinidazole." | ( Triangular test design to evaluate tinidazole in the prevention of Plasmodium vivax relapse. Cheah, PY; Lwin, KM; Macareo, L; Miller, RS; Nosten, F; Yuentrakul, P, 2013) | 0.57 |
| "Randomized controlled trials (RCTs) and quasi-RCTs comparing various primaquine dosing regimens with the standard primaquine regimen (15 mg/day for 14 days), or with no primaquine, in people with vivax malaria treated for blood stage infection with chloroquine." | ( Primaquine for preventing relapse in people with Plasmodium vivax malaria treated with chloroquine. Galappaththy, GN; Kirubakaran, R; Tharyan, P, 2013) | 0.79 |
| " Theoretically, CQ should be dosed according to body surface area (BSA)." | ( Chloroquine is grossly under dosed in young children with malaria: implications for drug resistance. Bergqvist, Y; Blessborn, D; Eksborg, S; Kofoed, PE; Rodrigues, A; Rombo, L; Ursing, J, 2014) | 1.85 |
| "CQ is under-dosed in children and should ideally be dosed according to BSA." | ( Chloroquine is grossly under dosed in young children with malaria: implications for drug resistance. Bergqvist, Y; Blessborn, D; Eksborg, S; Kofoed, PE; Rodrigues, A; Rombo, L; Ursing, J, 2014) | 1.85 |
| " Dosing of AZCQ was approximately 30 mg/kg AZ and 10 mg/kg CQ once daily for 3 days (for ≥20 kg weight: AZ/CQ 300/100 mg per tablet; 5 to <20 kg weight: AZ/CQ 150/50 mg per tablet)." | ( Population pharmacokinetics of azithromycin and chloroquine in healthy adults and paediatric malaria subjects following oral administration of fixed-dose azithromycin and chloroquine combination tablets. Chandra, R; Mould, DR; Tensfeldt, TG; Zhao, Q, 2014) | 0.66 |
| " Assuming equivalent dosing (mg/kg), AZ and CQ exposure in children would be expected to be lower than that in adults, suggesting that children may require a higher dose (mg/kg) than adults to achieve the same AZ and CQ exposure." | ( Population pharmacokinetics of azithromycin and chloroquine in healthy adults and paediatric malaria subjects following oral administration of fixed-dose azithromycin and chloroquine combination tablets. Chandra, R; Mould, DR; Tensfeldt, TG; Zhao, Q, 2014) | 0.66 |
| "3 µM) dosage increased lysosomal activity and induced autophagy and higher (1." | ( Realgar (As4S4) nanoparticles and arsenic trioxide (As2O3) induced autophagy and apoptosis in human melanoma cells in vitro. Balaz, P; Bujnakova, Z; Cholujova, D; Duraj, J; Gronesova, P; Hunakova, L; Lee, TC; Pastorek, M; Sedlak, J, 2014) | 0.4 |
| "Subgroup analyses for the response to antimalarials considering CLE subtypes, type, and dosage of antimalarials could not be performed because of the lack of available data." | ( Influence of smoking on the efficacy of antimalarials in cutaneous lupus: a meta-analysis of the literature. Amoura, Z; Arnaud, L; Barete, S; Chasset, F; Francès, C, 2015) | 0.42 |
| " Within 1 month after initiating dapsone therapy and increasing the dosage of prednisone, skin lesions promptly resolved." | ( Detection of Type VII Collagen Autoantibodies Before the Onset of Bullous Systemic Lupus Erythematosus. Chong, BF; Grabell, DA; Matthews, LA; Yancey, KB, 2015) | 0.42 |
| " A new study indicates that toxicity is not as rare as once believed, but depends critically on daily dosage and duration of use, as well as other risk factors." | ( A Critical Review of the Effects of Hydroxychloroquine and Chloroquine on the Eye. Brézin, AP; Costedoat-Chalumeau, N; Dunogué, B; Jallouli, M; Le Guern, V; Leroux, G; Marmor, MF; Melles, RB; Morel, N; Piette, JC, 2015) | 0.68 |
| " Established risk factors are duration and dosage of treatment while the involvement of genetic factors contributing to toxic maculopathy is largely unclear." | ( Common synonymous variants in ABCA4 are protective for chloroquine induced maculopathy (toxic maculopathy). Bergholz, R; Grassmann, F; Jägle, H; Mändl, J; Ruether, K; Weber, BH, 2015) | 0.66 |
| " If the quinoline-based strategies should nevertheless be pursued in future studies, particular care must be devoted to the dosage selection, in order to maximize the chances to obtain effective in vivo drug concentrations." | ( Chloroquine and beyond: exploring anti-rheumatic drugs to reduce immune hyperactivation in HIV/AIDS. Savarino, A; Shytaj, IL, 2015) | 1.86 |
| " Furthermore, analogue 40 exhibited excellent in vivo antimalarial activity when dosed orally at 50 mg/kg once daily for 4 days in the Plasmodium berghei mouse model, which is superior to the activity seen with previously reported compounds, and with a slightly improved hERG profile." | ( Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines. Chibale, K; Douelle, F; Gonzàlez Cabrera, D; Han, Z; Lawrence, N; Le Manach, C; Njoroge, M; Paquet, T; Street, LJ; Taylor, D; Waterson, D; Wiesner, L; Wittlin, S; Witty, MJ, 2015) | 0.42 |
| " Both CQ and 3-MA were synergistic with VCR to inhibit the growth of retinoblastoma cells and the combinational use significantly reduced the dosage of each drug." | ( Low concentrations of chloroquine and 3-methyladenine suppress the viability of retinoblastoma cells synergistically with vincristine independent of autophagy inhibition. Chen, X; Chen, YH; Jiang, PF; Li, LJ; Li, W; Shen, HQ; Zheng, XY, 2015) | 0.73 |
| " To optimize ID PfSPZ dosing so as to achieve 100% infection, 30 adults aged 18-45 years were randomized to one of six groups composed of five volunteers each." | ( Optimizing Intradermal Administration of Cryopreserved Plasmodium falciparum Sporozoites in Controlled Human Malaria Infection. Adams, M; Billingsley, PF; Chakravarty, S; Dube, TJ; Edelman, R; Green, M; Hoffman, SL; James, E; Laurens, MB; Li, ML; Lyke, KE; Manoj, A; Plowe, CV; Ruben, A; Sim, BKL; Strauss, K, 2015) | 0.42 |
| " Pharmacokinetic evaluation of these compounds showed low oral bioavailability and this affected in vivo efficacy when compounds were dosed orally." | ( Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model. Andayi, A; Chibale, K; Dambuza, NS; Egan, T; Evans, A; Norman, J; Smith, P; Taylor, D; Wiesner, L, 2015) | 0.42 |
| " berghei-infected mice when dosed intravenously, but parasites recrudesced 24 h after the administration of the least dose." | ( Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model. Andayi, A; Chibale, K; Dambuza, NS; Egan, T; Evans, A; Norman, J; Smith, P; Taylor, D; Wiesner, L, 2015) | 0.42 |
| " After a 2-month course of treatment with hydroxychloroquine dosage of 200 mg per day and a break of 3 months between courses, we observed a complete remission." | ( Unilateral unique Lupus tumidus: pathogenetic mystery and diagnostic problem. Bakardzhiev, I; Chokoeva, AA; Krasnaliev, I; Lotti, T; Tana, C; Tchernev, G; Wollina, U, 2016) | 0.69 |
| " In view of the limitations related to follow-up of patients and to assessing the plasma dosage of CQ and its metabolites, an alternative approach to monitor chemo-resistance (QR) is to use molecular markers." | ( Plasmodium vivax mdr1 genotypes in isolates from successfully cured patients living in endemic and non-endemic Brazilian areas. Almeida-de-Oliveira, NK; Brasil, P; Daniel-Ribeiro, CT; de Lavigne, AR; de Lima, SR; de Pina-Costa, A; Ferreira-da-Cruz, Mde F; Gomes, LR; Ménard, D, 2016) | 0.43 |
| "66) at the highest dosage administered (800 mg/kg) when compared with chloroquine diphosphate, the standard reference drug which had a % suppression of 90." | ( Antimalarial and cytotoxic properties of Chukrasia tabularis A. Juss and Turraea vogelii Hook F. Ex. Benth. Ajaiyeoba, EO; Fadare, AA; Fasinu, PS; Ogbole, OO; Saka, YA, 2016) | 0.67 |
| " It was nongenotoxic in an Ames assay, an in vitro micronucleus assay, and an in vivo rat micronucleus assay when dosed orally up to 2000 mg/kg." | ( Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. Berry, P; Campo, B; Cao, J; Ciaravino, V; Easom, EE; Erve, JCL; Freund, YR; Gamo, FJ; Guo, D; Jacobs, RT; Plattner, JJ; Rosenthal, PJ; Sanz, LM; Zhang, YK, 2017) | 0.46 |
| "Despite extensive use and accumulated evidence of safety, there have been few pharmacokinetic studies from which appropriate chloroquine (CQ) dosing regimens could be developed specifically for pregnant women." | ( Optimal antimalarial dose regimens for chloroquine in pregnancy based on population pharmacokinetic modelling. Baiwog, F; Davis, TME; Ilett, KF; Karunajeewa, HA; Kose, K; Mueller, I; Page-Sharp, M; Rogerson, SJ; Salman, S; Siba, PM, 2017) | 0.93 |
| " Lipid based nanodrug delivery systems have been very popular in the recent times as they are very less toxic, have drug targeting capabilities and also reduces the dosing frequency by increasing efficacy of the drug." | ( Optimisation of chloroquine phosphate loaded nanostructured lipid carriers using Box-Behnken design and its antimalarial efficacy. Baruah, UK; Gowthamarajan, K; Karri, VVSR; Ravisankar, V; Simhadri, PK; Singh, V, 2018) | 0.83 |
| " For potential clinical application, DC vaccine preparations treated with tumor cells that were already pretreated with chloroquine and shikonin further enhanced the antimetastatic activity of 4T1 tumors and reduced the effective dosage of doxorubicin." | ( Necroptosis promotes autophagy-dependent upregulation of DAMP and results in immunosurveillance. Fan, YT; Hsiao, PW; Hsieh, SY; Lin, SY; Tsai, DH; Wei, WC; Wu, TS; Yang, NS, 2018) | 0.69 |
| " The observation of atypical dose-response curves when some compounds were tested against multidrug resistant malaria parasite strains guided the optimization process to define a chemical space that led to typical sigmoidal dose-response and complete kill of multidrug resistant parasites." | ( Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains. Basarab, GS; Brunschwig, C; Chibale, K; Duffy, J; Eyermann, CJ; Fish, PV; Gibhard, L; Lawrence, N; Le Manach, C; Nchinda, AT; Njoroge, M; Paquet, T; Street, LJ; Taylor, D; Wicht, K; Wittlin, S, 2018) | 0.48 |
| " We applied pharmacokinetic modeling to develop a predictive model for CQ exposure to identify an optimal maternal/fetal dosing regimen to prevent ZIKV endocytosis in brain cells." | ( Dose Optimization of Chloroquine by Pharmacokinetic Modeling During Pregnancy for the Treatment of Zika Virus Infection. Badhan, RKS; Olafuyi, O, 2019) | 0.83 |
| " falciparum to artemisinin, chloroquine and piperaquine by both a standard dose-response analysis and a piperaquine survival assay." | ( Overexpression of plasmepsin II and plasmepsin III does not directly cause reduction in Plasmodium falciparum sensitivity to artesunate, chloroquine and piperaquine. Ansbro, MR; Chookajorn, T; Chotivanich, K; de Cozar, C; Gamo, FJ; Kochakarn, T; Kotanan, N; Kümpornsin, K; Lee, MCS; Loesbanluechai, D; Sanz, LM; White, NJ; Wilairat, P, 2019) | 1.01 |
| " These are important features that may help to improve the therapeutic dosing and efficacy of palbociclib." | ( Lysosomal trapping of palbociclib and its functional implications. Blanco-Aparicio, C; Hernández-Encinas, E; Llanos, S; Megias, D; Pietrocola, F; Rovira, M; Serrano, M, 2019) | 0.51 |
| " Furthermore, autophagy intervention experiments were achieved by the administration of rapamycin (RAPA) or chloroquine (CQ) one hour prior to dosing 300 mg/kg APAP." | ( Mitophagy protects against acetaminophen-induced acute liver injury in mice through inhibiting NLRP3 inflammasome activation. Kou, R; Shan, S; Shen, Z; Song, F; Xie, K; Zhang, C, 2019) | 0.73 |
| " In several endemic areas, including the Brazilian Amazon basin, anti-malarial drugs are dispensed in small plastic bags at a dosing regimen based on age." | ( Doses of chloroquine in the treatment of malaria by Plasmodium vivax in patients between 2 and 14 years of age from the Brazilian Amazon basin. de Ataide, MA; de Sena, LWP; Dias, RM; Ferreira, MVD; Mello, AGNC; Vieira, JLF, 2019) | 0.93 |
| " The unknown dose-response relationships of these drugs and the lack of definitions of the minimum dose needed for clinical efficacy and what doses are toxic pose challenges to clinical practice." | ( Mechanisms of action of hydroxychloroquine and chloroquine: implications for rheumatology. Dörner, T; Schrezenmeier, E, 2020) | 0.84 |
| " Using the PBPK models, hydroxychloroquine concentrations in lung fluid were simulated under 5 different dosing regimens to explore the most effective regimen while considering the drug's safety profile." | ( In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Cui, C; Dong, E; Huang, B; Li, H; Liu, D; Liu, X; Lu, R; Niu, P; Song, C; Tan, W; Yao, X; Ye, F; Zhan, S; Zhang, M; Zhao, L, 2020) | 1.07 |
| " The current dosage recommended in clinical treatment is larger than that in previous treatment of malaria and the period of treatment is longer." | ( Trial of Chloroquines in the Treatment of COVID-19 and Its Research Progress in Forensic Toxicology. Duan, YJ; Huang, F; Liu, L; Liu, Q; Ren, L; Zhao, SQ; Zhou, YW, 2020) | 0.98 |
| " Clinical experience has shown that chloroquine has a narrow safety margin, as three times the adult therapeutic dosage for malaria can be lethal when given as a single dose." | ( Chloroquine for SARS-CoV-2: Implications of Its Unique Pharmacokinetic and Safety Properties. Knibbe, CAJ; Peeters, MYM; Smit, C; van den Anker, JN, 2020) | 2.28 |
| "The preliminary findings of this study suggest that the higher CQ dosage should not be recommended for critically ill patients with COVID-19 because of its potential safety hazards, especially when taken concurrently with azithromycin and oseltamivir." | ( Effect of High vs Low Doses of Chloroquine Diphosphate as Adjunctive Therapy for Patients Hospitalized With Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infection: A Randomized Clinical Trial. Albuquerque, BC; Alexandre, MAA; Baía-da-Silva, D; Balieiro, AAS; Bassat, Q; Borba, MGS; Brito, M; Brito-Sousa, JD; Croda, J; Daniel-Ribeiro, CT; Fontes, CJ; Guerra, MVF; Hajjar, LA; Lacerda, MVG; Melo, GC; Monteiro, WM; Mourão, MPG; Naveca, FG; Nogueira, ML; Pacheco, AGF; Pinto, RC; Romero, GAS; Sampaio, VS; Santos, JDO; Schwarzbold, A; Siqueira, AM; Val, FFA; Xavier, MS, 2020) | 0.84 |
| " Although in some recent studies a clinical improvement in COVID-19 patients has been observed, the clinical efficacy of CQ and HCQ in COVID-19 has yet to be proven with randomized controlled studies, many of which are currently ongoing, also considering pharmacokinetics, optimal dosing regimen, therapeutic level and duration of treatment and taking into account patients with different severity degrees of disease." | ( The possible mechanisms of action of 4-aminoquinolines (chloroquine/hydroxychloroquine) against Sars-Cov-2 infection (COVID-19): A role for iron homeostasis? Biasiotto, G; Magro, P; Quiros Roldan, E; Zanella, I, 2020) | 0.8 |
| " The suggested dose of chloroquine for COVID-19 infection is considerably higher than the usual dosage for malaria treatment; therefore, it is plausible that the ototoxic effects will be greater." | ( Clinical Implications of Chloroquine and Hydroxychloroquine Ototoxicity for COVID-19 Treatment: A Mini-Review. Baguley, DM; Kasbekar, AV; Prayuenyong, P, 2020) | 1.17 |
| "There is widespread suboptimal dosing of chloroquine that is probably due to the dosing regimen based on patient age, which reduces the drug exposure with a possible influence on parasite clearance." | ( The extent of chloroquine underdosing in adult patients with malaria by Plasmodium vivax from an endemic area of the Brazilian Amazon basin. Gabryelle Nunes Cardoso Mello, A; Luiz Fernandes Vieira, J; Regina Matos Lopes, T; Sena, LWP; Valéria Dias Ferreira, M, 2020) | 1.18 |
| "Il existe un dosage sous-optimal répandu de chloroquine qui est probablement dû au schéma posologique basé sur l'âge du patient, ce qui réduit l'exposition au médicament avec une influence possible sur la clairance des parasites." | ( The extent of chloroquine underdosing in adult patients with malaria by Plasmodium vivax from an endemic area of the Brazilian Amazon basin. Gabryelle Nunes Cardoso Mello, A; Luiz Fernandes Vieira, J; Regina Matos Lopes, T; Sena, LWP; Valéria Dias Ferreira, M, 2020) | 1.18 |
| " The dosage is a critical factor in a clinical trial: too low and the drug will not have an effect, too high and the side effects may counteract any potential benefits." | ( Concentration-dependent mortality of chloroquine in overdose. Baud, FJ; Clemessy, JL; Hoglund, RM; Megarbane, B; Tarning, J; Watson, JA; White, NJ, 2020) | 0.83 |
| "This review will focus on the antiviral mechanism, effectiveness and safety, dosage and DDIs of chloroquine, for the purpose of providing evidence-based support for rational use of chloroquine in the treatment of COVID-19." | ( Updates on the Pharmacology of Chloroquine against Coronavirus Disease 2019 (COVID-19): A Perspective on its Use in the General and Geriatric Population. Cui, C; Hou, Z; Li, H; Liu, D; Tu, S; Yao, X; Zhang, M, 2020) | 1.06 |
| " This position statement recommends dosage adjustment for these drugs in the context of renal impairment." | ( Position statement from the Brazilian Society of Nephrology regarding chloroquine and hydroxychloroquine drug dose adjustment according to renal function. Andreoli, MCC; Bastos, K; D'Avila, R; Kraychete, A; Misael, AM; Moura-Neto, JA; Nascimento, MMD; Silva, DRD, 2020) | 0.79 |
| " Studies of previous military operations show that compliance is consistently higher with weekly versus daily dosing regimens." | ( An open label study of the safety and efficacy of a single dose of weekly chloroquine and azithromycin administered for malaria prophylaxis in healthy adults challenged with 7G8 chloroquine-resistant Plasmodium falciparum in a controlled human malaria inf Bennett, J; Cicatelli, S; DeLuca, J; Duncan, EH; Hamer, M; Hutter, J; Kreishman-Deitrick, M; Lee, C; Livezey, J; Mills, K; Moon, JE; Morrison, M; Oliver, T; Poon, L; Sedegah, M; Selig, D; Sikaffy, A; Sousa, J; Tosh, D; Twomey, P; Vuong, C; Waterman, P, 2020) | 0.79 |
| " The choice of (typically subtherapeutic) dosing regimens, influenced partly by "QT-phobia," varied widely and seems anecdotal without any pharmacologically reliable supporting clinical evidence." | ( Chloroquine and hydroxychloroquine for COVID-19: Perspectives on their failure in repurposing. Shah, RR, 2021) | 2.06 |
| "To evaluate the association and dose-response pattern between antimalarial drugs and overall and cause specific mortality in SLE patients." | ( Association of antimalarial drugs with decreased overall and cause specific mortality in systemic lupus erythematosus. Da, Z; Ding, X; Feng, X; Hu, H; Jin, Z; Li, J; Liu, L; Pan, W; Qian, X; Sun, L; Tan, J; Tao, J; Wang, F; Wang, M; Wei, H; Wu, J; Wu, M; Zhang, M; Zou, Y, 2021) | 0.62 |
| " Interestingly, both the time and the daily dosage of HCQ/CQ use were related to decreased mortality of SLE in a linear dose-response relationship." | ( Association of antimalarial drugs with decreased overall and cause specific mortality in systemic lupus erythematosus. Da, Z; Ding, X; Feng, X; Hu, H; Jin, Z; Li, J; Liu, L; Pan, W; Qian, X; Sun, L; Tan, J; Tao, J; Wang, F; Wang, M; Wei, H; Wu, J; Wu, M; Zhang, M; Zou, Y, 2021) | 0.62 |
| " The protective effects for survival might be augmented by adherence and full dosage of these drugs." | ( Association of antimalarial drugs with decreased overall and cause specific mortality in systemic lupus erythematosus. Da, Z; Ding, X; Feng, X; Hu, H; Jin, Z; Li, J; Liu, L; Pan, W; Qian, X; Sun, L; Tan, J; Tao, J; Wang, F; Wang, M; Wei, H; Wu, J; Wu, M; Zhang, M; Zou, Y, 2021) | 0.62 |
| " Understanding the pharmacokinetics (PK) in COVID-19 patients is essential to study its exposure-efficacy/safety relationship and provide a basis for a possible dosing regimen optimization." | ( Population-based meta-analysis of chloroquine: informing chloroquine pharmacokinetics in COVID-19 patients. Cai, T; Cui, C; Hou, Z; Li, H; Lin, J; Liu, D; Liu, Q; Wang, X; Xiong, Z; Yan, X; Yao, X; Zhang, S, 2021) | 0.9 |
| "Model-based simulation using PK parameters from the COVID-19 patients shows that the concentrations under the currently recommended dosing regimen are below the safety margin for side-effects, which suggests that these dosing regimens are generally safe." | ( Population-based meta-analysis of chloroquine: informing chloroquine pharmacokinetics in COVID-19 patients. Cai, T; Cui, C; Hou, Z; Li, H; Lin, J; Liu, D; Liu, Q; Wang, X; Xiong, Z; Yan, X; Yao, X; Zhang, S, 2021) | 0.9 |
| " Tissue-to-plasma CQ ratios at 50 hours after dosing were highest in lung, kidney, liver, and spleen (182-318) and lower in heart, muscle, brain, eye, and skin (11-66)." | ( Physiologically Based Pharmacokinetics of Lysosomotropic Chloroquine in Rat and Human. Jusko, WJ; Liu, X, 2021) | 0.87 |
| " This review summarizes the current data for the most commonly used drugs for coronavirus disease 2019 and will cover the unique factors that may affect the dosing of these medications in patients with CKD." | ( Treatment Options for Coronavirus Disease 2019 in Patients With Reduced or Absent Kidney Function. Govil, A; Luckett, K; Miller-Handley, H, 2020) | 0.56 |
| " Additional liabilities of these medications include pharmacokinetic profiles that require extended dosing to achieve therapeutic tissue concentrations." | ( Nanomedicine Reformulation of Chloroquine and Hydroxychloroquine. Crist, RM; Stern, ST; Stevens, DM, 2020) | 0.85 |
| " Nine trials compared HCQ with standard care (7779 participants), and one compared HCQ with placebo (491 participants); dosing schedules varied." | ( Chloroquine or hydroxychloroquine for prevention and treatment of COVID-19. Chaplin, M; Fletcher, T; Kredo, T; Ryan, H; Singh, B, 2021) | 2.06 |
| " Authors discretion is to conduct more studies considering the optimal dosing regimen and pharmacokinetics assessment." | ( Exploring insights of hydroxychloroquine, a controversial drug in Covid-19: An update. Joshi, G; Poduri, R; Thakur, S, 2021) | 0.91 |
| "Research findings reported in this article may facilitate the repositioning, quality control, and biological monitoring of chloroquine in modern pharmaceutical dosage forms and treatments." | ( HPLC methods for choloroquine determination in biological samples and pharmaceutical products. Gonçalves, TM; Lopez, RFV; Martins, YA, 2021) | 0.83 |
| "The dosage was consistent in both groups: 250 mg of chloroquine or 200 mg of hydroxychloroquine daily." | ( Chloroquine and hydroxychloroquine - safety profile of potential COVID-19 drugs from the rheumatologist's perspective. Grygiel-Górniak, B; Majewska, KA; Majewski, D; Naskręcka, M, 2021) | 2.31 |
| " Data from the literature show that high dosage as recommended in COVID-19 treatment may pose a risk of toxicity and require precise management, but prophylactic, long-term use of lower, safe doses might be a promising solution." | ( Chloroquine and hydroxychloroquine - safety profile of potential COVID-19 drugs from the rheumatologist's perspective. Grygiel-Górniak, B; Majewska, KA; Majewski, D; Naskręcka, M, 2021) | 2.06 |
| "This study investigated the possible influence of the choice of solvents (methanol and water) for extracting MAMA Powder (MP) against Plasmodium berghei-infected mice to optimize its antimalarial activity and for developing other pharmaceutical dosage forms." | ( Comparative in vivo antimalarial activities of aqueous and methanol extracts of MAMA powder - A herbal antimalarial preparation. Adepiti, AO; Adeyoju, EO; Ajayi, CO; Elujoba, AA, 2022) | 0.72 |
| "The study concluded that the water extract with higher antimalarial activity could be optimized for chloroquine-resistant malaria and can thus facilitate the production of liquid and solid dosage forms." | ( Comparative in vivo antimalarial activities of aqueous and methanol extracts of MAMA powder - A herbal antimalarial preparation. Adepiti, AO; Adeyoju, EO; Ajayi, CO; Elujoba, AA, 2022) | 0.94 |
| " We aimed to determine appropriate oral tafenoquine paediatric dosing regimens, including a dispersible formulation, and evaluated tafenoquine efficacy and safety in children infected with P vivax." | ( Tafenoquine exposure assessment, safety, and relapse prevention efficacy in children with Plasmodium vivax malaria: open-label, single-arm, non-comparative, multicentre, pharmacokinetic bridging, phase 2 trial. Breton, JJ; Chau, NH; Duparc, S; Ernest, TB; Goyal, N; Green, JA; Hien, TT; Hoa, NT; Jones, SW; Martin, A; Mohamed, K; Rolfe, K; Rousell, VM; Sharma, H; Tan, LK; Taylor, M; Vélez, ID, 2022) | 0.72 |
| " Dosing groups were assigned by body weight, predicted to achieve similar median exposures as the approved 300 mg dose for adults: patients who weighed 5 kg or more to 10 kg received 50 mg, those who weighed more than 10 to 20 kg received 100 or 150 mg, those who weighed more than 20 to 35 kg received 200 mg, and patients who weighed more than 35 kg received 300 mg." | ( Tafenoquine exposure assessment, safety, and relapse prevention efficacy in children with Plasmodium vivax malaria: open-label, single-arm, non-comparative, multicentre, pharmacokinetic bridging, phase 2 trial. Breton, JJ; Chau, NH; Duparc, S; Ernest, TB; Goyal, N; Green, JA; Hien, TT; Hoa, NT; Jones, SW; Martin, A; Mohamed, K; Rolfe, K; Rousell, VM; Sharma, H; Tan, LK; Taylor, M; Vélez, ID, 2022) | 0.72 |
| " A physiologically based pharmacokinetic model with detailed respiratory physiology was used to predict regional airway exposure and optimize dosing regimens." | ( Translational Modeling of Chloroquine and Hydroxychloroquine Dosimetry in Human Airways for Treating Viral Respiratory Infections. Calvino-Martin, F; Hoeng, J; Kolli, AR, 2022) | 1.02 |
| "Our analysis provides a framework for extrapolating in vitro effective concentrations of chloroquine and hydroxychloroquine to in vivo dosing regimens for treating viral respiratory infections." | ( Translational Modeling of Chloroquine and Hydroxychloroquine Dosimetry in Human Airways for Treating Viral Respiratory Infections. Calvino-Martin, F; Hoeng, J; Kolli, AR, 2022) | 1.24 |
| "9 years, and the mean drug dosage was 244 mg." | ( Oral pigmentation as an adverse effect of chloroquine and hydroxychloroquine use: A scoping review. Blumenberg, C; Cardoso, SV; Franco, A; Oliveira, MB; Paranhos, LR; Silva, PUJ; Siqueira, WL; Vieira, W, 2022) | 0.99 |
| "The outcomes of this study suggest that hyperpigmentation depend on drug dosage and treatment length." | ( Oral pigmentation as an adverse effect of chloroquine and hydroxychloroquine use: A scoping review. Blumenberg, C; Cardoso, SV; Franco, A; Oliveira, MB; Paranhos, LR; Silva, PUJ; Siqueira, WL; Vieira, W, 2022) | 0.99 |
| " Drug sensitivity against a panel of antimalarials, the ring-stage survival assay (RSA), the PPQ survival assay (PSA), and bimodal dose-response curves were used to evaluate antimalarial susceptibility." | ( A single point mutation in the Plasmodium falciparum 3'-5' exonuclease does not alter piperaquine susceptibility. Boonyalai, N; Griesenbeck, JS; Kirativanich, K; Praditpol, C; Thamnurak, C; Vesely, BA; Waters, NC; Wojnarski, M, 2022) | 0.72 |
| " In conclusion, the CQ dosage and regimen used to treat COVID-19 induced adverse effects in diabetic rats, suggesting the need to reevaluate the effective dose of CQ in humans." | ( Safety considerations of chloroquine in the treatment of patients with diabetes and COVID-19. Gao, X; Guo, D; Ji, H; Jiang, S; Jing, X; Peng, L; Qiu, Y; Wang, J; Wu, W; Zheng, Y, 2022) | 1.02 |
| " However, local safety profile should also be evaluated depending on the new indication, administration route and dosage form." | ( Antivirals and the Potential Benefits of Orally Inhaled Drug Administration in COVID-19 Treatment. Akbal-Dagistan, O; Basarir, NS; Culha, M; Erturk, A; Sahin, G; Sancar, S; Yildiz-Pekoz, A, 2022) | 0.72 |
| " The dosing regimen used in preclinical models of nephrotoxicity may impact the success of therapeutic candidates in clinical trials." | ( Pharmacological inhibitors of autophagy have opposite effects in acute and chronic cisplatin-induced kidney injury. Beverly, LJ; Doll, MA; Feng, JL; Krueger, AM; Orwick, A; Sears, SM; Shah, PP; Siskind, LJ; Vega, AA, 2022) | 0.72 |
| " The established correlation equations can be useful in therapeutic drug monitoring (TDM) and dosing regimen optimization." | ( The investigation of the complex population-drug-drug interaction between ritonavir-boosted lopinavir and chloroquine or ivermectin using physiologically-based pharmacokinetic modeling. Alsmadi, MM, 2023) | 1.12 |
| " Surprisingly, oral dosing of both compounds suppressed scratching behaviors that were observed in mice." | ( Anti-pruritic effect of isothiocyanates: Potential involvement of toll-like receptor 3 signaling. Hayashi, I; Kainoh, M; Konno, M; Majima, Y; Moriyama, M; Serizawa, K; Suzuki, T; Yuzawa, N, 2022) | 0.72 |
| " A model-informed strategy based on preclinical data, which incorporates pharmacokinetic-pharmacodynamic (PK-PD) properties with physiologically based pharmacokinetic (PBPK) modeling, is proposed to optimally predict an efficacious human dose and dosage regimen for the treatment of Plasmodium falciparum malaria." | ( Integrating Pharmacokinetic-Pharmacodynamic Modeling and Physiologically Based Pharmacokinetic Modeling to Optimize Human Dose Predictions for Plasmodium falciparum Malaria: a Chloroquine Case Study. Chibale, K; Gibhard, L; Mulubwa, M; Redhi, D, 2023) | 1.1 |
| " Conversely, when the W2 systems were dosed with chloroquine, parasitemia levels were moderately decreased when compared to the 3D7 model." | ( Development of a human malaria-on-a-chip disease model for drug efficacy and off-target toxicity evaluation. Comiter, B; Hickman, JJ; Long, CJ; McAleer, CW; Rupar, MJ; Sasserath, T; Smith, E; Sriram, N, 2023) | 1.16 |
| " Tests related to adsorption kinetics, equilibrium isotherms and adsorbent reuse were studied, and optimization parameters related to the initial pH of the solution and the adsorbent dosage were defined." | ( Adsorption of chloroquine, propranolol, and metformin in aqueous solutions using magnetic graphene oxide nanocomposite. Cavalcanti, JVFL; da Motta Sobrinho, MA; de Araújo, CMB; Del Carmen Pinto Osorio, D; do Nascimento, BF; Dotto, GL; Silva, LFO, 2023) | 1.27 |
| Role | Description |
|---|---|
| antimalarial | A drug used in the treatment of malaria. Antimalarials are usually classified on the basis of their action against Plasmodia at different stages in their life cycle in the human. |
| antirheumatic drug | A drug used to treat rheumatoid arthritis. |
| dermatologic drug | A drug used to treat or prevent skin disorders or for the routine care of skin. |
| autophagy inhibitor | Any compound that inhibits the process of autophagy (the self-digestion of one or more components of a cell through the action of enzymes originating within the same cell). |
| anticoronaviral agent | Any antiviral agent which inhibits the activity of coronaviruses. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| aminoquinoline | Any member of the class of quinolines in which the quinoline skeleton is substituted by one or more amino or substituted-amino groups. |
| secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| organochlorine compound | An organochlorine compound is a compound containing at least one carbon-chlorine bond. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| COVID-19, thrombosis and anticoagulation | 7 | 5 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.3548 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| PPM1D protein | Homo sapiens (human) | Potency | 4.2501 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| TDP1 protein | Homo sapiens (human) | Potency | 0.7511 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 25.1189 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 89.1251 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| Interferon beta | Homo sapiens (human) | Potency | 4.2501 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| Ataxin-2 | Homo sapiens (human) | Potency | 14.1254 | 0.0119 | 12.2221 | 68.7989 | AID588378 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| glucose-6-phosphate dehydrogenase-6-phosphogluconolactonase | Plasmodium berghei | IC50 (µMol) | 67.6667 | 0.8890 | 21.0286 | 71.5000 | AID602131; AID602132; AID602133 |
| Spike glycoprotein | Betacoronavirus England 1 | IC50 (µMol) | 5.4700 | 0.0300 | 2.7283 | 9.5100 | AID1804127 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | IC50 (µMol) | 5.4700 | 0.0040 | 3.4388 | 9.5100 | AID1804127 |
| glucose-6-phosphate 1-dehydrogenase isoform b | Homo sapiens (human) | IC50 (µMol) | 80.0000 | 8.8700 | 12.8518 | 17.8000 | AID602130 |
| Transmembrane protease serine 2 | Homo sapiens (human) | IC50 (µMol) | 5.4700 | 0.0180 | 2.6198 | 9.5100 | AID1804127 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 103.9000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
| Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 134.0000 | 0.1100 | 7.1903 | 10.0000 | AID1443980; AID1473738 |
| Dihydrofolate reductase | Bos taurus (cattle) | IC50 (µMol) | 0.0301 | 0.0017 | 0.0435 | 0.1007 | AID1462733; AID1486840 |
| Amyloid-beta precursor protein | Homo sapiens (human) | IC50 (µMol) | 9.9000 | 0.0005 | 3.8895 | 10.0000 | AID1391090; AID1391091 |
| Histidine-rich protein PFHRP-II | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 (µMol) | 396,967.5905 | 0.0765 | 1.1255 | 2.9000 | AID152007; AID157847; AID157853; AID157874; AID218557; AID258363; AID268410; AID274221; AID275795; AID277607; AID278900; AID341400; AID401645 |
| Procathepsin L | Homo sapiens (human) | IC50 (µMol) | 5.4700 | 0.0002 | 1.6661 | 9.5100 | AID1804127 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 4.6774 | 0.0000 | 0.6902 | 10.0000 | AID1409619 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 5.7544 | 0.0000 | 0.7951 | 9.1201 | AID1409621 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 349.9450 | 0.0001 | 1.7536 | 10.0000 | AID428564 |
| Muscarinic acetylcholine receptor M5 | Homo sapiens (human) | Ki | 21.8776 | 0.0000 | 0.7292 | 6.9183 | AID1409622 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 4.3652 | 0.0001 | 0.8074 | 10.0000 | AID1409617 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | IC50 (µMol) | 5.4700 | 0.0300 | 2.2971 | 9.5100 | AID1804127 |
| Replicase polyprotein 1ab | Human coronavirus 229E | IC50 (µMol) | 5.4700 | 0.0300 | 2.1441 | 9.5100 | AID1804127 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 (µMol) | 5.4700 | 0.0040 | 2.9266 | 9.9600 | AID1804127 |
| Spike glycoprotein | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 3.5800 | 0.0380 | 3.1995 | 7.0000 | AID1756670; AID1781212 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 8.2500 | 0.0002 | 2.4585 | 9.9600 | AID1804127; AID1804171 |
| Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | Ki | 9.1201 | 0.0000 | 0.5972 | 9.1201 | AID1409612 |
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | IC50 (µMol) | 1.5000 | 0.0027 | 1.6287 | 9.9000 | AID540067 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 31.6228 | 0.0002 | 0.7257 | 10.0000 | AID1409618 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 10.0000 | 0.0003 | 0.4834 | 10.0000 | AID1409610 |
| DNA ligase 1 | Homo sapiens (human) | IC50 (µMol) | 823.0000 | 0.6000 | 0.6000 | 0.6000 | AID1798278; AID1798279 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 3.3113 | 0.0000 | 0.5405 | 7.7600 | AID1409620 |
| Serine/threonine-protein kinase mTOR | Homo sapiens (human) | IC50 (µMol) | 0.2700 | 0.0000 | 0.8575 | 10.0000 | AID1894033 |
| Beta-secretase 1 | Homo sapiens (human) | IC50 (µMol) | 9.8500 | 0.0006 | 1.6194 | 10.0000 | AID1414154; AID1414155 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | IC50 (µMol) | 5.4700 | 0.0300 | 2.7731 | 9.5100 | AID1804127 |
| MO15-related protein kinase Pfmrk | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 (µMol) | 150.0000 | 0.7000 | 4.3200 | 7.0000 | AID242065 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 2.5030 | 0.0009 | 1.9014 | 10.0000 | AID1193564; AID240820; AID346849; AID576612 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | Ki | 5.3311 | 0.0021 | 1.8407 | 10.0000 | AID1059571; AID1409624 |
| Sigma intracellular receptor 2 | Homo sapiens (human) | Ki | 0.5012 | 0.0001 | 0.8360 | 4.6005 | AID1409615 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0794 | 0.0000 | 0.4901 | 10.0000 | AID1409616 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | IC50 (µMol) | 6.2350 | 0.0004 | 2.2079 | 10.0000 | AID1781212; AID1804127 |
| Cysteine proteinase falcipain 2a | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 (µMol) | 0.0200 | 0.0058 | 0.4403 | 5.0000 | AID1391502 |
| Cysteine proteinase falcipain 2a | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 (µMol) | 0.2000 | 0.2000 | 0.2000 | 0.2000 | AID1391503 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Spike glycoprotein | Betacoronavirus England 1 | EC50 (µMol) | 5.3333 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 (µMol) | 5.3333 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 (µMol) | 5.3333 | 0.0030 | 4.5168 | 9.8200 | AID1804127 |
| Riboflavin-binding protein | Gallus gallus (chicken) | Kd | 2.1000 | 0.0050 | 0.3595 | 2.1000 | AID642884 |
| Major prion protein | Homo sapiens (human) | EC50 (µMol) | 4.0000 | 0.3000 | 4.9000 | 10.0000 | AID161627 |
| Procathepsin L | Homo sapiens (human) | EC50 (µMol) | 5.3333 | 0.0030 | 4.4874 | 9.8200 | AID1804127 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 5.3333 | 0.0030 | 4.6136 | 9.8200 | AID1804127 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 (µMol) | 5.3333 | 0.0030 | 4.6136 | 9.8200 | AID1804127 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 5.3333 | 0.0030 | 4.4554 | 9.8200 | AID1804127 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 (µMol) | 5.3333 | 0.0030 | 4.1105 | 9.8200 | AID1804127 |
| Nuclear receptor subfamily 4 group A member 2 | Homo sapiens (human) | EC50 (µMol) | 48.5000 | 0.0100 | 2.8912 | 5.1000 | AID1764403; AID1885207 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 5.3333 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
| Calcium-dependent protein kinase 1 | Plasmodium falciparum K1 | EC50 (µMol) | 0.0680 | 0.0680 | 0.1760 | 0.2300 | AID1799369 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 (µMol) | 5.3333 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1323893 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 infected in red blood cells | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | 7-Chloro-4-aminoquinoline γ-hydroxy-γ-lactam derived-tetramates as a new family of antimalarial compounds. |
| AID1439851 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for erythrocytic stage of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity. |
| AID1457211 | Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID212500 | Compound was tested for antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS, activity is expressed as the mortality rate at a concentration of 10 mg/kg. in experiment 2; 5 out of 5 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID285473 | Cytotoxicity against human HCT cells assessed as [3H]thymidine incorporation | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
| AID356604 | Antiplasmodial activity after 18 hrs against chloroquine-resistant Plasmodium falciparum FcB1 in human blood by [3H]hypoxanthine uptake | 2003 | Journal of natural products, Nov, Volume: 66, Issue:11 | Flavonoids from Dalbergia louvelii and their antiplasmodial activity. |
| AID519269 | Antiparasitic activity against chloroquine-resistant Plasmodium falciparum R1H6/2 pretreated with 0.1 uM phenobarbitone for 48 hrs by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
| AID1428721 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Zika virus infected in African green monkey Vero cells | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | 2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine. |
| AID310606 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Bre1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues. |
| AID1758487 | Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors. |
| AID318186 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. |
| AID1231608 | Inhibition of Cu2+-induced amyloid beta (1 to 42) aggregation (unknown origin) at 50 uM after 24 hrs by thioflavin T fluorescence assay (Rvb = 100%) | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis and evaluation of selegiline derivatives as monoamine oxidase inhibitor, antioxidant and metal chelator against Alzheimer's disease. |
| AID509176 | Inhibition of TLR7/TLR9-mediated maturation of aldrithiol-2-treated HIV1 Ada-stimulated human PBMC assessed as CD83 expressing cells at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID284886 | Anti-infective activity against Plasmodium falciparum W2 in erythrocytes | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis and evaluation of isosteres of N-methyl indolo[3,2-b]-quinoline (cryptolepine) as new antiinfective agents. |
| AID1538873 | Antimalarial activity against Plasmodium falciparum FCR3 infected in human erythrocytes by Giemsa staining analysis | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway. |
| AID480225 | Inhibition of CYP2B6 in human liver microsomes assessed as metabolite produced at 1 uM by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1892264 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBC assessed as reduction in parasite growth after 72 hrs by LDH assay | 2022 | Bioorganic & medicinal chemistry, 07-15, Volume: 66 | New antimalarials identified by a cell-based phenotypic approach: Structure-activity relationships of 2,3,4,9-tetrahydro-1H-β-carboline derivatives possessing a 2-((coumarin-5-yl)oxy)alkanoyl moiety. |
| AID366985 | Antimalarial activity as increased mean survival time in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus) at 10 mg/kg peroral dose day 1 with intraperitoneal dose over 4 days | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline. |
| AID1304201 | Antimalarial activity against chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities. |
| AID267109 | Antimalarial activity against Plasmodium falciparum TM91C235 | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Tetraoxane antimalarials and their reaction with Fe(II). |
| AID594419 | Antimalarial activity against Plasmodium falciparum by flow cytometry | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | Potent antiprotozoal activity of a novel semi-synthetic berberine derivative. |
| AID754531 | Inhibition of hemozoin formation in 0.5 M acetate buffer at pH 4.8 after 12 hrs by tube-based high-throughput assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID1504889 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12 | Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana. |
| AID1126159 | Antiplasmodial activity against erythrocytic stages of Plasmodium falciparum NF54 | 2014 | Journal of natural products, Apr-25, Volume: 77, Issue:4 | Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4. |
| AID1625412 | Antiplasmodial activity against chloroquine/antifolate-sensitive Plasmodium falciparum TM4 infected in human RBC incubated for 18 to 20 hrs by microdilution radioisotope method | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | Antimalarial Oxoprotoberberine Alkaloids from the Leaves of Miliusa cuneata. |
| AID389452 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
| AID343939 | Antimalarial activity against mefloquine, chloroquine and quinine-resistant Plasmodium falciparum TM91C235 | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Mixed tetraoxanes containing the acetone subunit as antimalarials. |
| AID1230200 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human type A-positive red blood cells assessed as parasite growth inhibition after 72 hrs by lactate dehydrogenase assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Glycosyl hydroperoxides: a new class of potential antimalarial agents. |
| AID540239 | Phospholipidosis-positive literature compound observed in dog | |||
| AID756890 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
| AID1494382 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as decrease in path searching behavior at 30 mg/kg/day, po for 80 days by Morris water maze test | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID434579 | Terminal half life in human | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. |
| AID1236488 | Selectivity index, ratio of GI50 for human HepG2 cells to IC50 for asexual intraerythrocytic ring stage of chloroquine-sensitive Plasmodium falciparum 3D7 infected in human O+ erythrocytes | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites. |
| AID519274 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum K1Hf pretreated with 0.1 uM phenobarbitone for 48 hrs and in presence of 5 uM verapamil by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
| AID151995 | Displacement of chloroquine from Fe(3+) FPIX-loaded membrane | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum. |
| AID580696 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of schizont stage parasite growth at 100 times IC50 after 1 hr by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID274300 | Cytotoxicity against L6 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
| AID318210 | Cytotoxicity against human Daudi cells after 48 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID675864 | Antiplasmodial activity against Plasmodium falciparum assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Disulfide prodrugs of albitiazolium (T3/SAR97276): synthesis and biological activities. |
| AID427290 | Therapeutic index, ratio of MTD for Plasmodium berghei infected ICR mice (Mus musculus) to MCD for Plasmodium berghei | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents. |
| AID158716 | Inhibitory concentration against chloroquine-sensitive Plasmodium falciparum | 2004 | Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2 | Discovery of a bulky 2-tert-butyl group containing primaquine analogue that exhibits potent blood-schizontocidal antimalarial activities and complete elimination of methemoglobin toxicity. |
| AID337550 | Selectivity index, ratio of ED50 for human ZR-75-1 cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID623646 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum HB3 after 72 hrs SYBR green 1 dye based by fluorometric method | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Antiplasmodial and antiproliferative pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest. |
| AID323676 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum 7G8-mdr7G8 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID1899007 | Antiplasmodial activity against CQ-susceptible Plasmodium falciparum 3D7 assessed as inhibition of parasite growth measured after 48 hrs by SYBR Green 1 dye based fluorescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. |
| AID763616 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected in Swiss mouse assessed as suppression of parasitaemia level at 10 mg/kg, po for 4 days relative to control | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID1563888 | Antiplasmodial activity against chloroquine-resistant asexual blood stage of Plasmodium falciparum K1 by LDH assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights. |
| AID1457209 | Antimalarial activity against Plasmodium falciparum TM90C2A infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation count | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID1323218 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in parasitemia after 72 hrs by lactate dehydrogenase assay | 2016 | Journal of natural products, 07-22, Volume: 79, Issue:7 | Cyclopeptide Alkaloids from Hymenocardia acida. |
| AID768459 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as abnormal mitochondria at 40 uM after 0.5 hrs by MitoTracker Red CMXRos-based fluorescence microscopic analysis relative to untreated contr | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1188451 | Antimalarial activity against tightly synchronized Plasmodium falciparum W2 assessed as parasite stage accumulation index at trophozoites stages at 10 uM treated at 30 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cyt | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID477944 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum FCR3 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID1204113 | Cytotoxic activity against human HeLa cells assessed as cell viability at 100 ug/ml incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID529759 | Antimicrobial activity against Plasmodium falciparum at ring stage | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Stronger activity of human immunodeficiency virus type 1 protease inhibitors against clinical isolates of Plasmodium vivax than against those of P. falciparum. |
| AID242065 | Inhibition of Plasmodium falciparum cyclin-dependent kinase | 2004 | Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22 | A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors. |
| AID768487 | Antimalarial activity against trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as growth inhibition after 5 hrs by SYBR Green-I fluorescence assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID159013 | Inhibitory concentration against Plasmodium falciparum K1 infected erythrocytes | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Synthesis and in vitro evaluation of 9-anilino-3,6-diaminoacridines active against a multidrug-resistant strain of the malaria parasite Plasmodium falciparum. |
| AID456798 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
| AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID277797 | Toxicity against murine J774 macrophage cells | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Synthesis and antimalarial activity of new isotebuquine analogues. |
| AID538324 | Inhibition of Plasmodium falciparum-mediated human hemoglobin degradation at 100 uM | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone. |
| AID1585805 | Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 asynchronous cultures infected in human erythrocytes | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis of isatin based N |
| AID333071 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2004 | Journal of natural products, Aug, Volume: 67, Issue:8 | Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases. |
| AID453366 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Bre1 assessed as inhibition of [3H]hypoxanthine incorporation | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID212501 | Compound was tested for antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS, activity is expressed as the mortality rate at a concentration of 1 mg/kg. in experiment 1; 5 out of 5 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID477946 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum K2 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID704124 | Mutagenicity against Salmonella typhimurium TA100 assessed as revertants at 40 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID513991 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 48 hrs by SYBR Green 1-based fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14 | New antimalarials with a triterpenic scaffold from Momordica balsamina. |
| AID564285 | Antimalarial activity against Plasmodium falciparum W2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID597176 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 by FACS-based assay | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies. |
| AID1537214 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Antiviral Compounds from Codiaeum peltatum Targeted by a Multi-informative Molecular Networks Approach. |
| AID468919 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining method | 2009 | Journal of natural products, Aug, Volume: 72, Issue:8 | Antimalarial benzylisoquinoline alkaloid from the rainforest tree Doryphora sassafras. |
| AID272290 | Viability of human HeLa cells at 200 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID606928 | Antimalarial activity against GFP-transfected Plasmodium berghei strain ANKA infected in NMRI mouse assessed as reduction in parasitemia at 10 mg/kg/day, po administered for 4 consecutive days measured 24 hrs after last treatment by FACS analysis relative | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Antimalarial pyrido[1,2-a]benzimidazoles. |
| AID499810 | Antimalarial activity against Plasmodium falciparum W2 after 72 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
| AID569316 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by parasite LDH assay | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores. |
| AID355991 | Antileishmanial activity against Leishmania donovani promastigotes expressing luciferase | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge. |
| AID232836 | Vacuolar accumulation ratio (VAR) on beta-hematin inhibitory activity | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID284374 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. |
| AID1639284 | Antiplasmodial activity against drug-resistant Plasmodium falciparum Dd2 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens. |
| AID1229883 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 14 post infection by Giemsa st | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID678310 | Inhibition of Plasmodium falciparum PLM2 using Lys-Glu-Phe-Val-Phe-NPhe-Ala-Leu-Lys as substrate by spectrophotometry | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID105829 | Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 1 uM concentration | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID543844 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected ICR mouse assessed as survival of mouse at 25 mg/kg/day, po for 4 days measured after 30 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID1808279 | Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene ass | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID343599 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 in human erythrocytes by [3H]hypoxanthine uptake | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors. |
| AID748223 | Cytotoxicity against human HepG2 cells after 48 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria. |
| AID355965 | Cytotoxicity against african green monkey Vero cells at 4.7 ug/mL | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Antimicrobial and antiparasitic (+)-trans-hexahydrodibenzopyrans and analogues from Machaerium multiflorum. |
| AID1204843 | Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by neutral red assay | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID1174526 | Cytotoxicity against African green monkey Vero cells after 72 hrs by neutral red assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | 4-Aminoquinoline-pyrimidine hybrids: synthesis, antimalarial activity, heme binding and docking studies. |
| AID158703 | In vitro inhibitory concentration against Plasmodium falciparum F32 | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | The imidazo[2,1-a]isoindole system. A new skeletal basis for antiplasmodial compounds. |
| AID1655713 | Selectivity index, ratio of IC50 for human AB943 cells to IC50 for antiplasmodial activity against chloroquine resistant Plasmodium falciparum FcB1/Colombia infected in human erythrocytes | |||
| AID362469 | Antimalarial activity against Plasmodium falciparum 3D7 in human erythrocytes after 48hrs by [3H]hypoxanthine uptake | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Enhanced antimalarial activity of novel synthetic aculeatin derivatives. |
| AID380422 | Selectivity index, ratio of ED50 for human KB cells to IC50 for Plasmodium falciparum W2 | 2006 | Journal of natural products, Mar, Volume: 69, Issue:3 | Antimalarial compounds from Grewia bilamellata. |
| AID1776174 | Antimalarial activity against asexual blood stage drug-sensitive Plasmodium falciparum NF54 infected in erythrocytes assessed as reduction in parasitemia incubated up to 72 hrs by [3H]hypoxanthine incorporation assay | |||
| AID1829871 | Antimalarial activity against Plasmodium berghei ANKA infected in Balb/c mouse assessed as suppression of parasitemia at 50 mg/kg, po administered for 4 days by microscopic analysis | |||
| AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
| AID317958 | Relative IC50 against Plasmodium falciparum K1 and 3D7 | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum. |
| AID564235 | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID372492 | Cmax in patient with kidney disease at 300 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast. |
| AID1182769 | Antiplasmodial activity against Plasmodium berghei infected in mouse assessed as reduction in parasitemia at 30 mg/kg treated with four once daily doses | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
| AID1204133 | Toxicity in Plasmodium berghei NK65 infected Swiss albino mouse assessed as mouse survival at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 12 post infection relative to untreated control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1636440 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID404784 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FCB after 72 hrs by SYBR green assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID294067 | Antiparasitic activity against chloroquine, pyrimethamine-resistant Plasmodium falciparum K1 in erythrocytes by [3H]hypoxanthine uptake | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis and antiplasmodial activity of new N-[3-(4-{3-[(7-chloroquinolin-4-yl)amino]propyl}piperazin-1-yl)propyl]carboxamides. |
| AID1696538 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes incubated for 72 hrs by SYBR green staining based fluorescence assay | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Structural hybridization as a facile approach to new drug candidates. |
| AID1894310 | Inhibition of hemozoin formation in sorbitol-synchronized early ring stage plasmodium falciparum NF54 trophozoites assessed as increase in free heme-Fe level at 0.5 to 3 times EC50 incubated for 32 hrs by flow cytometry analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID553544 | Drug level in malaria patient whole blood on day 4 | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID502865 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity. |
| AID1808477 | Modulation of full length human NOR1 expressed in PC12 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID763615 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected in Swiss mouse assessed as mean survival time at 10 mg/kg, po for 4 days | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID1055856 | Antimalarial activity against ring-stage Plasmodium falciparum 3D7 assessed as schizonticidal activity after 42 hrs | 2013 | European journal of medicinal chemistry, , Volume: 70 | Skeletal hybridization and PfRIO-2 kinase modeling for synthesis of α-pyrone analogs as anti-malarial agent. |
| AID477939 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum 8425 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID1593296 | Inhibition of Plasmodium falciparum cytochrome b-c1 | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials. |
| AID472375 | Antimalarial activity against chloroquine, pyrimethamine, proguanil-resistant Plasmodium falciparum infected in human erythrocytes after 48 hrs by flow cytometry | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Synthesis and biological evaluation of new heterocyclic quinolinones as anti-parasite and anti-HIV drug candidates. |
| AID667436 | Antiplasmodial activity against Plasmodium falciparum NF54 infected in human erythrocytes after 24 hrs by geimsa staining | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain. |
| AID72011 | Compound was tested for cytotoxicity against FM3A mouse mammary cells. | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | New type of febrifugine analogues, bearing a quinolizidine moiety, show potent antimalarial activity against Plasmodium malaria parasite. |
| AID1174542 | Binding affinity to mu-oxo-heme (unknown origin) assessed as binding constant at pH 5.8 | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | 4-Aminoquinoline-pyrimidine hybrids: synthesis, antimalarial activity, heme binding and docking studies. |
| AID1188918 | Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for Plasmodium falciparum K1 | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents. |
| AID1198731 | Antimalarial activity against asynchronic culture of Plasmodium falciparum NF54 assessed as parasite growth inhibition after 48 hrs by ethidium bromide staining-based spectrofluorometric analysis | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | An efficient synthesis of new caffeine-based chalcones, pyrazolines and pyrazolo[3,4-b][1,4]diazepines as potential antimalarial, antitrypanosomal and antileishmanial agents. |
| AID498018 | Inhibition of GST-fused Plasmodium falciparum recombinant CDPK1 expressed in Escherichia coli Rosetta 2 assessed as inhibition of [gamma-33P]ATP incorporation into substrate peptide by scintillation counting | 2008 | Nature chemical biology, Jun, Volume: 4, Issue:6 | Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. |
| AID422749 | Cytotoxicity against african green monkey Vero cells at 4760 ng/mL | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1 | Indolizidine, antiinfective and antiparasitic compounds from Prosopis glandulosa var. glandulosa. |
| AID1457207 | Antimalarial activity against Plasmodium falciparum T9/94 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation countin | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID1544796 | Antimicrobial activity against Pseudomonas aeruginosa assessed as zone of inhibition at 2000 uM/disk after 24 hrs by disk diffusion method | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13 | Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones. |
| AID406391 | Cytotoxicity against human MCF7 cells assessed as [3H]hypoxanthine incorporation | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID441888 | Cytotoxicity against C57B1/6J mouse splenic lymphocyte after 24 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum. |
| AID1191134 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I-based fluorescence method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters. |
| AID1185518 | Antimalarial activity against chloroquine-resistant ring stage Plasmodium falciparum W2 assessed as parasitemia after 48 hrs by flow cytometry | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | β-amino-alcohol tethered 4-aminoquinoline-isatin conjugates: synthesis and antimalarial evaluation. |
| AID1193544 | Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 infected in human red blood cells assessed as reduction in parasite viability after 48 hrs by [3H]-hypoxanthine incorporation assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities. |
| AID1405074 | Antiplasmodial activity against synchronized ring stage of chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by SYBR Green 1 dye based fluorescence assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Facile synthesis of vanillin-based novel bischalcones identifies one that induces apoptosis and displays synergy with Artemisinin in killing chloroquine resistant Plasmodium falciparum. |
| AID725352 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBC by flow cytometry analysis | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Addition of thiols to o-quinone methide: new 2-hydroxy-3-phenylsulfanylmethyl[1,4]naphthoquinones and their activity against the human malaria parasite Plasmodium falciparum (3D7). |
| AID775981 | Cytotoxicity against mouse NIH/3T3 cells assessed as cell viability after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents. |
| AID160044 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR3 | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | New type of febrifugine analogues, bearing a quinolizidine moiety, show potent antimalarial activity against Plasmodium malaria parasite. |
| AID568766 | Antimalarial activity against chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen". |
| AID1771333 | Antimalarial activity against Plasmodium falciparum Cam3.1 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps, pf-kelch13 mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillati | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials. |
| AID1327394 | Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin. |
| AID157674 | Antiparasitic activity for Plasmodium falciparum 3D7 | 2001 | Bioorganic & medicinal chemistry letters, Oct-08, Volume: 11, Issue:19 | Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine. |
| AID212377 | Compound was tested for antimalarial activity in mice (Mus musculus), infected with Plasmodium berghei N., activity is expressed as the mortality rate at a concentration of 10 mg/kg. in experiment 1; 5 out of 5 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID337539 | Selectivity index, ratio of ED50 for human COL1 cells to ED50 for chloroquine-resistant Plasmodium falciparum W2 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID221572 | Percent of infected erythrocytes in Blood schizonticidal activity against Plasmodium chabaudi in mice at a concentration of 10 mg/kg/day on day 5 | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
| AID619716 | Antimalarial activity against erythrocyte stages of chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes by lactate dehydrogenase assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). |
| AID423726 | AUC (0 to infinity) in Paua New Guinean children with uncomplicated malaria at 10 mg/kg daily for 3 days | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. |
| AID243140 | Binding constant dissolved in DMSO against hematin receptor at pH 7.4 (HEPES Buffer) upon incubation at 23 degree C | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: design, construction, characterization, and pharmacology of metaquine. |
| AID356093 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 by LDH reporter assay | 2003 | Journal of natural products, Jul, Volume: 66, Issue:7 | Antiparasitic alkaloids from Psychotria klugii. |
| AID446173 | Selectivity index, ratio of CC50 for human KB cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and antiplasmodial activity of new indolone N-oxide derivatives. |
| AID356386 | Antimalarial activity against Plasmodium falciparum K1 | 2003 | Journal of natural products, Sep, Volume: 66, Issue:9 | Ancistrotanzanine A, the first 5,3'-coupled naphthylisoquinoline alkaloid, and two further, 5,8'-linked related compounds from the newly described species Ancistrocladus tanzaniensis. |
| AID336325 | Antimalarial activity against mefloquine-resistant Plasmodium falciparum D6 (Sierra Leone) after 24 to 60 hrs by [G-H3]hypoxanthine uptake | 1993 | Journal of natural products, Nov, Volume: 56, Issue:11 | A new antimalarial quassinoid from Simaba guianensis. |
| AID522073 | Peripheral compartment volume of distribution in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic base model at 450 mg/day, po administered as three divided doses in presence of sulfadoxine-pyrimethamine by HPLC meth | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID157865 | In vitro inhibitory activity against chloroquine-sensitive Plasmodium falciparum HB3 | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain. |
| AID336129 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2002 | Journal of natural products, Sep, Volume: 65, Issue:9 | Antiplasmodial compounds from Cochlospermum tinctorium. |
| AID1306833 | Inhibition of beta-hematin formation | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Bistacrine derivatives as new potent antimalarials. |
| AID278816 | Antimalarial activity against Plasmodium falciparum D10 | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Synergistic interactions of the antiretroviral protease inhibitors saquinavir and ritonavir with chloroquine and mefloquine against Plasmodium falciparum in vitro. |
| AID717115 | Antimalarial activity against chloroquine-sensitive ring stage plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24 | Synthesis and antimalarial evaluation of a screening library based on a tetrahydroanthraquinone natural product scaffold. |
| AID378863 | Antimalarial activity reduced schizont maturation in Plasmodium berghei at 10 ug/mL after 16 hrs | 2006 | Journal of natural products, Oct, Volume: 69, Issue:10 | Antimalarial 4-phenylcoumarins from the stem bark of Hintonia latiflora. |
| AID1272516 | Resistant index, ratio of IC50 for chloroquine, quinine and pyrimethamine-resistant Plasmodium falciparum W2 to IC50 for mefloquine-resistant Plasmodium falciparum D6 | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | In vitro efficacy of 2,N-bisarylated 2-ethoxyacetamides against Plasmodium falciparum. |
| AID404601 | Selectivity index, Ratio of IC50 for L6 cells to IC50 for Plasmodium falciparum K1 | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense. |
| AID635306 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by beta liquid scintillation counting method | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives. |
| AID158375 | In vitro antimalarial activity against Plasmodium falciparum D2 | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | Novel endoperoxide antimalarials: synthesis, heme binding, and antimalarial activity. |
| AID522070 | Central compartment volume of distribution in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic final covariate model at 450 mg/day, po administered as three divided doses in presence of sulfadoxine-pyrimethamine by H | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1415878 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 3 days by SYBR green1 dye based assay | 2017 | MedChemComm, May-01, Volume: 8, Issue:5 | Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti- |
| AID664775 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in O-positive human RBC assessed as [3H]-hypoxanthine incorporation after 48 hrs by scintillation counting | 2012 | ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1 | Sphingolipid analogues inhibit development of malaria parasites. |
| AID524783 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by 1536-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID159003 | Effective concentration for gametocidal activity against Plasmodium falciparum FDL-HD; No data | 2002 | Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24 | Isolation and antimalarial activity of peroxydisulfate oxidation products of primaquine. |
| AID509192 | Inhibition of TLR7/TLR9-mediated upregulation of indoleamine 2,3-dioxygenase expression in aldrithiol-2-treated HIV1 MN-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID1143814 | Antimicrobial activity against chloroquine and mefloquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by SYBR Green I assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, synthesis and biological evaluation of novel 4-alkapolyenylpyrrolo[1,2-a]quinoxalines as antileishmanial agents--part III. |
| AID558836 | Antimalarial activity against Plasmodium falciparum IMT A4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID655688 | Antiplasmodial activity Plasmodium falciparum 3D70087/N9 infected in NODscidIL2Rgammac-/- mouse assessed as reduction of parasitemia administered 3 days after infection measured on day 3 to 7 by flow cytometry | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11 | Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS). |
| AID1513842 | Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition and measured after 24 hrs by liquid scintillation counting | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains. |
| AID318188 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. |
| AID285479 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 2 & 3) | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
| AID159747 | Inhibition of Plasmodium falciparum GP1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker. |
| AID268569 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by pLDH reporter assay | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Exploration of a new type of antimalarial compounds based on febrifugine. |
| AID1162960 | Gametocytocidal activity against transgenic Plasmodium falciparum NF54-pfs16-GFP late stage gametocytes at 120 uM after 72 hrs by mitotracker red CM-H2XRos dye based confocal imaging assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides: a new class of antiplasmodial compounds. |
| AID1431678 | Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication after 24 hrs by RT-PCR method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives, synthesized by thermal and ultrasonic means, are endowed with anti-Zika virus activity. |
| AID1472105 | Increase in free heme levels in chloroquine-sensitive synchronized ring stage of Plasmodium falciparum NF54 after 32 hrs by flow cytometric analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 | 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. |
| AID1887443 | Antimalarial activity against blood stage chloroquine-sensitive Plasmodium falciparum 3D7 assessed as reduction in parasite growth incubated for 72 hrs by SYBR Green dye based fluorescence assay | |||
| AID360362 | Antimalarial activity after 48 hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake | 2007 | The Journal of biological chemistry, Jan-26, Volume: 282, Issue:4 | In vitro efficacy, resistance selection, and structural modeling studies implicate the malarial parasite apicoplast as the target of azithromycin. |
| AID667440 | Antiplasmodial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as decrease in parasitemia measured on day 4 post-treatment by geimsa staining (Rvb = 3.28 +/- 0.11%) | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain. |
| AID341407 | Dissociation constant, pKa of the compound | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | 2-tert-butyl-8-quinolinamines exhibit potent blood schizontocidal antimalarial activity via inhibition of heme crystallization. |
| AID1201510 | Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID562552 | Antiplasmodial activity against Plasmodium vinckei petteri infected in po dosed CD mouse assessed as mean survival time at 5 mg/kg/day, ip for 4 days measured upto day 21 post-infection | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID1439476 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Synthesis, antimalarial activity, heme binding and docking studies of N-substituted 4-aminoquinoline-pyrimidine molecular hybrids. |
| AID1829857 | Selectivity index, ratio of CC50 for human HEK293 cells to IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum INDO | |||
| AID1717748 | Antiviral activity against 2019-nCoV BetaCoV/Wuhan/WIV04/2019 infected in African green monkey VeroE6 cells assessed as reduction in viral yield preincubated with virus for 1 hr followed by cell infection and measured after 2 hrs by qRT-PCR method | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID1409624 | hERG binding assays: Displacement of [3H]-Dofetilide (5 nM final) from hERG membranes obtained from HEK293 cells | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID316377 | Antimalarial activity against Plasmodium falciparum W2 in MSF assay | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Synthesis and heme-binding correlation with antimalarial activity of 3,6-bis-(omega-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone. |
| AID1647972 | Antiplasmodial activity against asexual erythrocytic stage of Plasmodium falciparum 3D7 assessed as reduction in parasite growth after 72 hrs by LDH assay | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Ikoamide, an Antimalarial Lipopeptide from an |
| AID1156430 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and in vitro evaluation of 4-trichloromethylpyrrolo[1,2-a]quinoxalines as new antiplasmodial agents. |
| AID1504883 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based confocal microplate imaging method | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12 | Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana. |
| AID1196102 | Antiplasmodial activity against chloroquine-resistant asexual erythrocytic stage of Plasmodium falciparum Dd2 assessed as [3H]-hypoxanthine incorporation by lactate dehydrogenase assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis of functionalized 3-, 5-, 6- and 8-aminoquinolines via intermediate (3-pyrrolin-1-yl)- and (2-oxopyrrolidin-1-yl)quinolines and evaluation of their antiplasmodial and antifungal activity. |
| AID1373908 | Antimalarial activity against chloroquine-susceptible Plasmodium berghei ANKA infected in Balb-C mouse assessed as parasitemia at 10 mg/kg, ip administered once daily for 4 days measured post last dose by Giemsa staining based method (Rvb = 65.8 +/- 4.38% | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
| AID290012 | Antiplasmodial activity against Plasmodium falciparum D6 | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Synthesis and antimalarial evaluation of a series of piperazinyl flavones. |
| AID568765 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen". |
| AID1763365 | Binding affinity to monomeric heme in HEPES buffer at pH 7.4 | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | A trio of quinoline-isoniazid-phthalimide with promising antiplasmodial potential: Synthesis, in-vitro evaluation and heme-polymerization inhibition studies. |
| AID1140162 | Antimalarial activity against Plasmodium yoelii MR4 MRA-428 infected in mouse CF1 assessed as reduction on parasite burden at 64 mg/kg administered through oral gavage once daily for 4 days | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers. |
| AID259771 | Antimalarial activity against Plasmodium yoelii infected Swiss mice (Mus musculus) at 48 mg/kg peroral dose | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | 8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro (4.5) decane, a new 1,2,4-trioxane effective against rodent and simian malaria. |
| AID636377 | Acute toxicity in po dosed Sprague-Dawley rat assessed as maximum tolerated dose | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID482244 | Antiplasmodial activity against Plasmodium berghei ANKA infected in mice (Mus musculus) assessed as mice (Mus musculus) survival at 10 mg/kg, intraperitoneal for 5 consecutive days measured on day 11 post parasitic infection | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis and evaluation of alpha-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials. |
| AID1755247 | Disaggregation of copper-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 50 uM measured after 24 hrs by ThT fluorescence assay | |||
| AID1859909 | Inhibition of hemin (unknown origin) assessed as inhibition of heme polymerization by measuring reduction in beta-hematin formation at 1 mM measured after 48 hrs by microplate reader assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID660300 | Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Amino acid, dipeptide and pseudodipeptide conjugates of ring-substituted 8-aminoquinolines: synthesis and evaluation of anti-infective, β-haematin inhibition and cytotoxic activities. |
| AID300107 | Selectivity index, ratio of CC50 for human KB cells to IC50 for Plasmodium falciparum K1 | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Anti-malarial activity of N6-modified purine analogues. |
| AID256081 | Antiplasmodial activity for Plasmodium falciparum FcB1 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities. |
| AID1247013 | Cytotoxicity against human HepG2A16 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype. |
| AID1405076 | Antiplasmodial activity against synchronized ring stage of chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes after 48 hrs by SYBR Green 1 dye based fluorescence assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Facile synthesis of vanillin-based novel bischalcones identifies one that induces apoptosis and displays synergy with Artemisinin in killing chloroquine resistant Plasmodium falciparum. |
| AID1494324 | Induction of cell proliferation in C57BL/6 mouse hippocampal neurons in DG region assessed as BrdU-incorporation at 0.5 uL/hr, icv for 7 days by immunohistochemical analysis (Rvb = 7.8%) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID630943 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in po dosed NMRI mouse assessed as reduction in parasitemia administered as single dose after 72 hrs by flow cytometry | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID263348 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | Synthesis and evaluation of febrifugine analogues as potential antimalarial agents. |
| AID1858879 | Antimalarial activity against Plasmodium falciparum Dd2 treated for 48 hrs followed by hypoxanthine addition | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Antimalarial application of quinones: A recent update. |
| AID441886 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 72 hrs by fluorescence based method | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum. |
| AID754524 | Inhibition of hemozoin formation in 9.7 M acetate buffer at pH 4.8 at 60 degC after 2 hrs by microtiter-based high-throughput assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID760424 | Cytotoxicity against rat L6 cells after 70 hrs by Alamar Blue assay | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine. |
| AID763603 | Clearance in Sprague-Dawley rat at 5 mg/kg, po | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID554758 | Antimalarial activity against Plasmodium berghei NK-65 infected in Swiss Webster mouse assessed as cure from parasite infection at 30 mg/kg, ip QD for 3 days administered 2 hrs post infection measured on day 28 | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID622802 | Ratio of EC50 for human HepG2 cells to EC50 for Plasmodium falciparum K1 infected in human erythrocytes | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | Synthesis and evaluation of 7-substituted 4-aminoquinoline analogues for antimalarial activity. |
| AID461611 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss Webster mice (Mus musculus) assessed as average parasitaemia at 200 mg/kg, perorally administered 1 day after infection measured after 21 days post infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID502864 | Cytotoxicity against rat L6 cells | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity. |
| AID322131 | In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. |
| AID1899029 | Selectivity index, ratio of IC50 for antiplasmodial activity against CQ-susceptible Plasmodium falciparum 3D7 to IC50 for antiplasmodial activity CQ-resistant Plasmodium falciparum W2 by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. |
| AID675404 | Antimalarial activity against asexual erythrocyte stages of chloroquine-resistant Plasmodium falciparum Dd2 | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Synthesis and in vitro antimalarial activity of a series of bisquinoline and bispyrrolo[1,2a]quinoxaline compounds. |
| AID1241109 | Inhibition of beta haematin formation after 5 to 6 hrs by pyridine-ferrichrome method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. |
| AID1422824 | Selectivity index, ratio of cytotoxic concentration for human MRC5 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme. |
| AID511254 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum HB3 by ELISA | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda. |
| AID644818 | Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents. |
| AID515053 | Drug level in chloroquine-sensitive Plasmodium falciparum D6 digestive vacuole assessed as ratio of drug level in vacuole to medium at 5 uM after 1 hr | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID93345 | The compound was tested for the dose required to cause 50% suppression of Plasmodium berghei growth in mice. | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID458587 | Cytotoxicity against human 184B5 cells after 48 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4 | Design and synthesis of anti-breast cancer agents from 4-piperazinylquinoline: a hybrid pharmacophore approach. |
| AID114292 | Antimalarial efficacy against Plasmodium berghei in mice (Mus musculus) when administered subcutaneously each day for 4 days to five mice (Mus musculus) per dose regimen | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | Antimalarial simplified 3-aryltrioxanes: synthesis and preclinical efficacy/toxicity testing in rodents. |
| AID1892265 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human RBC assessed as reduction in parasite growth after 72 hrs by LDH assay | 2022 | Bioorganic & medicinal chemistry, 07-15, Volume: 66 | New antimalarials identified by a cell-based phenotypic approach: Structure-activity relationships of 2,3,4,9-tetrahydro-1H-β-carboline derivatives possessing a 2-((coumarin-5-yl)oxy)alkanoyl moiety. |
| AID421810 | Cytotoxicity against human MCF7 cells assessed as [3H]hypoxanthin incorporation after 24 to 72 hrs | 2009 | Journal of natural products, May-22, Volume: 72, Issue:5 | Cytotoxic and antiplasmodial xanthones from Pentadesma butyracea. |
| AID1199921 | Antiprotozoal activity against intraerythrocytic stage of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Antiprotozoal activity and DNA binding of dicationic acridones. |
| AID340595 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by almar blue assay | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Kinetic studies and bioactivity of potential manzamine prodrugs. |
| AID1688326 | Antimalarial activity against Plasmodium falciparum 3D7 asexual forms incubated for 72 hrs by luminescence method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID644816 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7A infected in human A-positive erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 48 hrs by semi-automated microdilution technique | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents. |
| AID285478 | Antimalarial activity against Plasmodium yoelii nigeriensis infected subcutaneously dosed mice (Mus musculus) | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
| AID107433 | In vitro effect on methemoglobin reductase activity in blood of dog at 33 uM concentration | 1999 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 9, Issue:5 | Synthesis of bisquinolines and their in vitro ability to produce methemoglobin in canine hemolysate. |
| AID636371 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum VS/1 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID1070212 | Cytotoxicity against CHO cells by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity. |
| AID268572 | Antimalarial activity against Plasmodium berghei NK65 infected ICR mice (Mus musculus) peroral dose | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Exploration of a new type of antimalarial compounds based on febrifugine. |
| AID553554 | Toxicity in malaria patient assessed as vomiting on day 1 after treatment at quartile 4 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID157874 | Inhibition of 1-monooleoyl glycerol (MOG) induced beta-hematin formation | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID764883 | Antiprotozoal activity against chloroquine- and pyrimethamine-resistant Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom. |
| AID722962 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Isolation and identification of β-hematin inhibitors from Flacourtia indica as promising antiplasmodial agents. |
| AID412363 | Antimalarial activity after 24 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human A+ erythrocytes by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID1779352 | Antiplasmodial activity against bloodstream form of Plasmodium falciparum NF54 transfected assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Synthesis, in vitro antiprotozoal activity, molecular docking and molecular dynamics studies of some new monocationic guanidinobenzimidazoles. |
| AID515031 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mice (Mus musculus) assessed as survival rate at 30 mg/kg, perorally administered as single dose | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID1201514 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID159625 | In vitro inhibitory activity against chloroquine-sensitive Plasmodium falciparum African D6 | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Mixed steroidal 1,2,4,5-tetraoxanes: antimalarial and antimycobacterial activity. |
| AID355989 | Antimalarial activity against Plasmodium falciparum D6 | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge. |
| AID553552 | Toxicity in malaria patient assessed as vomiting on day 1 after treatment at quartile 2 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID1155331 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for asexual blood stage of Plasmodium falciparum 3D7 | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
| AID630944 | Ratio of cytotoxicity against rat L6 cells to IC50 for chloroquine-sensitive Plasmodium falciparum K1 | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID595214 | Antimalarial activity against Plasmodium falciparum D6 | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus. |
| AID624622 | Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID630761 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse assessed as reduction in parasitemia at 10 mg/kg, po administered as single dose after 72 hrs by flow cytometry | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID768176 | Binding affinity to Escherichia coli pUC18 DNA at 30 uM by fluorescence assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID519202 | Antimicrobial activity against slow-growing synchronous Plasmodium falciparum by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID392461 | Antileishmanial activity against Leishmania donovani | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity. |
| AID1815873 | Antiplasmodial activity against chloroquine, pyrimethamine and mefloquine-resistant asexual blood stage of Plasmodium falciparum Dd2 assessed as reduction in parasite growth after 72 hrs by SYBR green I staining based fluorescence assay | 2022 | ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3 | Enantiopure Benzofuran-2-carboxamides of 1-Aryltetrahydro-β-carbolines Are Potent Antimalarials |
| AID510919 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 50 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measure | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
| AID554759 | Toxicity in Plasmodium berghei NK-65 infected Swiss Webster mouse at 30 mg/kg, ip QD for 3 days | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID1228732 | Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for Sindbis virus strain HRsp | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID255858 | In vitro antimalarial activity for Plasmodium falciparum W2 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives. |
| AID1763364 | Binding affinity to monomeric heme in MES buffer at pH 5.6 | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | A trio of quinoline-isoniazid-phthalimide with promising antiplasmodial potential: Synthesis, in-vitro evaluation and heme-polymerization inhibition studies. |
| AID151361 | In vitro efficacy for chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24 | A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline. |
| AID1894309 | Inhibition of hemozoin formation in sorbitol-synchronized early ring stage plasmodium falciparum NF54 trophozoites assessed as increase in free heme level at 0.5 to 3 times EC50 incubated for 32 hrs by flow cytometry analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID1673539 | Antimalarial activity against Plasmodium chabaudi ASS infected in NIH mouse assessed as inhibition of parasitemia at 10 mg/kg, po qd for 4 days starting from 4 hrs post-parasite inoculation and measured at 24 hrs after last-drug treatment by Peter's 4-day | |||
| AID419129 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 molecules of heme to 1 equivalent of drug in presence of 5 mM CTAB by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID99681 | In vitro cytotoxicity against mammalian L6 cells; ND = not determined | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. |
| AID606262 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction of parasitemia level at 0.032 uM after 3 days by Geimsa staining based light microscopic analysis (Rvb = 2.55 +/- 0.21%) | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | A new class of phenazines with activity against a chloroquine resistant Plasmodium falciparum strain and antimicrobial activity. |
| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID564289 | Antimalarial activity against Plasmodium falciparum PA assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID579588 | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by microtiter plate scintillation counting | 2011 | Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5 | An automated, polymer-assisted strategy for the preparation of urea and thiourea derivatives of 15-membered azalides as potential antimalarial chemotherapeutics. |
| AID491990 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hrs by LDH assay | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Bioactive 1,4-dihydroxy-5-phenyl-2-pyridinone alkaloids from Septoria pistaciarum. |
| AID1432053 | Anti-parasitic activity against CQ-sensitive Plasmodium falciparum D10 assessed as growth inhibition by measuring increase in LDH release after 72 hrs by spectrophotometric method | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure-Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents. |
| AID775984 | Inhibition of papaya papain using Z-Leu-Leu-Arg-AMC as substrate after 30 mins by fluorescence microplate reader analysis | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents. |
| AID1405716 | Induction of mitotic arrest in human HeLa cells assessed as formation of disorganized spindles at 15 to 25 uM after 6 hrs by DAPI staining-based immunofluorescence analysis | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
| AID1403755 | Antimalarial activity against chloroquine-resistant/mefloquine-sensitive Plasmodium falciparum W2 ring stage forms infected in human erythrocytes assessed as reduction in parasite growth after 48 hrs by parasite LDH release assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Antimalarial naphthoquinones. Synthesis via click chemistry, in vitro activity, docking to PfDHODH and SAR of lapachol-based compounds. |
| AID318194 | Survival of Plasmodium Berghei ANKA infected BALB/c mice (Mus musculus) at 10 mg/kg, intraperitoneally | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. |
| AID1616475 | Antiprotozoal activity against erythrocytic stage of Plasmodium falciparum 3D7 incubated for 72 hrs by lactate dehydrogenase assay | 2019 | Journal of natural products, 10-25, Volume: 82, Issue:10 | Isolation and Total Synthesis of Mabuniamide, a Lipopeptide from an |
| AID1254177 | Antiplasmodial activity against multidrug resistant Plasmodium falciparum K1 infected in human erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines. |
| AID636370 | Antimalarial activity against Plasmodium falciparum TM4 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID1545511 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR Green1 dye based fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID564292 | Antimalarial activity against Plasmodium falciparum IMT Bres assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID517480 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A+ erythrocytes after 72 hrs by SYBR Green I assay | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. |
| AID1713138 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability up to 500 ug/L incubated for 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Polyvalent effect enhances diglycosidic antiplasmodial activity. |
| AID768733 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as reduction parasitemia at 51.5 mg/kg, ip treated 4 times per day for 3 days by Giemsa staining relative to control | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives. |
| AID1426240 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 infected in human RBC | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and evaluation of 4-aminoquinoline-purine hybrids as potential antiplasmodial agents. |
| AID1808471 | Modulation of full length human Nur77 expressed in PC12 cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID354807 | Antiplasmodial activity against Plasmodium falciparum D6 | 1996 | Journal of natural products, Jul, Volume: 59, Issue:7 | Antimalarial activity: the search for marine-derived natural products with selective antimalarial activity. |
| AID760221 | Inhibition of beta-hematin formation after 60 mins relative to beta-hematin | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids. |
| AID700788 | Selectivity ratio of IC50 for plasmodium falciparum 3D7A to IC50 for human 5HT2c receptor | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5 | A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. |
| AID461596 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss Webster mice (Mus musculus) assessed as inhibition of parasitaemia at 200 mg/kg, perorally administered 1 day after infection measured after 5 days post infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID497108 | Antimalarial activity against Plasmodium falciparum infected in human O+ erythrocytes after 48 hrs by HRP2-ELISA method | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents. |
| AID1655711 | Antiplasmodial activity against chloroquine resistant Plasmodium falciparum FcB1/Columbia infected in human erythrocytes preincubated for 24 hrs followed by [3H]-hypoxanthine addition and measured after 24 hrs by liquid scintillation analysis | |||
| AID361515 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. |
| AID1533545 | Inhibition of lysosome fusion with autophagosome in human HeLa cells harboring GFP-LC3 assessed as increase in GFP-LC3-2 clustering at <50 uM after 6 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID701107 | Mutagenicity against Salmonella typhimurium TA100 assessed as revertants at 2.5 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID736390 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum NF54 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Journal of natural products, Jan-25, Volume: 76, Issue:1 | Antibacterial and antiplasmodial constituents of Beilschmiedia cryptocaryoides. |
| AID1426426 | Antiparasitic activity against drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as growth inhibition after 48 hrs by SYBR green 1 dye-based flow cytometry | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
| AID1332933 | Binding affinity to monomeric heme (unknown origin) assessed as association constant at pH 5.6 by UV-titration method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 4, 5-Dihydrooxazole-pyrazoline hybrids: Synthesis and their evaluation as potential antimalarial agents. |
| AID1359635 | Ratio of IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring forms infected in human RBC incubated for 15 mins followed by compound removal and further incubation for 48 hrs by [3H]-hypoxanthine incorporation assa | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID1541831 | Antimalarial activity against asexual stage of Plasmodium falciparum Dd2 infected in erythrocytes assessed as reduction in parasite growth incubated for 48 hrs under hypoxic condition by Hoechst 33342 staining based flow cytometry | |||
| AID1440396 | Inhibition of biofilm formation of Candida albicans ATCC 90028 after 48 hrs in presence of voriconazole by XTT assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Tackling Fungal Resistance by Biofilm Inhibitors. |
| AID282103 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 as LDH activity after 48 hrs | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database. |
| AID490033 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum F32 after 48 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and preparation of aza-analogues of benzo[c]phenanthridine framework with cytotoxic and antiplasmodial activities. |
| AID294986 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by hypoxanthine uptake | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9 | In vitro efficiency of new acridyl derivatives against Plasmodium falciparum. |
| AID1155338 | Antimalarial activity against late stage gametocyte stage of Plasmodium falciparum NF54 after 72 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
| AID1699559 | Antiplasmodial activity against multidrug-resistant asexual blood stage Plasmodium falciparum K1 strain assessed as reduction in parasite growth after 72 hrs by NBT reagent based LDH assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and |
| AID775956 | Resistant index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | In vitro antimalarial activity, β-haematin inhibition and structure-activity relationships in a series of quinoline triazoles. |
| AID1405797 | Induction of autophagy in human HeLa cells assessed as increase in LC3-2 to LC3-1 ratio at 1.25 uM after 6 hrs by immunoblot analysis relative to control | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
| AID1815886 | In vivo antimalarial activity against blood stage transgenic Plasmodium berghei ANKA strain (PbGFP-Luccon) infected in swiss Webster mouse assessed as supression of parasitemia at 40 mg/kg, po administered once daily starting from day 2 to 6 post infectio | 2022 | ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3 | Enantiopure Benzofuran-2-carboxamides of 1-Aryltetrahydro-β-carbolines Are Potent Antimalarials |
| AID287842 | Survival rate in Plasmodium berghei NK65 infected JCL-ICR mice (Mus musculus) at 50 mg/kg body weight after 14 days | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Antimalarial activity of 1-aryl-3,3-dialkyltriazenes. |
| AID362473 | Selectivity index, ratio of CC50 for human K562 cells to IC50 for Toxoplasma gondii RH-beta1 | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Enhanced antimalarial activity of novel synthetic aculeatin derivatives. |
| AID432049 | Cytotoxicity against rat L6 cells | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes. |
| AID256010 | In vitro antimalarial activity for Plasmodium falciparum W2 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives. |
| AID480227 | Inhibition of CYP2C19 in human liver microsomes assessed as metabolite produced at 1 uM by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1229874 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 5 post infection by Giemsa sta | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID234982 | Ratio of average life span of compound-treated mice (100 mg/kg, ip, 3 days) to that of mice treated with 4''-butoxy-2,4-dimethoxychalcone (comp.41) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | Antimalarial alkoxylated and hydroxylated chalcones [corrected]: structure-activity relationship analysis. |
| AID666733 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as reduction in parasitemia at 30 mg/kg, po administered as 4 doses measured on day 4 post-infection by flow cytometry | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID456800 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
| AID452319 | Growth inhibition of human BT-483 cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID573265 | Lipid accumulation ratio of the compound | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID1239244 | Antiplasmodial activity chloroquinone-resistant Plasmodium falciparum Dd2 by parasite lactate dehydrogenase assay | 2015 | Journal of natural products, Aug-28, Volume: 78, Issue:8 | Syntheses and in Vitro Antiplasmodial Activity of Aminoalkylated Chalcones and Analogues. |
| AID302130 | Therapeutic index, ratio of LD50 for Swiss mice (Mus musculus) to IC50 for Plasmodium berghei infected Swiss mice (Mus musculus) | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Synthesis and evaluation of naphthyridine compounds as antimalarial agents. |
| AID427288 | Antimalarial activity against Plasmodium berghei infected ICR mice (Mus musculus) daily intraperitoneal dose for 4 days by Thompson test | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents. |
| AID244623 | Selectivity index measured as CC50/IC50 | 2004 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17 | Design, synthesis and antimalarial activity of a glyoxylylhydrazone library. |
| AID318215 | Antimalarial activity against Plasmodium chabaudi AS infected CD1 mice (Mus musculus) assessed as suppression of parasitaemia at 10 mg/kg, perorally after 4 days | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID658765 | Binding affinity to calf thymus DNA after 5 mins by spectrofluorometric analysis | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies. |
| AID361170 | Selectivity index, ratio of ED50 for human KB cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of natural products, Jun, Volume: 64, Issue:6 | Antimalarial compounds from Rhaphidophora decursiva. |
| AID1383217 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in red blood cells assessed as reduction in mature schizonts formation after 24 hrs by Giemsa-staining based assay | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study. |
| AID1532619 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in RBC after 72 hrs by LDH release assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | N-Substituted aminoquinoline-pyrimidine hybrids: Synthesis, in vitro antimalarial activity evaluation and docking studies. |
| AID1617791 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1 infected in RBC (unknown origin) incubated for 48 hrs by SYBR green dye based fluorescence analysis | 2019 | Journal of natural products, 12-27, Volume: 82, Issue:12 | Structural Characterization and Anti-infective Activity of 9,10-Seco-29-norcycloartane Glycosides Isolated from the Flowers of the Peruvian Medicinal Plant |
| AID675269 | Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 infected in RBCs incubated for 72 hrs by SYBRgreen dye based fluorometric assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | One pot efficient diversity oriented synthesis of polyfunctional styryl thiazolopyrimidines and their bio-evaluation as antimalarial and anti-HIV agents. |
| AID1378977 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1R/Colombia infected in human erythrocytes after 24 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID496886 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Quinolines and structurally related heterocycles as antimalarials. |
| AID346857 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 in human erythrocytes after 48 hrs by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID549523 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human A-positive red blood cells after 72 hrs by lactate dehydrogenase assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Antimalarials based on the dioxane scaffold of plakortin. A concise synthesis and SAR studies. |
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| AID590137 | Inhibition of Plasmodium falciparum W2 recombinant falcipain-2 | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. |
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| AID636823 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1/Colombia infected in human A+ve erythrocytes assessed as inhibition of [G-3H]hypoxanthine uptake preincubated for 24 hrs prior to [G-3H]hypoxanthine addition measured after 1 | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark. |
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| AID1494374 | Antialzheimer activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as reduction in amyloid beta burden at 30 mg/kg/day, po for 80 days by immunochemical staining-based analysis relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID218557 | Inhibitory activity against beta-hematin formation | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. |
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| AID773677 | Antiplasmodial activity against liver stage of Plasmodium berghei infected in human HuH7 cells assessed as parasite growth inhibition incubated for 1 hr prior to parasite infection measured after 48 hrs | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Structural optimization of quinolon-4(1H)-imines as dual-stage antimalarials: toward increased potency and metabolic stability. |
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| AID1732337 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as parasitemia at 10 mg/kg, po administered for 4 days and measured on day 5 post infection by Giemsa staining based microscopic analysis (Rvb = 100 %) | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization. |
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| AID1533507 | Hepatotoxicity in 72 hrs post fertilized transgenic l-fabp:EGFP zebrafish embryo assessed as change in liver fluorescence up to 80 uM up to 120 hrs post fertilization by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
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| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
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| AID1704611 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes incubated for 48 hrs by lactate dehydrogenase colorimetric enzyme assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry. |
| AID468175 | Cytotoxicity against human THP1 cells assessed as cell viability after 72 hrs by Alamar blue assay | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Synthesis and antiprotozoal activity of 4-arylcoumarins. |
| AID1558333 | Antiviral activity against Zika virus MR 766 infected in African green monkey Vero cells measured 5 days post infection by CellTiter Blue assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Drugs for the Treatment of Zika Virus Infection. |
| AID1764056 | Antimalarial activity against Plasmodium falciparum 3D7 assessed as inhibition of parasite growth | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Anti-protozoal and anti-fungal evaluation of 3,5-disubstituted 1,2-dioxolanes. |
| AID522084 | Cmax in Papua new Guinean pregnant women at 450 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID480237 | Permeability by PAMPA assay at pH 7.4 | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1145675 | Antibacterial activity against chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 assessed as reduction in growth | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID1437497 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method | |||
| AID1682556 | Antiviral activity against SARS-CoV-2 betaCoV/KOR/KCDC03/2020 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect measured after 24 hrs by immunofluorescence assay | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2. |
| AID728702 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. |
| AID300105 | Cytotoxicity against human KB cells | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Anti-malarial activity of N6-modified purine analogues. |
| AID337525 | Cytotoxicity against human KBV1 cells after 3 days by sulforhodamine B assay | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1239634 | Inhibition of beta-hematin formation | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Quinoline-based antimalarial hybrid compounds. |
| AID302171 | Antiplasmodial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum FcM29-Cameroon by [3H]hypoxanthine uptake | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modifications of the chemical structure of terpenes in antiplasmodial and antifungal drug research. |
| AID554563 | Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID1359642 | Antiplasmodial activity against Plasmodium falciparum 3D7 late stage forms infected in immunoliposome encapsulated compound pre-loaded human RBC by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID1234235 | Inhibition of cell proliferation of breast cancer cells (unknown origin) | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. |
| AID1377007 | Cytotoxicity against human 184B5 cells assessed as growth inhibition after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Design, synthesis and characterization of novel quinacrine analogs that preferentially kill cancer over non-cancer cells through the down-regulation of Bcl-2 and up-regulation of Bax and Bad. |
| AID477957 | Antiproliferative activity against human carmustine-resistant NCH-89 cells assessed as BrdU incorporation after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID1533494 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring malformation of notochord up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID257594 | Antimalarial activity as growth inhibition after 48 hrs against chloroquine-sensitive Plasmodium falciparum FDL-B | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Anti-malarial activity of Baylis-Hillman adducts from substituted 2-chloronicotinaldehydes. |
| AID246157 | Effective concentration for Plasmodium falciparum 3D7 | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4 | Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities. |
| AID151211 | In vitro activity against drug-resistant Plasmodium falciparum D6 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Antiplasmodial activity and cytotoxicity of bis-, tris-, and tetraquinolines with linear or cyclic amino linkers. |
| AID355951 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Antimicrobial and antiparasitic (+)-trans-hexahydrodibenzopyrans and analogues from Machaerium multiflorum. |
| AID502040 | Antimicrobial activity against Entamoeba histolytica HM-1:IMSS after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas. |
| AID564304 | Antimalarial activity against Plasmodium falciparum IMT K4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID1391090 | Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 40 residues) production measured after 24 hrs | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | New phenylaniline derivatives as modulators of amyloid protein precursor metabolism. |
| AID1649416 | Antimalarial activity against blood stage Plasmodium yoelii MR4 MRA-428 infected in CF1 mouse assessed as suppression of parasitemia administered once daily via oral gavage for 4 days starting from 24 hrs post-infection and measured post-last dose by Giem | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
| AID323682 | Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID404792 | Binding affinity to mu dimeric heme in aqueous solution at pH 7.5 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID418751 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
| AID474758 | Inhibition of recombinant Plasmodium falciparum falcipain-2 | 2010 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7 | Comparison of the antiplasmodial and falcipain-2 inhibitory activity of beta-amino alcohol thiolactone-chalcone and isatin-chalcone hybrids. |
| AID1360913 | Cell cycle arrest in human KYSE410 cells assessed as accumulation at S phase at 5 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry (Rvb = 22.3%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma. |
| AID1558336 | Cytotoxicity against African green monkey Vero cells after 5 days by CellTiter Blue assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Drugs for the Treatment of Zika Virus Infection. |
| AID619815 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum RSA11 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). |
| AID477962 | Binding affinity to pUC18 DNA containing 50% AT assessed as maximum melting temperature at 1 uM by spectrophotometry analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID116778 | Mean survival time calculated for the mice which died during 28 day observation period at the dose of 48 mg/kg/day orally | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Geraniol-derived 1,2,4-trioxanes with potent in-vivo antimalarial activity. |
| AID1859904 | Resistance index, ratio of IC50 for antiplasmodial activity against multidrug-resistant Plasmodium falciparum Dd2 to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID487389 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hrs by parasite LDH assay | 2010 | Journal of natural products, Jun-25, Volume: 73, Issue:6 | Manadoperoxides A-D from the Indonesian sponge Plakortis cfr. simplex. Further insights on the structure-activity relationships of simple 1,2-dioxane antimalarials. |
| AID515055 | Binding affinity to heme after 4 hrs by equilibrium binding assay | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID232807 | Selective toxicity- EC50 value of FM3A / EC50 value of Plasmodium falciparum | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity. |
| AID675417 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for multidrug-resistant Plasmodium falciparum K1 ring stage | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Tandem synthesis and in vitro antiplasmodial evaluation of new naphtho[2,1-d]thiazole derivatives. |
| AID1494295 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation at compound to amyloid beta ratio of 1:1 after 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID158849 | Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes | 2001 | Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3 | Structure-activity relationships of novel anti-malarial agents. Part 2: cinnamic acid derivatives. |
| AID1140760 | Resistance index, ratio of IC90 for CQ-resistant, MFQ-susceptible Plasmodium falciparum W2 clone Indochina 1 isolate to IC90 for CQ, MFQ-susceptible Plasmodium falciparum D6 clone Sierra 1/UNC isolate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Second generation steroidal 4-aminoquinolines are potent, dual-target inhibitors of the botulinum neurotoxin serotype A metalloprotease and P. falciparum malaria. |
| AID376975 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 | 2006 | Journal of natural products, May, Volume: 69, Issue:5 | Weakly antimalarial flavonol arabinofuranosides from Calycolpus warszewiczianus. |
| AID417105 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity. |
| AID316592 | Antiplasmodial activity against Plasmodium falciparum K1 in [3H]hypoxanthine incorporation assay | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity. |
| AID1201530 | Inhibition of hemozoin polymerization after 24 hrs by spectroscopic analysis | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID284261 | Cytotoxicity against LLC-PK1 cells by neutral red assay | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID1265981 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and bio-evaluation of novel quinolino-stilbene derivatives as potential anticancer agents. |
| AID630762 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse assessed as reduction in parasitemia at 30 mg/kg, po administered as single dose after 72 hrs by flow cytometry | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID722959 | Inhibition of H2O2-induced hemin degradation at 20 uM incubated for 20 mins prior to H2O2-induction measured after 30 mins by spectrophotometric analysis relative to control | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Isolation and identification of β-hematin inhibitors from Flacourtia indica as promising antiplasmodial agents. |
| AID93347 | The compound was tested for survival of the ICR mice (infected with Plasmodium berghei) as a symptom indicative of toxicity on day 4, at a dose of 0.5 mg/kg/day | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID1472100 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ANKA infected in C57BL/6 mouse assessed as supression of parasitemia at 30 mg/kg, po administered for 4 consecutive days starting at 2 hrs post infection by peter's test relative to co | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 | 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. |
| AID401070 | Activation of LPS-induced NO production in BCG-treated ICR mouse macrophages at 1 mg/kg/day, po administered for 3 days before BCG immunization measured after 24 hrs of LPS challenge by Griess reagent method | 1998 | Journal of natural products, Jun-26, Volume: 61, Issue:6 | Enhancement of NO production in activated macrophages in vivo by an antimalarial crude drug, Dichroa febrifuga. |
| AID1624379 | Toxicity in Swiss mouse infected with Plasmodium berghei ANKA assessed as change in body weight at 10 mg/kg, ip administered once daily for 5 days measured on 4 days post infection (Rvb = 100%) | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID1176096 | Cytotoxicity against HMEC1 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Clofazimine analogs with antileishmanial and antiplasmodial activity. |
| AID1234218 | Cytotoxicity against human MDA-MB-361 cells assessed as reduction in cell number incubated for 72 hrs | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. |
| AID1915902 | Antiplasmodial activity against sorbitol-synchronized early ring stage plasmodium falciparum NF54 trophozoites assessed as inhibition of parasite growth incubated for 72 hrs by SYBR green-based parasite susceptibility assay | |||
| AID594532 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite LDH activity after 72 hrs by spectrophotometry | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Amodiaquine analogues containing NO-donor substructures: synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria. |
| AID1190841 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 by SYBR Green-based method | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Synthesis and biological evaluation of adamantane-based aminophenols as a novel class of antiplasmodial agents. |
| AID1191205 | Antimicrobial activity against Plasmodium falciparum D6 infected in human erythrocytes after 72 hrs by SYBR green I fluorescence-based method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Reemergence of chloroquine (CQ) analogs as multi-targeting antimalarial agents: a review. |
| AID342473 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1 by [3H]hypoxanthine uptake | 2008 | Journal of natural products, Aug, Volume: 71, Issue:8 | Agelasines J, K, and L from the Solomon Islands Marine Sponge Agelas cf. mauritiana. |
| AID1494362 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as swimming path length in virtual platform at 30 mg/kg/day, po for 80 days by Morris water maze test (Rvb = 9.1 +/- 2.8 cm) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
| AID248132 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15 | Application of multi-component reactions to antimalarial drug discovery. Part 1: Parallel synthesis and antiplasmodial activity of new 4-aminoquinoline Ugi adducts. |
| AID558841 | Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID158717 | Inhibitory activity against chloroquine-resistant Plasmodium falciparum W-2 Indochina III | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis and in vitro studies of novel pyrimidinyl peptidomimetics as potential antimalarial therapeutic agents. |
| AID357907 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of natural products, Sep, Volume: 64, Issue:9 | Synthesis of new artemisinin analogues from artemisinic acid modified at C-3 and C-13 and their antimalarial activity. |
| AID237416 | Distribution coeeficient for the compound at pH7.4 (Log D7.4) | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction. |
| AID596504 | Antimalarial activity against Plasmodium falciparum K1 intra-erythrocytic form | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Marinoquinolines A-F, pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes). |
| AID677005 | Antiplasmodial activity against Plasmodium falciparum N infected in C57/BL6 mouse assessed as parasitemia at 10 mg/kg, po dosed 30 mins post parasite infection and same dose repeated on days 1, 2 and 3 post infection measured on on parasitemia day 4 (Rvb | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID1306902 | Antiplasmodial activity against chloroquine/pyrimethamine resistant Plasmodium falciparum K1 infected in human red blood cells after 48 hrs by [3H]hypoxanthine incorporation assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead. |
| AID519584 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
| AID666489 | Selectivity ratio of IC50 for human HepG2 cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
| AID389017 | Antimalarial activity against Plasmodium falciparum | 2008 | Journal of natural products, Dec, Volume: 71, Issue:12 | Antileishmanial constituents of the Panamanian endophytic fungus Edenia sp. |
| AID703714 | Resistance ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1175723 | Antigametocytocidal activity against Plasmodium falciparum NF54-pfs16-GPF late (4 to 6) gametocyte assessed as viability at 120 uM after 72 hrs by MitoTracker Red CM-H2XRos/micro-plate confocal imaging system | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs. |
| AID1444635 | Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores. |
| AID119886 | In vivo antimalarial activity against Plasmodium yoelii in mice (Mus musculus) at 24 mg/kg/day orally on day 4 expressed as percent suppression | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Orally active amino functionalized antimalarial 1,2,4-trioxanes. |
| AID494151 | Antiplasmodial activity against Plasmodium falciparum D6 infected in human erythrocytes by SYBR green I fluorescence assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16 | Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. |
| AID1231846 | Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID1409625 | Selectivity index for SigmaR1/R2 on-target Kd values vs. hERG ion channel | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID572357 | Cytotoxicity against human HCT8 cells assessed as reduction in viable cells by neutral red assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of pyrvinium pamoate against Cryptosporidium parvum infection in vitro and in a neonatal mouse model. |
| AID509197 | Inhibition of TLR7/TLR9-mediated upregulation of PDL1 expression in aldrithiol-2-treated HIV1 Ada-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID753994 | Resistance index, ratio of IC50 for chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 to IC50 for chloroquine-sensitive erythrocytic stage of Plasmodium falciparum NF54 | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and antimalarial testing of neocryptolepine analogues: addition of ester function in SAR study of 2,11-disubstituted indolo[2,3-b]quinolines. |
| AID477947 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum K14 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID768471 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as nonviable parasite at 40 uM after 0.5 hrs by SYTO 61 staining-based flow cytometric analysis relative to untreated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1188444 | Antimalarial activity against tightly synchronized Plasmodium falciparum W2 assessed as parasite stage accumulation index at early ring stages at 10 uM treated at 6 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytolo | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID616030 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Targeting the human malaria parasite Plasmodium falciparum: in vitro identification of a new antiplasmodial hit in 4-phenoxy-2-trichloromethylquinazoline series. |
| AID1533495 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring malformation of tail up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1355326 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as reduction in parasitemia at 20 mg/kg, po administered via gavage for 3 consecutive days post infection measured on day 9 post infection relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
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| AID1421905 | Cytotoxicity against human NFF cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID267107 | Antimalarial activity against Plasmodium falciparum D6 | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Tetraoxane antimalarials and their reaction with Fe(II). |
| AID1241132 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as reduction in parasitemia at 30 mg/kg, po qd administered for 4 days measured on day 4 post last dose by flow cytometric analysis relative to control | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. |
| AID249050 | In vitro inhibition of Plasmodium falciparum K1 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: design, construction, characterization, and pharmacology of metaquine. |
| AID275794 | Antiplasmodial activity against Plasmodium falciparum NF54 | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Synthesis and antimalarial activity of side chain modified 4-aminoquinoline derivatives. |
| AID349011 | Cytotoxicity against human KB cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. |
| AID1204125 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as parasitemia level at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 12 post infection (Rvb = 8.81 +/- 1. | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID28681 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID570295 | Antiplasmodial activity against chloroquine and pyrimethamine-resistant ring stage Plasmodium falciparum V1/S infected in human red blood cells after 48 hrs | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Incorporation of basic side chains into cryptolepine scaffold: structure-antimalarial activity relationships and mechanistic studies. |
| AID595241 | Resistance index, ratio of IC50 for Plasmodium falciparum W2 to IC50 for Plasmodium falciparum D6 | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus. |
| AID294653 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by FACS | 2007 | European journal of medicinal chemistry, Jun, Volume: 42, Issue:6 | Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials. |
| AID419119 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 molecules of heme to 1 equivalent of drug in presence of 12 mM SDS by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID642884 | Binding affinity to chicken riboflavin binding protein assessed as dissociation constant at pH 7.4 in phosphate buffer by isothermal titration calorimetric assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study. |
| AID1057259 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as parasite growth inhibition after 48 hrs by SYBR green-1 dye-based fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers. |
| AID453921 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum 3D7 by giemsa stain | 2009 | Bioorganic & medicinal chemistry, Dec-15, Volume: 17, Issue:24 | Synthesis and structure-activity relationships of cassiarin A as potential antimalarials with vasorelaxant activity. |
| AID565417 | Antimalarial activity against Plasmodium falciparum Pf3D70087/N9 infected in immunodeficient HM-IL2Rgamma null mouse assessed as decreased parasitemia at 50 mg/kg, po for 4 days after 28 days | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rgammanull mice engrafted with human erythrocytes. |
| AID412365 | Antimalarial activity after 48 hrs against chloroquine-sensitive Plasmodium falciparum NF54 infected human A+ erythrocytes by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID340539 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 2-N-Methyl modifications and SAR studies of manzamine A. |
| AID558839 | Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID1064732 | Resistance index, ratio of IC50 for Plasmodium falciparum W2 to IC50 for Plasmodium falciparum 3D7 | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Synthesis, in vitro antimalarial activity and cytotoxicity of novel 4-aminoquinolinyl-chalcone amides. |
| AID337540 | Selectivity index, ratio of ED50 for human KB cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID382471 | Antileishmanial activity against Leishmania donovani infected in mouse peritoneal macrophages after 96 hrs | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and antiprotozoal activities of simplified analogs of naphthylisoquinoline alkaloids. |
| AID1158046 | Antimalarial activity against Plasmodium falciparum NFS4 assessed as inhibition of [3H]hypoxanthine incorporation preincubated for 48 hrs measured 24 hrs post [3H]hypoxanthine addition by liquid scintillation counting | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites. |
| AID468922 | Selectivity index, ratio of antimicrobial activity against Plasmodium falciparum Dd2 over cytotoxicity against human HEK293 cells | 2009 | Journal of natural products, Aug, Volume: 72, Issue:8 | Antimalarial benzylisoquinoline alkaloid from the rainforest tree Doryphora sassafras. |
| AID614145 | Cytotoxicity against human NFF cells at 50 uM after 3 days by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17 | Synthesis and antimalarial evaluation of novel benzopyrano[4,3-b]benzopyran derivatives. |
| AID1593331 | Antimalarial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mouse assessed as inhibition of parasitemia at 10 mg/kg, po administered once daily for 4 days starting from 4 hrs post-infection and measured on day 4 by Peter's | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | 4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides. |
| AID524785 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by 1536-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID232020 | Resistance index as IC50 for Plasmodium falciparum K1 and Thai strains | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. |
| AID775980 | Selectivity index, ratio of IC50 for HEK293T cells to IC50 for ring stage of Plasmodium falciparum W2 infected in human RBC | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents. |
| AID1241125 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as reduction in parasitemia at 10 mg/kg, po qd administered for 4 days measured on day 4 post last dose by flow cytometric analysis relative to control | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. |
| AID581964 | Antimicrobial activity against wild type Plasmodium falciparum HB3 infected in erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I-based fluorescence assay | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Changes in the plasmodial surface anion channel reduce leupeptin uptake and can confer drug resistance in Plasmodium falciparum-infected erythrocytes. |
| AID723089 | Cytotoxicity against african green monkey Vero cells up to 9 uM after 48 hrs by neutral red assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin. |
| AID419126 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 molecules of heme to 1 equivalent of drug in presence of 20 mM SDS by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID111040 | Number of survival out of 5 mice on day 28 at the dose of 96 mg/kg/day orally | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Geraniol-derived 1,2,4-trioxanes with potent in-vivo antimalarial activity. |
| AID480242 | Half life in CD1 mouse at 50 mg/kg, po | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID334011 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum V1/S after 48 hrs by [3H]hypoxanthine uptake | 1997 | Journal of natural products, Oct, Volume: 60, Issue:10 | Antiprotozoal compounds from Asparagus africanus. |
| AID419181 | Toxicity in po dosed mouse assessed as induction of hepatotoxicity at drug dose above no observed adverse effects level | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
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| AID1143189 | Cytotoxicity against HEK293T cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity. |
| AID1431677 | Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication at 10 uM after 24 hrs by RT-PCR method relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives, synthesized by thermal and ultrasonic means, are endowed with anti-Zika virus activity. |
| AID1067548 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria. |
| AID1764410 | Agonist activity at Gal4-fused human Nurr1 LBD expressed in HEK293T cells co-expressing renilla luciferase assessed as renilla luciferase activity up to 300 uM incubated for 12 to 14 hrs by hybrid reporter gene assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Fragment-like Chloroquinolineamines Activate the Orphan Nuclear Receptor Nurr1 and Elucidate Activation Mechanisms. |
| AID1769946 | Antiplasmodial activity against chloroquine-resistant erythrocytic stage Plasmodium falciparum Dd2 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Further investigation of harmicines as novel antiplasmodial agents: Synthesis, structure-activity relationship and insight into the mechanism of action. |
| AID594704 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10 | Antiplasmodial and antitumor activity of dihydroartemisinin analogs derived via the aza-Michael addition reaction. |
| AID515039 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mice (Mus musculus) assessed as parasitaemia level at 30 mg/kg, subcutaneously after 3 days relative to control | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID442269 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMT K2 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID300926 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Metallocene-based antimalarials: an exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. |
| AID558830 | Antimalarial activity against Plasmodium falciparum FCR3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID337533 | Selectivity index, ratio of ED50 for human HT1080 cells to ED50 for chloroquine-resistant Plasmodium falciparum W2 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1274382 | Antimalarial activity against Plasmodium berghei ANKA infected in C57Bl6 mouse at 80 mg/kg/day, po measured on day 3 to 5 by Thompson test | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? |
| AID1188435 | Antimalarial activity against tightly synchronized Plasmodium falciparum HB3 assessed as parasite stage accumulation index at early ring stages at 10 uM treated at 6 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytol | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID1713136 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 48 hrs by SYBR green 1 dye based fluorescence assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Polyvalent effect enhances diglycosidic antiplasmodial activity. |
| AID221571 | Percent of infected erythrocytes in Blood schizonticidal activity against Plasmodium chabaudi in mice at a concentration of 10 mg/kg/day on day 4 | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
| AID361516 | Selectivity index, ratio of IC50 for multidrug-resistant Plasmodium falciparum TM91C235 to IC50 for chloroquine and mefloquine-susceptible Plasmodium falciparum D6 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. |
| AID1275774 | Cytotoxicity against CHO cells by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
| AID678314 | Inhibition of Plasmodium vivax PLM4 using Lys-Glu-Phe-Val-Phe-NPhe-Ala-Leu-Lys as substrate by spectrophotometry | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID1880204 | Cytotoxicity against HEL 299 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
| AID562545 | Antiplasmodial activity against Plasmodium vinckei petteri infected in CD mouse assessed as suppression of parasitemia at 10 mg/kg/day, ip measured on day 5 post-infection by Giemsa staining | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID522089 | AUC (0 to infinity) in Papua new Guinean pregnant women at 600 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID286716 | Effect on survival of Plasmodium berghei NK65 infected ICR mice (Mus musculus) assessed as mean survival days at 10 mg/kg, intraperitoneal after 4 days | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and antimalarial property of orally active phenoxazinium salts. |
| AID434590 | Resistance factor, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. |
| AID734083 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite growth after 24 hrs by [3H]hypoxanthine incorporation assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis, cytotoxicity and antiplasmodial activity of novel ent-kaurane derivatives. |
| AID382475 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1R after 24 hrs by semiautomated micro dilution assay | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2 | Synthesis and antimalarial activity of new analogues of amodiaquine. |
| AID93350 | The compound was tested for survival of the ICR mice (infected with Plasmodium berghei) as a symptom indicative of toxicity on day 4, at a dose of 20 mg/kg/day | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID1426242 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBC assessed as decrease in parasite viability after 72 hrs by LDH assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and evaluation of 4-aminoquinoline-purine hybrids as potential antiplasmodial agents. |
| AID1439479 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Synthesis, antimalarial activity, heme binding and docking studies of N-substituted 4-aminoquinoline-pyrimidine molecular hybrids. |
| AID519266 | Antiparasitic activity against chloroquine-resistant Plasmodium falciparum R1H6/2 by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
| AID158048 | Growth inhibition of chloroquine-sensitive Plasmodium falciparum FcB1 | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID525489 | Antigametocyte activity against Plasmodium falciparum D10 trophozoites assessed as inhibition of parasite growth at 50 nM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID1756670 | Inhibition of spike glycoprotein S in SARS-CoV-2 pseudovirus infected in human 293T/ACE2 cells assessed as inhibition of viral infection pretreated the virus for 30 mins followed by viral infection measured after 48 hrs by by luciferase reporter gene assa | 2021 | Journal of natural products, 02-26, Volume: 84, Issue:2 | Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of |
| AID1865620 | Antiparasitic activity against Plasmodium falciparum 3D7 infected in erythrocytes assessed as parasite growth inhibition incubated for 48 hrs by SYBR Green I dye based fluorescence assay | 2022 | Journal of natural products, 12-23, Volume: 85, Issue:12 | Dactylosporolides: Glycosylated Macrolides from |
| AID1858888 | Antimalarial activity against Plasmodium falciparum Dd2 by SYBR green method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Antimalarial application of quinones: A recent update. |
| AID1518828 | Antimalarial activity against ring stage Plasmodium falciparum K1 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
| AID1125284 | Antimicrobial activity against Plasmodium berghei sporozoites infected in 12 hrs compound pretreated human HepG2 cells assessed as reduction in viability of exoerythrocytic forms measured after 48 hrs of incubation by luciferase bioluminescence assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP). |
| AID620095 | Antimalarial activity against antifolate-resistant Plasmodium falciparum W2 infected in human erythrocytes after 96 hrs by SYBR Green I-based fluorescence assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities. |
| AID300106 | Selectivity index, ratio of CC50 for human KB cells to IC50 for Plasmodium falciparum 3D7 | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Anti-malarial activity of N6-modified purine analogues. |
| AID1717750 | Selectivity index, ratio of CC50 for African green monkey Vero E6 cells to EC50 for 2019-nCoV Beta CoV/Wuhan/WIV04/2019 infected in African green monkey Vero E6 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID563687 | Antimalarial activity against Plasmodium falciparum assessed as parasite growth inhibition after 48 hrs by [3H]hypoxanthin incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Plasmodium falciparum drug resistance in Madagascar: facing the spread of unusual pfdhfr and pfmdr-1 haplotypes and the decrease of dihydroartemisinin susceptibility. |
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
| AID601638 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human A positive erythrocytes by [3H]hypoxanthine uptake assay in presence of serum in medium | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice. |
| AID1060786 | Antiplasmodial activity against chloroquine-resistant ring stage Plasmodium falciparum W2 assessed as parasitemia after 48 hrs by flow cytometry | 2014 | European journal of medicinal chemistry, Jan, Volume: 71 | Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation. |
| AID1391089 | Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | New phenylaniline derivatives as modulators of amyloid protein precursor metabolism. |
| AID151830 | In vivo effective dose for antimalarial activity by peroral dose | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20 | Metabolites of febrifugine and its synthetic analogue by mouse liver S9 and their antimalarial activity against Plasmodium malaria parasite. |
| AID1530035 | Antiprotozoal activity against chloroquine-resistant Plasmodium falciparum W2 | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Quinoline and quinolone dimers and their biological activities: An overview. |
| AID29359 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID522094 | Cmax in Papua new Guinean pregnant women assessed as monodesethychloroquine at 750 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1255395 | Antimalarial activity against the erythrocytic stages of chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]-hypoxanthine incorporation after 48 hr by liquid scintillation method | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery and optimisation studies of antimalarial phenotypic hits. |
| AID158047 | Growth inhibition of chloroquine-sensitive Plasmodium falciparum F32 | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID607823 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7A assessed as death of all detectable parasites at two days dosage of 0.5 to 500 uM using Hema 3 staining by microscopic analysis | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models. |
| AID401570 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 by LDH assay | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | A new antimalarial quassinoid from Simaba orinocensis. |
| AID453367 | Inhibition of beta-hematin formation after 18 hrs | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID1544799 | Antimicrobial activity against Pseudomonas aeruginosa assessed as zone of inhibition at 10 uM/disk after 24 hrs by disk diffusion method | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13 | Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones. |
| AID279313 | Inhibition of Plasmodium falciparum in HRP2 ELISA | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | In vitro antimalarial activity of azithromycin, artesunate, and quinine in combination and correlation with clinical outcome. |
| AID1378994 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells assessed as reduction in parasitic LDH activity by Malstat reagent based spectrophotometric method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID678311 | Inhibition of Plasmodium falciparum PLM4 using Lys-Glu-Phe-Val-Phe-NPhe-Ala-Leu-Lys as substrate by spectrophotometry | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID1717753 | Selectivity index, ratio of CC50 for golden hamster BHK-21 cells to EC50 for wild type HCoV-OC43 infected in BHK-21 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID444927 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mice (Mus musculus) assessed as reduction of parasitaemia level at 3 mg/kg, perorally daily once for 3 consecutive days measured after 4 days post-infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | The structure-activity relationship of the antimalarial ozonide arterolane (OZ277). |
| AID1353871 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum NF54 | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. |
| AID1638553 | Antimalarial activity against Plasmodium berghei infected in mouse inoculated with Plasmodium berghei infected RBCs dosed orally starting at 2 hrs after inoculation of infected RBCs followed by same dose administration for 3 more days after each 24 hrs pe | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | 3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity. |
| AID543842 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected ICR mouse assessed as survival of mouse at 5 mg/kg/day, po for 4 days measured after 25 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID1179399 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by SYBR Green-1 staining-based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Antiplasmodial activity of new 4-aminoquinoline derivatives against chloroquine resistant strain. |
| AID509189 | Inhibition of TLR7/TLR9-mediated activation of aldrithiol-2-treated HIV1 Ada-stimulated human PBMC assessed as CD38-MFI level in activated CD8-positive cells at 5 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID247059 | Effective dose against chloroquine-resistant, pyrimethamine-resistant, mefloquine-sensitive Plasmodium falciparum W2 | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID400316 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs as LDH activity by Makler assay | 1996 | Journal of natural products, Jan, Volume: 59, Issue:1 | A new quassinoid from Castela texana. |
| AID1687056 | Inhibition of autophagy in human PANC-1 cells cultured in nutrient-deprived medium assessed as accumulation of LC3-2 expression at 25 uM after 6 hrs by Western blot analysis relative to control | |||
| AID27572 | Partition coefficient (logD7.0) | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
| AID309397 | Selectivity index, Ratio of IC50 for human HeLa cells to IC50 for Plasmodium falciparum D10 | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential antimalarial and anticancer agents. |
| AID691736 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ANKA infected in ip dosed Swiss albino mouse assessed as suppression of parasitemia measured on day 4 post infection by Giemsa staining | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp. |
| AID318196 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID658605 | Resistant factor, ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies. |
| AID1617099 | Antiprotozoal activity against chloroquine-sensitive Plasmodium falciparum NF54 | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Ealamines A-H, a Series of Naphthylisoquinolines with the Rare 7,8'-Coupling Site, from the Congolese Liana |
| AID441887 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by fluorescence based method | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum. |
| AID1375185 | Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9 | Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ |
| AID361169 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2001 | Journal of natural products, Jun, Volume: 64, Issue:6 | Antimalarial compounds from Rhaphidophora decursiva. |
| AID568771 | Selectivity index, ratio of IC50 for human HEK293 cells to IC50 for chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2 | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen". |
| AID549612 | Antimalarial activity against mefloquine-resistant, chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine uptake in presence of 1 mM folinic acid | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones. |
| AID522252 | Apparent oral clearance in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic base model at 450 mg/day, po administered as three divided doses in presence of sulfadoxine-pyrimethamine by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1191136 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters. |
| AID688316 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum isolate Kenya after 72 hrs by lactate dehydrogenase assay | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and comparison of antiplasmodial activity of (+), (-) and racemic 7-chloro-4-(N-lupinyl)aminoquinoline. |
| AID606571 | Antimalarial activity against chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships. |
| AID105687 | Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 32 uM concentration; No toxicity | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID1155803 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as growth inhibition | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Microwave-assisted synthesis of C-8 aryl and heteroaryl inosines and determination of their inhibitory activities against Plasmodium falciparum purine nucleoside phosphorylase. |
| AID523427 | Antiplasmodial activity against artemisinin-tolerant Plasmodium falciparum F32-Tanzania assessed as time required to reach 5% parasitaemia at 0.2 uM treated for 48 hrs | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 | Increased tolerance to artemisinin in Plasmodium falciparum is mediated by a quiescence mechanism. |
| AID454899 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 by LDH release assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline-triazine conjugates. |
| AID765177 | Antiplasmodial activity chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A+ erythrocytes assessed as reduction of [3H]hypoxanthine incorporation after 24 hrs by scintillation counting | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. |
| AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1542987 | Antimalarial activity against CQ-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as inhibition of parasite growth incubated for for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Covalent Inhibitors of |
| AID1728298 | Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities. |
| AID666484 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in type A rhesus-positive human erythrocytes assessed as [3H]hypoxanthine incorporation after 48 hrs by scintillation counting | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
| AID404796 | Drug accumulation in digestive vacuole of chloroquine-sensitive Plasmodium falciparum assessed as vacuolar accumulation ratio at pH 5.6 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID1408339 | Antiviral activity against Influenza A virus A/PR/8/34(H1N1) GFP-fused pseudotyped lentiviral particle expressing H1-HA/N1-NA infected in MDCK cells assessed as inhibition of pseudoparticle entry after 3 days by flow cytometry | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents. |
| AID477945 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID1647632 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 incubated for 72 hrs by DAPI-staining based imaging analysis | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Orthoscuticellines A-E, β-Carboline Alkaloids from the Bryozoan |
| AID558843 | Antimalarial activity against Plasmodium falciparum IMT K14 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID688319 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human RBC assessed as inhibition of parasite growth after 72 hrs by lactate dehydrogenase assay | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and comparison of antiplasmodial activity of (+), (-) and racemic 7-chloro-4-(N-lupinyl)aminoquinoline. |
| AID580318 | Antimalarial activity against chloroquine-susceptible Plasmodium berghei ANKA infected in Balb-C mouse assessed as inhibition parasitemia at 20 mg/kg, ip qd for 4 days administered fourth day post infection | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents. |
| AID678315 | Inhibition of human cathepsin D | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID1383228 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as mean survival days at 5 mg/kg, po treated up to day 3 measured over 30 days (Rvb = 7.2 days) | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study. |
| AID152137 | Inhibitory activity against chloroquine-resistant Plasmodium falciparum K1 | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID352677 | Antiplasmodial activity as reduced parasitaemia against chloroquine-resistant Plasmodium yoelii N67 infected Swiss mice (Mus musculus) at 10 mg/kg/day peroral dose over 10 days | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9 | Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials. |
| AID303430 | Toxicity in Plasmodium chabaudi chabaudi infected C57BL/6J mice (Mus musculus) at 0.1 mg, intraperitoneally twice daily after 4 days | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Identification of phosphinate dipeptide analog inhibitors directed against the Plasmodium falciparum M17 leucine aminopeptidase as lead antimalarial compounds. |
| AID332191 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2002 | Journal of natural products, Jan, Volume: 65, Issue:1 | Indole and beta-carboline alkaloids from Geissospermum sericeum. |
| AID1541972 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for D-sorbitol synchronized ring stage of chloroquine-resistant Plasmodium falciparum W2 | 2020 | ACS medicinal chemistry letters, Feb-13, Volume: 11, Issue:2 | Functionalized Naphthalimide-4-aminoquinoline Conjugates as Promising Antiplasmodials, with Mechanistic Insights. |
| AID157849 | Growth inhibition of chloroquine-resistant Plasmodium falciparum KI | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Synthesis, antimalarial activity and inhibition of haem detoxification of novel bisquinolines. |
| AID1772390 | Inhibition of beta-hematin formation in Plasmodium falciparum assessed as decrease in beta-hematin | |||
| AID480223 | Half life in human liver microsome at 1 uM by LC-MS/MS analysis in presence of NADPH | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID625399 | Cytotoxicity against african green monkey BGMK cells after 24 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3. |
| AID1421902 | Antiplasmodial activity against drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1255407 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase in mouse survival at 10 mg/kg, ip qd administered as single dose on day 0 to 4 of exposure measured on day 5 post exposure by FACS method (Rvb | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery and optimisation studies of antimalarial phenotypic hits. |
| AID1700299 | Cytotoxicity against monkey BGM cells assessed as reduction in cell viability incubated for 24 hrs by neutral red dye based assay | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission. |
| AID477963 | Binding affinity to pUC18 DNA containing 50% AT assessed as middle of the peak at half height melting temperature at 1 uM by spectrophotometry analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID348955 | Antimalarial activity against asexual blood stage of Plasmodium falciparum 3D7 after 48 hrs by candle jar method | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7 | Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro. |
| AID362662 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum F32-Tanzania | 2008 | Journal of natural products, Sep, Volume: 71, Issue:9 | Benzoic acid derivatives from Piper species and their antiparasitic activity. |
| AID323683 | Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum K1 infected erythrocytes after 90 min | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID540237 | Phospholipidosis-positive literature compound observed in rat | |||
| AID1445942 | Antispasmodial activity against chloroquine-sensitive asexual blood stages of Plasmodium falciparum 3D7 after 72 hrs by HRP2-based ELISA | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally. |
| AID1229873 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 4 post infection by Giemsa sta | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID677004 | Antiplasmodial activity against Plasmodium falciparum N infected in C57/BL6 mouse assessed as parasitemia at 10 mg/kg, po dosed 30 mins post parasite infection and same dose repeated on days 1, 2 and 3 post infection measured on on parasitemia day 2 (Rvb | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID452988 | Antimalarial activity against Plasmodium berghei infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 3 mg/kg, perorally administered for 3 days post infection | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2 | The comparative antimalarial properties of weak base and neutral synthetic ozonides. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID423719 | Absorption half life in Papua New Guinean children with uncomplicated malaria at 10 mg/kg daily for 3 days | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. |
| AID701109 | Mutagenicity against Salmonella typhimurium TA100 assessed as revertants at 10 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1649435 | Half life in mouse liver microsomes at 1 uM in presence of NADP by LC-MS | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
| AID300099 | Antiplasmodial activity against chloroquine, pyrimethamine-resistant Plasmodium falciparum K1 after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals. |
| AID1633712 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as mean survival time at 33.3 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 28 post infection (Rvb = 13.2 days) | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID1714084 | Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs b | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle. |
| AID264020 | Selectivity ratio of EC50s against Plasmodium falciparum FCR3 to mice (Mus musculus) FM3A cells | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Antimalarial effect of bis-pyridinium salts, N,N'-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide). |
| AID401067 | Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay | 1998 | Journal of natural products, Jun-26, Volume: 61, Issue:6 | Novel quinone methides from Salacia kraussii with in vitro antimalarial activity. |
| AID1128651 | Antimalarial activity against drug-sensitive Plasmodium falciparum NF54 | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1. |
| AID1156431 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for chloroquine-, pyrimethamine- and proguanil-resistant Plasmodium falciparum K1 infected in human erythrocytes | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and in vitro evaluation of 4-trichloromethylpyrrolo[1,2-a]quinoxalines as new antiplasmodial agents. |
| AID1160928 | Antimalarial activity against multi-drug-resistant Plasmodium falciparum TM90-C2B infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
| AID1533500 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring yolk edema up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1229875 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 6 post infection by Giemsa sta | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID1313992 | Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 infected in human erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenzimidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense. |
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| AID442265 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMTL1 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID511253 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D6 by ELISA | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda. |
| AID274743 | Antiplasmodial activity against Plasmodium falciparum K1 | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Limonoid orthoacetates and antiprotozoal compounds from the roots of Pseudocedrela kotschyi. |
| AID1433153 | Cytotoxicity against MDCK cells assessed as inhibition of cell viability by colorimetric formazan-based MTS assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID1639467 | Antiplasmodial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation c | |||
| AID1408799 | Antiplasmodial activity against the multidrug-resistant Plasmodium falciparum FRC-3 infected in human red blood cells assessed as reduction in parasite growth after 48 hrs by Hoechst 33342 staining based flow cytometric analysis | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Novel antimalarial chloroquine- and primaquine-quinoxaline 1,4-di-N-oxide hybrids: Design, synthesis, Plasmodium life cycle stage profile, and preliminary toxicity studies. |
| AID1720812 | Bactericidal activity against Chromobacterium violaceum ATCC 31532 at 400 uM by resazurin dye based assay relative to control | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16 | Chloroquine fumardiamides as novel quorum sensing inhibitors. |
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| AID1810598 | Antiplasmodial activity against asexual blood stage of multidrug-resistant Plasmodium falciparum 7G8 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | |||
| AID130239 | Compound was tested for antimalarial activity against mice (Mus musculus) malaria parasite Plasmodium berghei in vivo and the samples were administarted intraperitoneally. | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | New type of febrifugine analogues, bearing a quinolizidine moiety, show potent antimalarial activity against Plasmodium malaria parasite. |
| AID703895 | Mutagenicity against Salmonella typhimurium TA98 assessed as revertants at 40 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID730538 | Antimalarial activity against schizont stage of chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by SYBR Green I-based fluorescence assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Synthesis and insight into the structure-activity relationships of chalcones as antimalarial agents. |
| AID290019 | Antiplasmodial activity against Plasmodium falciparum FcB1 | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Synthesis and antimalarial evaluation of a series of piperazinyl flavones. |
| AID525279 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
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| AID1880206 | Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
| AID1193545 | Selectivity index, ratio of CC50 for rat L6 cells to IC50 for chloroquine and pyrimethamine resistant Plasmodium falciparum K1 | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities. |
| AID318614 | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Chemical stability of the peroxide bond enables diversified synthesis of potent tetraoxane antimalarials. |
| AID543641 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected in ICR mouse assessed as chemosuppression of parasitemia at 5 mg/kg/day, po administered 24 hrs post-treatment measured after 4 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID1830991 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 | 2021 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 54 | THC shows activity against cultured Plasmodium falciparum. |
| AID1327392 | Cytotoxicity against human WI38 cells assessed as reduction in cell viability measured after 48 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin. |
| AID427685 | Selectivity index, ratio IC50 for human HepG2 cells to IC50 for chloroquine, pyrimethamine and proguanil-resistant Plasmodium falciparum W2 | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines. |
| AID522076 | Clearance in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic final covariate model assessed as monodesethychloroquine at 450 mg/day, po administered as three divided doses in presence of sulfadoxine-pyrimethamine by | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1128650 | Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1. |
| AID1676924 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines. |
| AID377367 | Antiplasmodial activity against Plasmodium falciparum W2 | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | Bisnortriterpenes from Salacia madagascariensis. |
| AID663062 | Antimalarial activity against Plasmodium berghei KBG173 infected in mouse assessed as decrease in parasitemia at 5 mg/kg, ip BID administered on day 3, 4 and 5 post infection measured on day 31 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin. |
| AID1408798 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells assessed as reduction in parasite growth after 48 hrs by Hoechst 33342 staining based flow cytometric analysis | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Novel antimalarial chloroquine- and primaquine-quinoxaline 1,4-di-N-oxide hybrids: Design, synthesis, Plasmodium life cycle stage profile, and preliminary toxicity studies. |
| AID608680 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives. |
| AID1243885 | Antiplasmodial activity against blood stage of chloroquine-sensitive Plasmodium falciparum NF54 by parasite lactate dehydrogenase assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity. |
| AID1377006 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Sep-08, Volume: 137 | Design, synthesis and characterization of novel quinacrine analogs that preferentially kill cancer over non-cancer cells through the down-regulation of Bcl-2 and up-regulation of Bax and Bad. |
| AID1201063 | Antiplasmodial activity against chloroquine/mefloquine-resistant Plasmodium falciparum SKF58 | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Synthesis of isocryptolepine analogues and their structure-activity relationship studies as antiplasmodial and antiproliferative agents. |
| AID1487409 | Antiplasmodial activity against chloroquine-sensitive IEF stage of Plasmodium falciparum NF54 infected in human RBC assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16 | Structure-activity relationship studies on thiaplidiaquinones A and B as novel inhibitors of Plasmodium falciparum and farnesyltransferase. |
| AID675165 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by SYBR Green-I based fluorescence assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum. |
| AID397827 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 24 hrs as reduced [3H]phenylalanine uptake | 2002 | Journal of natural products, Dec, Volume: 65, Issue:12 | Leishmanicidal and antiplasmodial activity of constituents of Smirnowia iranica. |
| AID565415 | Antimalarial activity against Plasmodium falciparum Pf3D70087/N9 infected in immunodeficient HM-beta2 m null mouse after 7 days | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rgammanull mice engrafted with human erythrocytes. |
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| AID774660 | Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum at 100 uM after 72 hrs by image-based HTS assay relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Approaches to protozoan drug discovery: phenotypic screening. |
| AID701108 | Mutagenicity against Salmonella typhimurium TA100 assessed as revertants at 5 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1193233 | Antimalarial activity against ring stage Plasmodium falciparum W2 infected with human red blood cells incubated for 48 hrs by flow cytometry | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity. |
| AID504268 | Cytotoxicity against HDF after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID586923 | Resistant index, ratio of EC50 for tafenoquine-resistant promastigotes of Leishmania major R4 to EC50 for promastigotes of Leishmania major MHOM/JL/80/Friedlin | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Increased glycolytic ATP synthesis is associated with tafenoquine resistance in Leishmania major. |
| AID1533492 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring malformation of eyes up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1541618 | Antiplasmodial activity against Plasmodium falciparum NF54 measured after 24 hrs in presence of [3H] hypoxanthine by liquid scintillation counter analysis | 2019 | Journal of natural products, 12-27, Volume: 82, Issue:12 | Structure, Biosynthesis, and Bioactivity of Photoditritide from |
| AID401645 | Inhibition of beta-hematin formation by BHIA assay | 2005 | Journal of natural products, May, Volume: 68, Issue:5 | Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound. |
| AID337538 | Selectivity index, ratio of ED50 for human COL1 cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1335178 | Antimalarial activity against chloroquine-resistant asexual erythrocyte stage of Plasmodium falciparum K1 infected in human type O+ erythrocytes assessed as growth inhibition incubated for 48 hrs by NBT dye based LDH release assay | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active against |
| AID1059571 | Inhibition of human ERG expressed in CHO cells | 2013 | ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11 | Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties. |
| AID688332 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and antiplasmodial activity of new heteroaryl derivatives of 7-chloro-4-aminoquinoline. |
| AID1439478 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Synthesis, antimalarial activity, heme binding and docking studies of N-substituted 4-aminoquinoline-pyrimidine molecular hybrids. |
| AID1153184 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Tetraoxane-pyrimidine nitrile hybrids as dual stage antimalarials. |
| AID1304520 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1/Columbia infected in erythrocytes assessed as inhibition of parasite growth after 48 hrs by 3H-hypoxanthine incorporation assay | 2016 | Journal of natural products, Mar-25, Volume: 79, Issue:3 | Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum. |
| AID356915 | Antimalarial activity against Plasmodium falciparum D6 | 2002 | Journal of natural products, Dec, Volume: 65, Issue:12 | Araguspongines K and L, new bioactive bis-1-oxaquinolizidine N-oxide alkaloids from Red Sea specimens of Xestospongia exigua. |
| AID1593255 | Antimalarial activity against atovaquone-resistant Plasmodium falciparum Tm90-C2B infected in human erythrocytes by SYBR green 1-based fluorescence assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials. |
| AID522096 | AUC (0 to infinity) in Papua new Guinean pregnant women assessed as monodesethychloroquine at 450 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1444621 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by Malstat reagent based LDH assay | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | N-Piperonyl substitution on aminoquinoline-pyrimidine hybrids: Effect on the antiplasmodial potency. |
| AID327133 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum GCO3 after 72 hrs by SYBR green 1 assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines. |
| AID272982 | Antimalarial activity against Plasmodium falciparum 3D7 | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20 | Evaluation of azasterols as anti-parasitics. |
| AID732340 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID659136 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected Swiss mouse assessed as mean survival time at 20 mg/kg/day, po qd for 4 days | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Antiplasmodial activity of novel keto-enamine chalcone-chloroquine based hybrid pharmacophores. |
| AID1443524 | Antiplasmodial activity against chloroquine/cycloguanil-resistant Plasmodium falciparum FCR3 by [3H]-hypoxanthine incorporation assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | New hydrazine and hydrazide quinoxaline 1,4-di-N-oxide derivatives: In silico ADMET, antiplasmodial and antileishmanial activity. |
| AID564300 | Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID159726 | Parasitaemia (%) in tail blood smears of Plasmodium berghei infected ICR mice (Mus musculus) at 5 mg/kg/day after 4 days | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID294989 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Bre1 by hypoxanthine uptake | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9 | In vitro efficiency of new acridyl derivatives against Plasmodium falciparum. |
| AID1145681 | Antibacterial activity against sensitive Streptococcus faecium ATCC 8043 assessed as reduction in growth in presence of 0.002 ug/ml folic acid | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID1772393 | Inhibition of Escherichia coli DNA gyrase at 50 uM by fluorescence based assay relative to control | |||
| AID1153185 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by FACS analysis | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Tetraoxane-pyrimidine nitrile hybrids as dual stage antimalarials. |
| AID1501232 | Antiprotozoal activity against erythrocytic form of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | Journal of natural products, 09-22, Volume: 80, Issue:9 | Antiprotozoal Linear Furanosesterterpenoids from the Marine Sponge Ircinia oros. |
| AID1426425 | Antiparasitic activity against drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
| AID264019 | Cytotoxicity against mouse FM3A cell line | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Antimalarial effect of bis-pyridinium salts, N,N'-hexamethylenebis(4-carbamoyl-1-alkylpyridinium bromide). |
| AID323374 | Growth inhibition of Plasmodium vivax isolate 1 assessed as parasite LDH synthesis after 48 hrs by double-site Plasmodium LDH antigen capture enzyme-linked immunosorbent assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Improved assessment of plasmodium vivax response to antimalarial drugs by a colorimetric double-site plasmodium lactate dehydrogenase antigen capture enzyme-linked immunosorbent assay. |
| AID116771 | Mean survival time against Plasmodium yoelii in mice (Mus musculus) which died during 28-day observation period at 24 mg/kg/day orally | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Orally active amino functionalized antimalarial 1,2,4-trioxanes. |
| AID1808464 | Modulation of full length human NOR1 expressed in HEK293 cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1533493 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring malformation of sacculi/otoliths up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID675865 | Antimalarial activity against Plasmodium vinckei petteri 279BY infected in ip dosed Swiss mouse assessed as reduction in parasitemia administered QD for 4 days measured on day 5 | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Disulfide prodrugs of albitiazolium (T3/SAR97276): synthesis and biological activities. |
| AID1221982 | Fraction absorbed in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID423724 | Apparent clearance with respect to bioavailability in Paua New Guinean children with uncomplicated malaria at 10 mg/kg daily for 3 days | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. |
| AID1188437 | Antimalarial activity against tightly synchronized Plasmodium falciparum HB3 assessed as parasite stage accumulation index at trophozoites stages at 10 uM treated at 6 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cyt | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID1402365 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells incubated for 72 hrs by parasite LDH release based colorimetric assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Bioactive products from singlet oxygen photooxygenation of cannabinoids. |
| AID247109 | Effective dose required to reduce the parasitemia in mice when compound administered with Tween-80 after 3 day postinfection | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. |
| AID453266 | Antimalarial activity against Plasmodium berghei ANKA infected in Swiss mice (Mus musculus) assessed as mice (Mus musculus) survival at 10 mg/kg, intraperitoneally dosed for 5 consecutive days measured 7 days post infection | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues. |
| AID232018 | Resistance index as ratio of IC50 for Plasmodium falciparum FcB1 and Thai strains | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. |
| AID401573 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | A new antimalarial quassinoid from Simaba orinocensis. |
| AID337536 | Selectivity index, ratio of ED50 for human MEL2 cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID468918 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining method | 2009 | Journal of natural products, Aug, Volume: 72, Issue:8 | Antimalarial benzylisoquinoline alkaloid from the rainforest tree Doryphora sassafras. |
| AID374060 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) erythrocytes at 10 uM after 18 hrs as reduced hemoglobin hydrolysis | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and antimalarial activity of pyrazolo and pyrimido benzothiazine dioxide derivatives. |
| AID1530037 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Quinoline and quinolone dimers and their biological activities: An overview. |
| AID519201 | Antimicrobial activity against fast-growing synchronous Plasmodium falciparum by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID1237960 | Inhibition of beta-haematin formation by microplate reader analysis relative to hemin | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity. |
| AID1649434 | Half life in human liver microsomes at 1 uM in presence of NADP by LC-MS | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
| AID1631452 | Antiviral activity against Dengue virus 2 infected in BHK21 cells assessed after 3 to 5 days by crystal violet staining based plaque assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | The Medicinal Chemistry of Dengue Virus. |
| AID1405717 | Inhibition of mitotic progression in human HeLa cells assessed as upregulation of phosphorylated histone H3 (Ser10) level up to 100 uM after 6 hrs by immunoblot analysis | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
| AID1355327 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as reduction in parasitemia at 20 mg/kg, ip administered for 3 consecutive days post infection measured on day 9 post infection relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
| AID554568 | Inhibition of beta-hematin formation after 14 hrs by spectrophotometry | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID470783 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24 | Synthesis of 9-anilinoacridine triazines as new class of hybrid antimalarial agents. |
| AID1228554 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides. |
| AID1221960 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID452345 | Stimulation of reactive oxygen species in human HeLa cells at 10 uM in presence of 10 uM CuCl2 after 1 hr by dihydroethidium dye based fluorescence assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID373519 | Antiparasitic activity against Plasmodium falciparum K1 | 2009 | European journal of medicinal chemistry, May, Volume: 44, Issue:5 | Synthesis and antiparasitic and antifungal evaluation of 2'-arylsubstituted-1H,1'H-[2,5']bisbenzimidazolyl-5-carboxamidines. |
| AID509179 | Inhibition of TLR7-mediated upregulation of IRAK4 expression in aldrithiol-2-treated HIV1 Ada-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID378978 | Antimalarial activity after 24 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | Lupeol long-chain fatty acid esters with antimalarial activity from Holarrhena floribunda. |
| AID419122 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 equivalent of drug to 1 molecule of heme in presence of 1.5 mM CTAB by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID252578 | In vivo antimalarial activity of compound against Plasmodium berghei in mice (Mus musculus) expressed as mean survival time at 20 mg/kg | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1 | Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials. |
| AID600556 | Antioxidant activity assessed as DPPH radical scavenging activity at 80 uM after 30 mins | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Antiprotozoal activity of chloroquinoline based chalcones. |
| AID399303 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Smith by semiautomated micro dilution assay | |||
| AID327131 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by SYBR green 1 assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines. |
| AID728699 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as survival at 30 mg/kg, po | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. |
| AID729926 | Antimalarial activity against Plasmodium falciparum 3D7 assessed as parasite growth inhibition after 72 hrs by MSF assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents. |
| AID1234221 | Cytotoxicity against human HepG2 cells assessed as reduction in cell number incubated for 72 hrs | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. |
| AID1500569 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay | |||
| AID509190 | Inhibition of TLR7/TLR9-mediated activation of exogenous rIFNalpha2A-stimulated human CD8-positive T cells assessed as CD3/CD8 expressing cells at 5 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID515054 | Drug level in chloroquine-sensitive Plasmodium falciparum Dd2 digestive vacuole assessed as ratio of drug level in vacuole to medium at 5 uM after 1 hr | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID270223 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | A chloroquine-like molecule designed to reverse resistance in Plasmodium falciparum. |
| AID439585 | Antimalarial activity against chloroquine-susceptible Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 48 hrs by [3H]hypoxanthine reuptake assay | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity. |
| AID1183264 | Antimalarial activity against chloroquine ane quinine-sensitive ring stage of Plasmodium falciparum assessed as inhibition of parasite growth after 48 hrs | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening. |
| AID303248 | Selectivity index, ratio for IC50 of rat L6 cells to IC50 of chloroquine-resistant Plasmodium falciparum K1 | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations. |
| AID300927 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Metallocene-based antimalarials: an exploration into the influence of the ferrocenyl moiety on in vitro antimalarial activity in chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. |
| AID442258 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 96 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID480234 | Inhibition of CYP2D6 in human liver microsomes assessed as metabolite produced at 10 uM by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1533164 | Inhibition of recombinant Plasmodium falciparum NDH2 expressed in Escherichia coli using NADH as substrate | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Potent Antimalarial 2-Pyrazolyl Quinolone |
| AID444929 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mice (Mus musculus) assessed as curing of parasitaemia at 3 mg/kg, perorally daily once for 3 consecutive days measured after 30 days post-infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | The structure-activity relationship of the antimalarial ozonide arterolane (OZ277). |
| AID607063 | Antimalarial activity against Plasmodium falciparum FCR3 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Antimalarial pyrido[1,2-a]benzimidazoles. |
| AID491769 | Antiplasmodial activity against Plasmodium falciparum F32-Tanzania after 24 hrs | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13 | Synthesis and antiplasmodial activity of lycorine derivatives. |
| AID382480 | Antimalarial activity in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus) as reduced parasitaemia at 10 mg/kg initial oral dose and further intraperitoneal dose after 4 days | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2 | Synthesis and antimalarial activity of new analogues of amodiaquine. |
| AID70548 | In vitro hemolytic concentration on uninfected erythrocytes; ND is no data | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
| AID1204112 | Cytotoxic activity against human HeLa cells assessed as cell viability at 1000 ug/ml incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1437499 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method | |||
| AID1145678 | Antibacterial activity against chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 assessed as reduction in growth | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID1717754 | Antiviral activity against SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells incubated for 3 days | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID321729 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for Plasmodium falciparum W2 | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines. |
| AID406385 | Selectivity index ratio of IC50 for human MCF7 cells to IC50 for chloroquine-sensitive Plasmodium falciparum F32 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID112564 | In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after subcutaneous administration | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides. |
| AID268406 | Antimalarial activity against Plasmodium falciparum Dd2 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Probing the role of the covalent linkage of ferrocene into a chloroquine template. |
| AID29338 | Dissociation constant (pKa) | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
| AID754528 | Inhibition of hemozoin formation in 0.1 M acetate buffer at pH 4.8 after 12 hrs by tube-based high-throughput assay in presence of Plasmodium yoelii homogenate | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID1238801 | Selectivity index, ratio of MLC50 for African green monkey BGM cells to IC50 for chloroquine and sulfadoxine-resistant and mefloquine-sensitive Plasmodium falciparum W2 | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Anti-Plasmodium falciparum activity of quinoline-sulfonamide hybrids. |
| AID361168 | Selectivity index, ratio of ED50 for human KB cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2001 | Journal of natural products, Jun, Volume: 64, Issue:6 | Antimalarial compounds from Rhaphidophora decursiva. |
| AID768213 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID456797 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in African green monkey (Cercopithecus aethiops) Vero cells assessed as parasite LDH activity after 72 hrs by Malstat reagent method | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group. |
| AID1057938 | Antiproliferative activity against human MCF7 cells after 2 days by sulforhodamine B assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues. |
| AID1808465 | Modulation of full length human NOR1 expressed in HEK293 cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID549910 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 by LDH assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis, antiprotozoal, antimicrobial, β-hematin inhibition, cytotoxicity and methemoglobin (MetHb) formation activities of bis(8-aminoquinolines). |
| AID576571 | Antimalarial activity against Plasmodium falciparum at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax. |
| AID1614009 | Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents. |
| AID1529413 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | Antiplasmodial imidazopyridazines: structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles. |
| AID1457821 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 30 mg/kg/day administered for 4 days via oral gavage starting at 1 hr post infection measured after 30 days relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane. |
| AID378980 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FCR3 Gambia as 24 hrs [3H]hypoxanthine uptake | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | Lupeol long-chain fatty acid esters with antimalarial activity from Holarrhena floribunda. |
| AID519190 | Antimicrobial activity against Plasmodium vivax trophozoites by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID1533540 | Inhibition of cathepsin B activity in human HeLa cells at 10 uM after 12 hrs by magic red substrate based fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1442734 | Drug uptake in lymphoblasts (unknown origin) at 100 nM in presence of vacuolar type ATPase inhibitor concanamycin A measured after 2.5 hrs | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA). |
| AID519270 | Antiparasitic activity against chloroquine-resistant Plasmodium falciparum R1H6/2 pretreated with 0.1 uM phenobarbitone for 48 hrs and in presence of 5 uM verapamil by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
| AID105679 | Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 12.5 uM concentration; No toxicity | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID1431589 | Antimalarial activity against Plasmodium falciparum NF54 harboring pfs16-LUC-GFP late stage 4 to 5 gametocytes after 48 hrs by MitoTracker Red staining based confocal microscopy | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity. |
| AID459097 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human O+ RBC by parasite LDH assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo. |
| AID1199046 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Chikungunya virus 899 infected in African green monkey Vero cells | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID1586761 | Antiplasmodial activity against IEF stage of Plasmodium falciparum NF54 assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting method | 2018 | Journal of natural products, 12-28, Volume: 81, Issue:12 | Antiprotozoal Isoprenoids from Salvia hydrangea. |
| AID251727 | Inhibition of hemoglobin hydrolysis in mice (Mus musculus) infected with Plasmodium berghei at 100 uM | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives. |
| AID1287598 | Antiparasitic activity against chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 infected in human RPMI1640 cells after 72 hrs by NBT staining based spectroscopic analysis | 2016 | European journal of medicinal chemistry, May-04, Volume: 113 | In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51. |
| AID1808454 | Modulation of full length human Nurr1 expressed in SK-N-BE(2) cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by luciferase reporter g | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID449703 | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26 | In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. |
| AID105830 | Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 1.6 uM concentration | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID1771330 | Antimalarial activity against Plasmodium falciparum K1 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting meth | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials. |
| AID1858895 | Antimalarial activity against drug sensitive Plasmodium falciparum NF54 | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Antimalarial application of quinones: A recent update. |
| AID668911 | Antiplasmodial activity against chloroquine, pyrimethamine, and proguanil-resistant Plasmodium falciparum K1 infected in human A+ erythrocytes after 72 hrs by SYBR Green-I fluorescence-based method | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | 4-Thiophenoxy-2-trichloromethyquinazolines display in vitro selective antiplasmodial activity against the human malaria parasite Plasmodium falciparum. |
| AID294069 | Cytotoxicity against L6 cells | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis and antiplasmodial activity of new N-[3-(4-{3-[(7-chloroquinolin-4-yl)amino]propyl}piperazin-1-yl)propyl]carboxamides. |
| AID544217 | Antiplasmodial activity against Plasmodium falciparum FcM29 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | In vitro and in vivo properties of ellagic acid in malaria treatment. |
| AID419115 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 equivalent of drug to 1 molecule of heme in presence of 40% DMSO by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID1167408 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K14 infected in human red blood cells after 48 hrs by [3H]hypoxanthine incorporation assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Diastereoselective synthesis of potent antimalarial cis-β-lactam agents through a [2 + 2] cycloaddition of chiral imines with a chiral ketene. |
| AID160047 | Antiparasitic activity against chloroquine-resistant Plasmodium falciparum W2 | 2004 | Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3 | Diamine derivatives with antiparasitic activities. |
| AID1859906 | Resistance index, ratio of IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID1461810 | Antimalarial activity against synchronized ring stage of chloroquine-resistant Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth at 1 uM after 72 hrs by YOYO-1 staining based flow cytometric analysis relative to control | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | KBE009: An antimalarial bestatin-like inhibitor of the Plasmodium falciparum M1 aminopeptidase discovered in an Ugi multicomponent reaction-derived peptidomimetic library. |
| AID562536 | Antiplasmodial activity against Plasmodium falciparum F32 assessed as suppression of parasitemia after 4 hrs by Giemsa staining | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID1204111 | Cytotoxic activity against human HepG2 cells assessed as cell viability at 0.1 ug/ml incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID420343 | Antimalarial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Design, synthesis and structure-activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials. |
| AID616291 | Antiparasitic activity against Plasmodium falciparum K1 amastigotes IEF stage forms incubated for 72 hrs by Alamar Blue staining based fluorometric assay | 2011 | Journal of natural products, Sep-23, Volume: 74, Issue:9 | Antimalarial β-carbolines from the New Zealand ascidian Pseudodistoma opacum. |
| AID1628536 | Inhibition of hemozoin formation in Plasmodium falciparum assessed as change in free heme per cell at 2.5 times beta-hematin IC50 by cell fractionation assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
| AID1505096 | Antiplasmodial activity against chloroquine/cycloguanil/pyrimethamine-resistant blood stage Plasmodium falciparum K1 by SYBR green 1 staining based fluorescence assay | 2018 | Journal of natural products, 01-26, Volume: 81, Issue:1 | Isolation, Derivative Synthesis, and Structure-Activity Relationships of Antiparasitic Bromopyrrole Alkaloids from the Marine Sponge Tedania brasiliensis. |
| AID377552 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2000 | Journal of natural products, Sep, Volume: 63, Issue:9 | Absolute configuration and antiprotozoal activity of minquartynoic acid. |
| AID1713137 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth incubated for 48 hrs by SYBR green 1 dye based fluorescence assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Polyvalent effect enhances diglycosidic antiplasmodial activity. |
| AID515040 | Therapeutic index, ratio of IC50 for mice (Mus musculus) spleen lymphocytes to IC50 for chloroquine-resistant Plasmodium falciparum Dd2 | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID601826 | Antimalarial activity against Plasmodium berghei ANKA NK65 infected in Swiss Webster mouse assessed as reduction of parasitemia level at 2 mg/kg, po qd administered for 4 days measured 24 hrs after last dose by light microscopic analysis | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice. |
| AID1204137 | Toxicity in Plasmodium berghei NK65 infected Swiss albino mouse assessed as mouse mortality at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 12 post infection relative to untreated control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID656017 | Antagonist activity at TLR7 in human PBMC assessed as inhibition of gardiquimod-induced TNF-alpha release after 12 hrs by bead array assay | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Toll-like receptor (TLR)-7 and -8 modulatory activities of dimeric imidazoquinolines. |
| AID1532624 | Cytotoxicity against African green monkey Vero cells up to 10 uM after 48 hrs by neutral red assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | N-Substituted aminoquinoline-pyrimidine hybrids: Synthesis, in vitro antimalarial activity evaluation and docking studies. |
| AID360000 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha. |
| AID682567 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum F-32 Tanzania assessed as inhibition of parasitemia after 3 days | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18 | Synthesis and antimalarial activity of new haemanthamine-type derivatives. |
| AID377692 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 24 hrs by alamar blue assay | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID300101 | Cytotoxicity against rat L6 cells after 72 hrs by microplate assay | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals. |
| AID544214 | Antiplasmodial activity against Plasmodium falciparum Dd2 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | In vitro and in vivo properties of ellagic acid in malaria treatment. |
| AID152005 | Inhibition of chloroquine uptake from intact parasites | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum. |
| AID158649 | In vivo antimalarial activity against Plasmodium berghei infected mice (Mus musculus) | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Potent antimalarial febrifugine analogues against the plasmodium malaria parasite. |
| AID668289 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Discovery of a new antileishmanial hit in 8-nitroquinoline series. |
| AID1204841 | Cytotoxicity against human SK-MEL cells assessed as cell growth inhibition after 48 hrs by neutral red assay | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID1457202 | Antimalarial activity against Plasmodium falciparum 3D7 0087/N9 infected in NOD/SCID IL2R gamma null mouse assessed as decrease in parasitemia at 2.5 to 50 mg/kg up to 7 days post infection | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID346862 | Antimalarial activity as ED100 in peripheral blood against Plasmodium yoelii 17X infected CD1 mice (Mus musculus) after 4 days | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID1444625 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | N-Piperonyl substitution on aminoquinoline-pyrimidine hybrids: Effect on the antiplasmodial potency. |
| AID1903646 | Antiproliferative activity against human MCF7 cells measured after 2 days by SRB assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233 | Discovery of novel ataxia telangiectasia mutated (ATM) kinase modulators: Computational simulation, biological evaluation and cancer combinational chemotherapy study. |
| AID1688343 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3 infected in human erythrocytes incubated for 48 hrs by [3H]-hypoxanthine incorporation assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID1360909 | Cell cycle arrest in human KYSE410 cells assessed as accumulation at G1 phase at 1 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry (Rvb = 65.4%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma. |
| AID360935 | Cytotoxicity against human KB cells after 72 hrs | 2001 | Journal of natural products, Jun, Volume: 64, Issue:6 | Antimalarial compounds from Rhaphidophora decursiva. |
| AID1167710 | Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis of chiral chloroquine and its analogues as antimalarial agents. |
| AID1145679 | Fold increase in resistance, ratio of IC50 for chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 to IC50 for sensitive Pediococcus cerevisiae ATCC 808 | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID1202798 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives. |
| AID628230 | Antimalarial activity against chloroquine- and mefloquine-resistant Plasmodium falciparum W2-Mef infected in human O-positive erythrocytes assessed as inhibition of schizonts growth after 48 hrs | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | 3-bromohomofascaplysin A, a fascaplysin analogue from a Fijian Didemnum sp. ascidian. |
| AID1829873 | Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay | |||
| AID318209 | Cytotoxicity against mouse NSO cells after 48 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID272291 | Uptake in human HepG2 cells at 100 uM after 4 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID573267 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID1348096 | Antiplasmodial activity against ring-stage of chloroquine-resistant/mefloquine-sensitive Plasmodium falciparum W2 assessed as parasite growth inhibition after 48 hrs by YOYO-1 dye-based flow cytometric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Microwave-promoted facile access to 4-aminoquinoline-phthalimides: Synthesis and anti-plasmodial evaluation. |
| AID1203063 | Ratio of hydroxychloroquine IC50 to compound IC50 for human H460 cells | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID636813 | Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 assessed as parasitaemia after 72 hrs using SYBR Green 1 staining by fluorescence method | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Antimalarial β-carboline and indolactam alkaloids from Marinactinospora thermotolerans, a deep sea isolate. |
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| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
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| AID1706559 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 incubated for 48 hrs by parasite lactate dehydrogenase assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities. |
| AID1815917 | Antimalarial activity against Plasmodium berghei ANKA expressing luciferase, PbGFP-Luccon infected in mouse assessed as reduction in parasitemia at 40 mg/kg, po measured after 4 days by luminescence assay | |||
| AID159725 | Parasitaemia (%) in tail blood smears of Plasmodium berghei infected ICR mice (Mus musculus) at 2 mg/kg/day after 4 days | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID1894267 | Antiplasmodial activity against asexual blood stage Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID1706560 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 incubated for 48 hrs by parasite lactate dehydrogenase assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities. |
| AID459109 | Therapeutic index, Cytotoxicity against human KB cells to Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo. |
| AID418858 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum PH3 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID1859901 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID1676923 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in microbial growth after 72 hrs by SYBR green I staining based fluorescence assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines. |
| AID1059595 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human RBC | 2013 | ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11 | Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties. |
| AID1700301 | Antimalarial activity against Plasmodium berghei NK65 infected in mouse assessed as parasite growth at 20 mg/kg, po administered for 3 days and measured on day 5 Giemsa staining based assay relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission. |
| AID25339 | Association constant was determined | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Carbon isosteres of the 4-aminopyridine substructure of chloroquine: effects on pK(a), hematin binding, inhibition of hemozoin formation, and parasite growth. |
| AID764878 | Antiprotozoal activity against chloroquine- and pyrimethamine-resistant Plasmodium falciparum K1 infected in NMRI mouse assessed as reduction in parasitemia at 50 mg/kg, ip qd for administered 3 days post-inoculation for 4 consecutive days | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom. |
| AID274293 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
| AID740949 | Antitrypanosomal activity against Trypanosoma brucei brucei blood-stream forms | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3 | 8,8-dialkyldihydroberberines with potent antiprotozoal activity. |
| AID1727382 | Inhibition of beta-hematin formation at 12.5 to 200 uM after 16 hrs by inverted microscopic analysis | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Discovery of fast-acting dual-stage antimalarial agents by profiling pyridylvinylquinoline chemical space via copper catalyzed azide-alkyne cycloadditions. |
| AID349756 | Inhibition of beta-hematin formation after 18 hrs by microtiter plate assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives. |
| AID1168868 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID278576 | Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 48 hrs | 2007 | Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1 | Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum. |
| AID1229876 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 7 post infection by Giemsa sta | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID1410112 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting m | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Mbandakamine-Type Naphthylisoquinoline Dimers and Related Alkaloids from the Central African Liana Ancistrocladus ealaensis with Antiparasitic and Antileukemic Activities. |
| AID158875 | In vitro antimalarial activity against Plasmodium falciparum W2 in human erythrocytes by [3H]hypoxanthine uptake | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10 | Synthesis and evaluation of new antimalarial analogues of quinoline alkaloids derived from Cinchona ledgeriana Moens ex Trimen. |
| AID277794 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Synthesis and antimalarial activity of new isotebuquine analogues. |
| AID360380 | Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake | 2007 | The Journal of biological chemistry, Jan-26, Volume: 282, Issue:4 | In vitro efficacy, resistance selection, and structural modeling studies implicate the malarial parasite apicoplast as the target of azithromycin. |
| AID1808277 | Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID663060 | Antimalarial activity against Plasmodium berghei KBG173 infected in mouse assessed as decrease in parasitemia at 1.25 mg/kg, iv BID administered on day 3, 4 and 5 post infection measured on day 31 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin. |
| AID1370897 | Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay | |||
| AID524779 | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by 1536-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID93348 | The compound was tested for survival of the ICR mice (infected with Plasmodium berghei) as a symptom indicative of toxicity on day 4, at a dose of 1.0 mg/kg/day | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID106635 | Cytotoxicity in macrophages; ND = Not determined | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Biological evaluation of substituted quinolines. |
| AID597182 | Solubility of the compound in 0.01 M hydrochloric acid at pH 2 | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies. |
| AID1247993 | Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | Synthesis, in vitro and in silico antimalarial activity of 7-chloroquinoline and 4H-chromene conjugates. |
| AID18982 | Lipophilicity at pH 5; ND = Not determined | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. |
| AID776775 | Antiplasmodial activity against chloroquine-resistant blood stage of Plasmodium falciparum W2 infected in human RBC after 48 hrs by flow cytometric analysis | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Flavones as isosteres of 4(1H)-quinolones: discovery of ligand efficient and dual stage antimalarial lead compounds. |
| AID346869 | Binding affinity to heme in 50 mM SDS surfactant assessed as equilibrium constant by UV-visible spectrophotometry | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID456262 | Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 infected in rat L6 cells | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Synthesis, stereoelectronic characterization and antiparasitic activity of new 1-benzenesulfonyl-2-methyl-1,2,3,4-tetrahydroquinolines. |
| AID675164 | Antimalarial activity against chloroquine-susceptible Plasmodium falciparum 3D7 after 72 hrs by SYBR Green-I based fluorescence assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum. |
| AID712443 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as reduction in parasitemia after 48 hrs by flow cytometry analysis | 2012 | ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12 | 1,4-naphthoquinone cations as antiplasmodial agents: hydroxy-, acyloxy-, and alkoxy-substituted analogues. |
| AID1373373 | Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability after 5 days by MTS/PMS method | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents. |
| AID159907 | Effective subcutaneous dose ED90 against Plasmodium yoelii sspNS | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID1696537 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes incubated for 72 hrs by SYBR green staining based fluorescence assay | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23 | Structural hybridization as a facile approach to new drug candidates. |
| AID318185 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. |
| AID598438 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7 | Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria. |
| AID763598 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected in Swiss mouse assessed as mouse survival at 10 mg/kg, ip qd for 4 days measured on day 28 post infection | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID1355295 | Therapeutic index, ratio of EC50 for human HepG2 cells to IC50 for chloroquine-sensitive blood parasite forms of Plasmodium falciparum 3D7 | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
| AID417936 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum W2 | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Iodine-catalyzed one-pot synthesis and antimalarial activity evaluation of symmetrically and asymmetrically substituted 3,6-diphenyl[1,2,4,5]tetraoxanes. |
| AID674366 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes by lactate dehydrogenase assay | 2012 | Journal of natural products, Jun-22, Volume: 75, Issue:6 | Lasionectrin, a naphthopyrone from a Lasionectria sp. |
| AID423745 | Apparent clearance with respect to bioavailability in human with malaria | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. |
| AID518541 | Antimalarial activity against Plasmodium berghei ANKA infected in NMRI mice (Mus musculus) assessed as survival rate at 100 mg/kg, perorally administered as single dose | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. |
| AID321727 | Cytotoxicity against human HepG2 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines. |
| AID579482 | Cytotoxicity against CHO cells by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 | Synthesis, in vitro antimalarial and cytotoxicity of artemisinin-aminoquinoline hybrids. |
| AID360001 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha. |
| AID1404600 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Microthecaline A, a Quinoline Serrulatane Alkaloid from the Roots of the Australian Desert Plant Eremophila microtheca. |
| AID1361083 | Cytotoxicity against African green monkey Vero cells after 3 days by resazurin dye based fluorescence assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones. |
| AID1571714 | Antiplasmodium activity against multidrug resistant Plasmodium falciparum K1 asexual blood stage forms infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles. |
| AID553551 | Toxicity in malaria patient assessed as vomiting on day 1 after treatment at quartile 1 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID768482 | Ratio of IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in presence of 5 uM ALLN to IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in absence of ALLN | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1649413 | Antimalarial activity against multidrug resistant Plasmodium falciparum Tm90-C2B infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
| AID562538 | Antiplasmodial activity against Plasmodium falciparum W2 assessed as suppression of parasitemia after 4 hrs by Giemsa staining | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID258363 | Inhibition of 1-monooleoyl glycerol induced beta-hematin formation | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | Design, synthesis and in vitro antimalarial activity of an acylhydrazone library. |
| AID1829875 | Anticancer activity against human L02 cells assessed as cell growth inhibition measured for 72 hrs by MTT assay | |||
| AID480244 | Cmax in CD1 mouse at 50 mg/kg, po | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1422823 | Cytotoxicity against human MRC5 cells after 7 days by MTT assay | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme. |
| AID1199050 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Semliki forest virus Vietnam infected in African green monkey Vero cells | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID1337667 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Discovery of new hit-molecules targeting Plasmodium falciparum through a global SAR study of the 4-substituted-2-trichloromethylquinazoline antiplasmodial scaffold. |
| AID1174529 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as reduction in parasitemia at 100 mg/kg/day, po dosed on days 0, 1 and 2 post infection measured on day 5 | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | 4-Aminoquinoline-pyrimidine hybrids: synthesis, antimalarial activity, heme binding and docking studies. |
| AID780279 | Antimalarial activity against ring stage of chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment. |
| AID158533 | In vitro antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum Haiti 135 | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Structure-activity relationships for antiplasmodial activity among 7-substituted 4-aminoquinolines. |
| AID346287 | Antiplasmodial activity against Plasmodium falciparum 3D7 by Giemsa staining | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Ceramicines B-D, new antiplasmodial limonoids from Chisocheton ceramicus. |
| AID1624371 | Antimalarial activity against Plasmodium berghei ANKA infected in Swiss mouse assessed as parasitaemia at 10 mg/kg, ip administered once daily for 5 days measured on 7 days post infection by flow cytometry (Rvb = 19%) | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID763623 | Inhibition of beta-hematin formation in Plasmodium yoelii-infected Swiss albino mouse plasma using hemin as substrate after 16 hrs | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID1648004 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as reduction in parasite growth incubated for 72 hrs by DAPI staining based fluorescence assay | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | A Meroisoprenoid, Heptenolides, and |
| AID366959 | Antimalarial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Synthesis and structure-activity relationship of 3-phenylquinoxaline 1,4-di-N-oxide derivatives as antimalarial agents. |
| AID1361082 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by SYBR Green 1 staining based fluorescence assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones. |
| AID453362 | Dissociation constant, pKa by spectrophotometry | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID504270 | Octanol-water partition coefficient, log P of the compound | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID256011 | In vitro antimalarial activity for Plasmodium falciparum TM91C235 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives. |
| AID1067545 | Selectivity index, ratio of IC50 for human NFF to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria. |
| AID1894268 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID452318 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID1188917 | Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for Plasmodium falciparum 3D7 | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents. |
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| AID723299 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents. |
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| AID310603 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23 | Design, synthesis, and antimalarial activity of structural chimeras of thiosemicarbazone and ferroquine analogues. |
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| AID675163 | Inhibition of beta hematin formation in Plasmodium yoelii infected swiss mouse RBC after 16 hrs | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum. |
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| AID1541969 | Binding affinity to monomeric heme assessed as binding constant in MES buffer in aqueous DMSO solution at pH 5.6 by UV-vis spectrophotometric titration analysis | 2020 | ACS medicinal chemistry letters, Feb-13, Volume: 11, Issue:2 | Functionalized Naphthalimide-4-aminoquinoline Conjugates as Promising Antiplasmodials, with Mechanistic Insights. |
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| AID1494377 | Induction of disaggregation of Cu2+ -associated amyloid beta (1 to 42) (unknown origin) fibrils assessed as small-sized nonfibrillar amorphos amyloid beta at compound/amyloid beta/Cu2+ ratio of 2:1:1 after 48 hrs by TEM analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
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| AID17461 | Acid dissociation constant evaluated towards Hematin mu-oxo dimer | 1999 | Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22 | Structural specificity of chloroquine-hematin binding related to inhibition of hematin polymerization and parasite growth. |
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| AID1169354 | Cytotoxicity against human BJ cells | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
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| AID321728 | Cytotoxicity against human THP1 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1 | Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines. |
| AID524776 | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by 96-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
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| AID1140759 | Resistance index, ratio of IC90 for CQ, MFQ-resistant Plasmodium falciparum TM91C235 clone Southeast asian isolate to IC90 for CQ, MFQ-susceptible Plasmodium falciparum D6 clone Sierra 1/UNC isolate | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Second generation steroidal 4-aminoquinolines are potent, dual-target inhibitors of the botulinum neurotoxin serotype A metalloprotease and P. falciparum malaria. |
| AID1254195 | Antiplasmodial activity against Plasmodium berghei ANKA expressing GFP infected in mouse assessed as reduction of parasitemia level at 30 mg/kg, po qd for 4 days | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines. |
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| AID1494301 | Inhibition of Cu2+ - induced amyloid beta (1 to 42) (unknown origin) aggregation at compound/amyloid beta/Cu2+ ratio of 2:1:1 after 48 hrs by thioflavin T-based fluorometric assay relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
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| AID1699558 | Antiplasmodial activity against multidrug-sensitive asexual blood stage Plasmodium falciparum NF54 strain assessed as reduction in parasite growth after 72 hrs by NBT reagent based LDH assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and |
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| AID1575013 | Antimalarial activity against GFP-fused Plasmodium berghei ANKA infected in NMRI mouse assessed as inhibition of parasitemia at 30 mg/kg, po administered for 4 consecutive days by flow cytometry relative to control | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria. |
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| AID1764403 | Agonist activity at Gal4-fused human Nurr1 LBD expressed in HEK293T cells co-expressing firefly luciferase assessed as luciferase activity incubated for 12 to 14 hrs by hybrid reporter gene assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Fragment-like Chloroquinolineamines Activate the Orphan Nuclear Receptor Nurr1 and Elucidate Activation Mechanisms. |
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| AID337519 | Cytotoxicity against human BCA1 cells after 3 days by sulforhodamine B assay | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
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| AID617829 | Antimalarial activity against mefloquine-resistant and chloroquine-sensitive Plasmodium falciparum D6 | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against Plasmodium falciparum. |
| AID284265 | Antifungal activity against Candida albicans | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID1808441 | Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as decrease in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by luciferase reporter gene as | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID509182 | Inhibition of TLR7-mediated upregulation of IRF7 expression in aldrithiol-2-treated HIV1 MN-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
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| AID482876 | Inhibition of Plasmodium falciparum falcipain-2 after 12 hrs by fluorescence spectroscopy-based on-bead assay | 2009 | Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18 | On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences. |
| AID666490 | Antibacterial activity against Streptococcus pneumoniae isolate SP030 by broth microdilution method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
| AID1228729 | Antiviral activity against Semliki forest virus strain Vietnam infected in african green monkey Vero cells assessed as inhibition of virus induced cell death measured after 7 days | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
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| AID705466 | Antiapicomplexan activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as growth inhibition after 72 hrs by MSF assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | Salicylanilide inhibitors of Toxoplasma gondii. |
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| AID722964 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by SYBR green assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Isolation and identification of β-hematin inhibitors from Flacourtia indica as promising antiplasmodial agents. |
| AID731503 | Cytocidal antimalarial activity against drug-sensitive Plasmodium falciparum HB3 intraerythrocytic stage | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3 | Antiproliferative and antiplasmodial dimeric phloroglucinols from Mallotus oppositifolius from the Madagascar Dry Forest (1). |
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| AID1894269 | Antiplasmodial activity against Plasmodium falciparum NF54 expressing transgenic luciferase assessed as parasite kill rate at trophozoite stage incubated for 72 hrs by bioluminescence relative rate of kill (BRRoK) assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID358507 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum PFB Brazil by [3H]hypoxanthine uptake | 2001 | Journal of natural products, Jan, Volume: 64, Issue:1 | Strychnogucines A and B, two new antiplasmodial bisindole alkaloids from Strychnos icaja. |
| AID1059807 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by [3H]hypoxanthine incorporation assay | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12 | Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
| AID1362632 | Inhibition of BACE 1 (unknown origin) at 10 to 50 uM using Rh-EVNLDAEFK-Quencher as substrate after 1 hr by FRET assay relative to control | |||
| AID1649433 | Inhibition of human ERG expressed in HEK293 cells at 10 uM by IonWorks patch clamp method relative to control | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
| AID603033 | Cytotoxicity against african green monkey Vero cells at 12.5 uM | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates. |
| AID1239623 | Antiplasmodial activity against CQ-resistant Plasmodium falciparum K1 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Quinoline-based antimalarial hybrid compounds. |
| AID636824 | Antileishmanial activity against Leishmania donovani MHOM/ET/L82/LV9 promastigotes after 3 days by MTT assay | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark. |
| AID673596 | Cytotoxicity against african green monkey Vero cells | 2012 | Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15 | Short synthesis and antimalarial activity of fagaronine. |
| AID123175 | Number of Plasmodium berghei infected mice died at 640 mg/kg; Toxic | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines. |
| AID1204135 | Toxicity in Plasmodium berghei NK65 infected Swiss albino mouse assessed as mouse mortality at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 7 post infection relative to untreated control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID444058 | Volume of distribution at steady state in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID1359552 | Antiplasmodial activity against Plasmodium falciparum D6 after 72 hrs by MSF assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID477964 | Binding affinity to pUC18 DNA containing 50% AT assessed as middle of the integrated surface melting temperature at 1 uM by spectrophotometry analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID704425 | Antimicrobial activity against Plasmodium falciparum NF54 | 2011 | ACS medicinal chemistry letters, Apr-14, Volume: 2, Issue:4 | 3-Alkoxy-1,2-Dioxolanes: Synthesis and Evaluation as Potential Antimalarial Agents. |
| AID106372 | Cytotoxicity against human diploid embryonic lung cell line (MRC5 cells) using the colorimetric MTT assay | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID768492 | Gametocytocidal activity against synchronous stage 4 to 5 of transgenic Plasmodium falciparum NF54 gametocyte harboring pfs16 promoter assessed as inhibition of parasite viability at 60 uM after 72 hrs by MitoTracker Red CMXRos-based assay relative to con | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID410199 | Antimalarial activity as reduced parasitaemia after 4 days against Plasmodium yoelii N67 infected Swiss mice (Mus musculus) at 50 mg/kg/day intraperitoneal dose | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents. |
| AID442268 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCM29 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID1203041 | Antiproliferative activity against human H460 cells after 72 hrs by SRB method | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID630861 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum NF54 | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID1432055 | Antiproliferative activity against SV40 large T-antigen 38 immortalized HMEC1 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure-Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents. |
| AID1810597 | Antiplasmodial activity against asexual blood stage of multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | |||
| AID389449 | Cytotoxicity against rat L6 cells | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
| AID636378 | Therapeutic index, ratio of MTD for Sprague-Dawley rat to MCD for blood stage of Plasmodium berghei NK65 | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID641577 | Antimalarial activity against chloroquine-, pyrimethamine-resistant ring stage Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Synthesis, antimalarial activity, and structure-activity relationship of 7-(2-phenoxyethoxy)-4(1H)-quinolones. |
| AID319200 | Antimalarial activity against Plasmodium falciparum TM4 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles. |
| AID1181517 | Resistance index, ratio of IC50 for Plasmodium falciparum K1 to IC50 for Plasmodium falciparum 3D7 | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Kojic acid derived hydroxypyridinone-chloroquine hybrids: synthesis, crystal structure, antiplasmodial activity and β-haematin inhibition. |
| AID480241 | Hepatotoxicity in Sprague-Dawley rat hepatocytes after 20 to 24 hrs by LDH assay | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1067546 | Cytotoxicity against human NFF after 72 hrs by SRB assay | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria. |
| AID1236482 | Resistance index, ratio of IC50 for asexual intraerythrocytic ring stage of chloroquine-resistant Plasmodium falciparum W2 infected in human O+ erythrocytes to IC50 for asexual intraerythrocytic ring stage of chloroquine-sensitive Plasmodium falciparum 3D | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites. |
| AID1056374 | Antimicrobial activity against mid-ring stage Plasmodium falciparum 3D7 infected in erythrocytes assessed as reduction in parasitemia at 500 nM after 8 hrs by Giemsa-staining based microscopy relative to control | 2013 | ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11 | Adamantyl derivative as a potent inhibitor of Plasmodium FK506 binding protein 35. |
| AID1457216 | Antimalarial activity against intraerythrocytic stage of Plasmodium falciparum assessed as time required for maximal killing effect at 10 times IC50 preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation coun | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID232837 | Vacuolar accumulation ratio was determined | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID605903 | Antimalarial activity against GFP-tagged Plasmodium berghei ANKA infected in NMRI mouse assessed as mouse survival at 30 mg/kg, po administered as single dose 24 hrs post infection measured on day 30 post infection | 2011 | Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14 | Imidazolopiperazines: hit to lead optimization of new antimalarial agents. |
| AID1633705 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as suppression in parasitemia at 11.1 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 7 post infection relative to untreated control | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID1236480 | Antiplasmodial activity against asexual intraerythrocytic ring stage of chloroquine-resistant Plasmodium falciparum W2 infected in human O+ erythrocytes assessed as inhibition of parasitic proliferation after 96 hrs by SYBR Green-1 based fluorescence assa | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites. |
| AID1422833 | Binding affinity to hemin assessed as protection against H2O2-induced hemin degradation up to 100 uM at pH 5.2 preincubated followed by H2O2 addition measured after 120 mins | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID597766 | Antiplasmodial activity against Plasmodium falciparum 3D7 by Geimsa staining method | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | New antiplasmodial indole alkaloids from Hunteria zeylanica. |
| AID1428722 | Antiviral activity against Zika virus infected in African green monkey Vero cells assessed as inhibition of viral RNA replication after 24 hrs by RT-PCR method | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | 2,8-bis(trifluoromethyl)quinoline analogs show improved anti-Zika virus activity, compared to mefloquine. |
| AID452325 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 1 uM CuCl2 | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID453369 | Cytotoxicity against human KB cells after 72 hrs by MTS assay | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID1348959 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by LDH release assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | A minimalistic approach to develop new anti-apicomplexa polyamines analogs. |
| AID159722 | Parasitaemia (%) in tail blood smears of Plasmodium berghei infected ICR mice (Mus musculus) at 1.0 mg/kg/day after 4 days | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID554750 | Antimalarial activity against Plasmodium berghei NK-65 infected in Swiss Webster mouse assessed as suppression of parasitemia at 30 mg/kg, ip QD for 3 days administered 2 hrs post infection measured on day 10 | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID1126851 | Selectivity index, ratio of CC50 for human MCF7 cells to IC50 for chloroquine-resistant Plasmodium falciparum FcB1 infected in RBC | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | 2-Aryl-3H-indol-3-ones: synthesis, electrochemical behaviour and antiplasmodial activities. |
| AID351793 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10 | Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids. |
| AID255870 | In vitro antimalarial activity for Plasmodium falciparum TM91C235 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives. |
| AID159755 | Growth inhibitory concentration against Plasmodium falciparum K1 | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Carbon isosteres of the 4-aminopyridine substructure of chloroquine: effects on pK(a), hematin binding, inhibition of hemozoin formation, and parasite growth. |
| AID1433151 | Antiviral activity against TK negative Varicella-zoster virus 07-1 infected in human HEL cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID1241102 | Antiplasmodial activity against Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. |
| AID1155336 | Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
| AID477943 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum Bres infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID678313 | Inhibition of Plasmodium ovale PLM4 using Lys-Glu-Phe-Val-Phe-NPhe-Ala-Leu-Lys as substrate by spectrophotometry | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID1274588 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis | 2015 | Journal of natural products, Dec-24, Volume: 78, Issue:12 | Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis. |
| AID1143813 | Antimicrobial activity against chloroquine-resistant and mefloquine-sensitive Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by SYBR Green I assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, synthesis and biological evaluation of novel 4-alkapolyenylpyrrolo[1,2-a]quinoxalines as antileishmanial agents--part III. |
| AID1533489 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as tail detachment up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID768483 | Ratio of IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in presence of 0.2 uM ALLN to IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs in absence of ALLN | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID607826 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7A assessed as death of all detectable parasites at 4 days dosage of 0.05 uM using Hema 3 staining by microscopic analysis | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models. |
| AID635309 | Cytotoxicity against mouse 3T3 cells after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives. |
| AID545363 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum C3 harboring Dd2 pfcrt allele infected in erythrocytes assessed as [3H]hypoxanthine incorporation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro. |
| AID152128 | Selectivity for FM3A cells over Plasmodium falciparum as mean EC50 ratio | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum. |
| AID425021 | Antiplasmodial activity against Plasmodium falciparum W2 | 2009 | Journal of natural products, May-22, Volume: 72, Issue:5 | Biologically active cannabinoids from high-potency Cannabis sativa. |
| AID491991 | Cytotoxicity against african green monkey Vero cell after 48 hrs by Neutral Red dye | 2010 | Journal of natural products, Jul-23, Volume: 73, Issue:7 | Bioactive 1,4-dihydroxy-5-phenyl-2-pyridinone alkaloids from Septoria pistaciarum. |
| AID442351 | Cytotoxicity against human K562 cells after 72 hrs by flow cytometry | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Original quinazoline derivatives displaying antiplasmodial properties. |
| AID1728293 | Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 strain | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities. |
| AID477948 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum FCM29 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID406386 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcM29 by [3H]hypoxanthine uptake | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID612145 | Toxicity in C57BL/6J mouse splenic lymphocytes after 72 hrs by Alamar blue Assay | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | Antimalarial activity of natural and synthetic prodiginines. |
| AID1234843 | Inhibition of haemozoin formation using hemin chloride assessed as beta-hematin formation at 5 to 100 uM after 48 hrs | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Synthesis, β-hematin inhibition studies and antimalarial evaluation of dehydroxy isotebuquine derivatives against Plasmodium berghei. |
| AID347213 | Antimalarial schizonticidal activity against Plasmodium falciparum 3D7 infected erythrocytes at 1.25 ug/ml after 30-39 hrs | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials. |
| AID1779235 | Selectivity index, ratio of IC50 for antimalarial activity against Plasmodium falciparum Dd2 to IC50 of antimalarial activity against Plasmodium falciparum 3D7 | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Discovery and development of 2-aminobenzimidazoles as potent antimalarials. |
| AID1138598 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as growth inhibition by lactate dehydrogenase assay | 2014 | Journal of natural products, Apr-25, Volume: 77, Issue:4 | Strychnobaillonine, an unsymmetrical bisindole alkaloid with an unprecedented skeleton from Strychnos icaja roots. |
| AID1486833 | Antimalarial activity against Plasmodium falciparum ring stage forms after 48 hrs | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | 1,2,4-Triazole and 1,3,4-oxadiazole analogues: Synthesis, MO studies, in silico molecular docking studies, antimalarial as DHFR inhibitor and antimicrobial activities. |
| AID333072 | Antileishmanial activity against Leishmania donovani | 2004 | Journal of natural products, Aug, Volume: 67, Issue:8 | Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases. |
| AID1714085 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by liquid | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle. |
| AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID1204122 | Selectivity index, ratio of CC50 for human HeLa cells to IC50 for CQ-sensitive Plasmodium falciparum 3D7 | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID553560 | Toxicity in malaria patient assessed as duration of vomiting at quartile 2 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID1228731 | Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for Chikungunya virus strain 899 | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID404449 | Antimalarial activity against Plasmodium falciparum W2 by hypoxanthine uptake | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
| AID623334 | Antimalarial activity against Plasmodium berghei NK65 infected in mouse assessed as reduction of host mortality at 50 mg/kg, ip qd for 4 days | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Antimalarial activity of physalins B, D, F, and G. |
| AID1771331 | Antimalarial activity against Plasmodium falciparum 7G8 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting met | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials. |
| AID377365 | Antiplasmodial activity against Plasmodium falciparum D6 | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | Bisnortriterpenes from Salacia madagascariensis. |
| AID1512687 | Cytotoxicity against human BT474 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy. |
| AID298579 | Antimalarial activity against Plasmodium falciparum W2 | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1). |
| AID372429 | Trypanocidal activity against Trypanosoma cruzi Tulahuen C4 trypomastigotes infected in mouse macrophage by reporter dye assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | 2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. |
| AID1145683 | Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction in growth in presence of 0.001 ug/ml folic acid | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID605904 | Antimalarial activity against GFP-tagged Plasmodium berghei ANKA infected in NMRI mouse assessed as mouse survival at 100 mg/kg, po administered as single dose 24 hrs post infection measured on day 30 post infection | 2011 | Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14 | Imidazolopiperazines: hit to lead optimization of new antimalarial agents. |
| AID768472 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as nonviable parasite at 200 uM after 0.5 hrs by SYTO 61 staining-based flow cytometric analysis relative to untreated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1808458 | Modulation of full length human NOR1 expressed in SK-N-BE(2) cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID586613 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. |
| AID1460343 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents. |
| AID247811 | Inhibitory concentration against chloroquine-sensitive Plasmodium falciparum | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Potent 4-aminopiperidine based antimalarial agents. |
| AID1203053 | Cytotoxicity against human C8161 cells after 72 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID762744 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as increase of survival days of host at 10 mg/kg, po qd for 4 days (Rvb = 20 +/- 2.7 days) | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16 | In vivo antimalarial activity of novel 2-hydroxy-3-anilino-1,4-naphthoquinones obtained by epoxide ring-opening reaction. |
| AID586611 | Antimalarial activity against Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. |
| AID316598 | Antiplasmodial activity against parasitemia in Plasmodium berghei ANKA infected NMRI mice (Mus musculus) at 5 mg/kg intraperitoneal dose after 4 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity. |
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| AID1848831 | Induction of autophagy in human HCT-116 cells assessed as increase in LC-3B puncta level measured after 12 to 24 hrs by immunofluorescence analysis | |||
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| AID1770444 | Selectivity index, ratio of CC50 for cytotoxicity against human HepG2 cells to EC50 for antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 infected in human erythrocytes | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Antiplasmodial 2-thiophenoxy-3-trichloromethyl quinoxalines target the apicoplast of Plasmodium falciparum. |
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| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
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| AID1057937 | Antiproliferative activity against human HFF1 cells after 2 days by sulforhodamine B assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues. |
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| AID502038 | Antimicrobial activity against Giardia intestinalis IMSS:0696:1 after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas. |
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| AID666492 | Antibacterial activity against Staphylococcus aureus ATCC 13709 by broth microdilution method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
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| AID1688338 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcM29(CQR)Cameroon incubated for 48 hrs by classical radioactive microdilution method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
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| AID774128 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as parasite growth inhibition after 72 hrs by SYBR green 1 dye-based fluorometric analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives. |
| AID1291841 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by SYBR test | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | New pentasubstituted pyrrole hybrid atorvastatin-quinoline derivatives with antiplasmodial activity. |
| AID426725 | Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 by Malstat LDH activity | 2009 | Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15 | Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes. |
| AID509187 | Inhibition of TLR7-mediated IFN-gamma production in aldrithiol-2-treated HIV1 Ada-stimulated human PBMC after 20 hrs by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID1593287 | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring V259L mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials. |
| AID564297 | Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID1176086 | Selectivity index, ratio of IC50 for HMEC1 to IC50 for Leishmania infantum MHOM/TN/80/IPT1 | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Clofazimine analogs with antileishmanial and antiplasmodial activity. |
| AID419125 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 equivalent of drug to 1 molecule of heme in presence of 1.22 mM TX-100 by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID400961 | Antiplasmodial activity against Plasmodium falciparum 3D7 by [3H]phenylalanine uptake | 2004 | Journal of natural products, Apr, Volume: 67, Issue:4 | Labdanes and isopimaranes from Platycladus orientalis and their effects on erythrocyte membrane and on Plasmodium falciparum growth in the erythrocyte host cells. |
| AID673603 | Antiplasmodial activity Plasmodium vinckei petteri infected in CD mouse assessed as survival of infected mouse at 10 mg/kg/day, ip administered from day 0 to day 3 and measured on day 4 (Rvb = 9.5 days) | 2012 | Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15 | Short synthesis and antimalarial activity of fagaronine. |
| AID1353880 | Binding affinity to mu-oxodimeric heme at pH 5.8 by titration-based UV-vis spectrophotometric analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. |
| AID337545 | Selectivity index, ratio of ED50 for mice (Mus musculus) P388 cells to ED50 for chloroquine-resistant Plasmodium falciparum W2 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1701747 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in po dosed NSG mouse assessed as reduction in parasitemia administered twice daily for 4 consecutive days starting from day 3 post-infection and measured 24 hrs post last dose by flow cyt | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity. |
| AID88262 | Inhibitory concentration of compound for inhibiting hematin polymerization | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Carbon isosteres of the 4-aminopyridine substructure of chloroquine: effects on pK(a), hematin binding, inhibition of hemozoin formation, and parasite growth. |
| AID1172870 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23 | Pentacycloundecylamines and conjugates thereof as chemosensitizers and reversed chloroquine agents. |
| AID1433150 | Antiviral activity against TK positive Varicella-zoster virus OKA infected in human HEL cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID384958 | Antimalarial activity as reduced parasitaemia against Plasmodium yoelii YM in CD1 mice (Mus musculus) after 7 peroral doses over 4 days | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9 | Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials. |
| AID446176 | Antimalarial activity against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) assessed as reduction in parasitemia at 48 mg/kg, intraperitoneally after 3 days measured on day 4 | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and antiplasmodial activity of new indolone N-oxide derivatives. |
| AID663058 | Antimalarial activity against Plasmodium berghei KBG173 infected in mouse assessed as decrease in parasitemia at 5 mg/kg, iv BID administered on day 3, 4 and 5 post infection measured on day 31 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin. |
| AID1359557 | Selectivity index, ratio of CC50 for human HepG2A16 cells by MTT assay to IC50 for multidrug-resistant Plasmodium falciparum FCR-3 | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID573258 | Toxicity in human RBC assessed as hemolysis at 50 uM | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID620093 | Antimalarial activity against drug-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 96 hrs by SYBR Green I-based fluorescence assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities. |
| AID606336 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of parasite growth after 24 hrs by Geimsa staining based light microscopic analysis | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | A new class of phenazines with activity against a chloroquine resistant Plasmodium falciparum strain and antimicrobial activity. |
| AID1085761 | Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 48 hr by neutral red assay | 2012 | Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Oct, Volume: 21, Issue:10 | Antimicrobial and antiprotozoal activities of secondary metabolites from the fungus Eurotium repens. |
| AID1673537 | Antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 incubated for 72 hrs by SYBR Green-1 dye based fluorescence assay | |||
| AID393081 | Antimalarial activity as mean survival days against Plasmodium berghei NK65 infected ICR mice (Mus musculus) at 30 mg/kg/day peroral dose | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Pharmacodynamics and pharmacokinetics studies of phenoxazinium derivatives for antimalarial agent. |
| AID740871 | Antimalarial activity against Plasmodium falciparum FCR-3 infected in human erythrocytes after 72 hrs by lactate dehydrogenase assay | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8 | Borrelidin analogues with antimalarial activity: design, synthesis and biological evaluation against Plasmodium falciparum parasites. |
| AID1202794 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as growth inhibition after 18 hrs by [3H]-hypoxanthine uptake assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives. |
| AID359667 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 1992 | Journal of natural products, Dec, Volume: 55, Issue:12 | Antimalarial activity of sesquiterpenes from the marine sponge Acanthella klethra. |
| AID1513841 | Antimalarial activity against Plasmodium falciparum K1 infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition and measured after 24 hrs by liquid scintillation counting | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains. |
| AID558834 | Antimalarial activity against Plasmodium falciparum IMT Bres assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID477934 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID358586 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of natural products, Nov, Volume: 64, Issue:11 | Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp. |
| AID1763361 | Antiplasmodial activity against CQ-resistant Plasmodium falciparum W2 | 2021 | Bioorganic & medicinal chemistry, 06-01, Volume: 39 | A trio of quinoline-isoniazid-phthalimide with promising antiplasmodial potential: Synthesis, in-vitro evaluation and heme-polymerization inhibition studies. |
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| AID1201061 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Synthesis of isocryptolepine analogues and their structure-activity relationship studies as antiplasmodial and antiproliferative agents. |
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| AID378570 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2005 | Journal of natural products, Mar, Volume: 68, Issue:3 | Ambigol C and 2,4-dichlorobenzoic acid, natural products produced by the terrestrial cyanobacterium Fischerella ambigua. |
| AID1212314 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
| AID562539 | Antiplasmodial activity against Plasmodium falciparum W2 gametocytes assessed as suppression of parasitemia after 4 hrs by Giemsa staining | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID1332932 | Binding affinity to mu-oxodimeric heme (unknown origin) assessed as association constant at pH 5.8 by UV-titration method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 4, 5-Dihydrooxazole-pyrazoline hybrids: Synthesis and their evaluation as potential antimalarial agents. |
| AID343940 | Antimalarial activity against chloroquine and pyrimethamine-sensitive Plasmodium falciparum D6 | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Mixed tetraoxanes containing the acetone subunit as antimalarials. |
| AID51933 | Cytotoxicity against Chinese hamster ovary cells; ND is no data | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
| AID323672 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
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| AID1494363 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as swimming path length in effective region at 30 mg/kg/day, po for 80 days by Morris water maze test (Rvb = 44.2 +/- 4.9 cm) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID477940 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum Voll infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID217953 | Concentration required for half-maximal inhibition of CpG-ODN effect on thymidine uptake by WEHI 231 murine B-cells in the presence of alpha-sIgM. | 1999 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 9, Issue:13 | Structure-activity relationship analysis of substituted 4-quinolinamines, antagonists of immunostimulatory CpG-oligodeoxynucleotides. |
| AID159721 | Parasitaemia (%) in tail blood smears of Plasmodium berghei infected ICR mice (Mus musculus) at 0.5 mg/kg/day after 4 days | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID480245 | AUClast in CD1 mouse at 50 mg/kg, po | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1234227 | Reduction in GFP expression in human HepG2 cells transfected with plasmids co-expressing GFP and shRNAs against REV-ERBbeta followed by compound treatment 24 hrs post-transfection and measured 48 hrs post dose | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. |
| AID1368006 | Antimalarial activity against Plasmodium falciparum in infected in human RBC | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Ionic liquid mediated stereoselective synthesis of alanine linked hybrid quinazoline-4(3H)-one derivatives perturbing the malarial reductase activity in folate pathway. |
| AID1542988 | Cytotoxicity in human HMEC1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Covalent Inhibitors of |
| AID1633693 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 incubated for 48 hrs by parasite lactate dehydrogenase assay | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID1460342 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents. |
| AID358585 | Antimalarial activity against Plasmodium falciparum D6 | 2001 | Journal of natural products, Nov, Volume: 64, Issue:11 | Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp. |
| AID499809 | Antimalarial activity against Plasmodium falciparum D6 after 72 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
| AID1378964 | Schizontocidal activity against chloroquine-sensitive Plasmodium falciparum after 3 days | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID285472 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcM29 | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
| AID349755 | Binding affinity to DNA assessed as intercalation after 24 hrs by DNA-methyl green assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives. |
| AID647314 | Antimalarial activity against ring stage chloroquine-resistant Plasmodium falciparum Dd2 infected in human O positive erythrocytes after 48 hrs by SYBR green 1 fluorescence assay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Stilbene-chalcone hybrids: design, synthesis, and evaluation as a new class of antimalarial scaffolds that trigger cell death through stage specific apoptosis. |
| AID748225 | Binding affinity to hematin (unknown origin) by UV-visible titration analysis | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria. |
| AID765175 | Antiplasmodial activity chloroquine-resistant Plasmodium falciparum W2 using YOYO-1 staining after 48 hrs by FACS analysis | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents. |
| AID1312226 | Selectivity index, ratio of MLD50 for african green monkey BGM cells to IC50 for chloroquine/sulfadoxine-resistant Plasmodium falciparum W2 | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Design, synthesis and anti-P. falciparum activity of pyrazolopyridine-sulfonamide derivatives. |
| AID1504881 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based confocal microplate imaging method | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12 | Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana. |
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| AID1713579 | Inhibition of beta-hematin formation measured after 24 hrs by spectrophotometry analysis | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents. |
| AID212183 | Number of survivals against Plasmodium yoelii in mice (Mus musculus) (out of 5) at 24 mg/kg/day orally on day 28 | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Orally active amino functionalized antimalarial 1,2,4-trioxanes. |
| AID285480 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 4 & 5) | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
| AID393025 | Antiparasitic activity against Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | New potent imidazoisoquinolinone derivatives as anti-Trypanosoma cruzi agents: biological evaluation and structure-activity relationships. |
| AID562541 | Cytotoxicity against human THP1 cells assessed as incorporation of [3H]hypoxanthine after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID346547 | Selectivity index, ratio of TC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Synthesis and evaluation of dihydroartemisinin and dihydroartemisitene acetal dimers showing anticancer and antiprotozoal activity. |
| AID346861 | Antimalarial activity as reduced parasitaemia against Plasmodium yoelii 17X infected CD1 mice (Mus musculus) after 4 days | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID399302 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum CAMP by semiautomated micro dilution assay | |||
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| AID519975 | Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs in presence of 40 uM protease inhibitor ALLN | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum. |
| AID311094 | Effect on erythrocyte shape in human erythrocytes assessed as stomatocytes at 100 ug/mL after 48 hrs | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Transformations of manool. tri- and tetracyclic norditerpenoids with in vitro activity against Plasmodium falciparum. |
| AID360381 | Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake | 2007 | The Journal of biological chemistry, Jan-26, Volume: 282, Issue:4 | In vitro efficacy, resistance selection, and structural modeling studies implicate the malarial parasite apicoplast as the target of azithromycin. |
| AID114291 | Antimalarial efficacy against Plasmodium berghei in mice (Mus musculus) when administered intravenously each day for 4 days to five mice (Mus musculus) per dose regimen | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19 | Antimalarial simplified 3-aryltrioxanes: synthesis and preclinical efficacy/toxicity testing in rodents. |
| AID1188457 | Antimalarial activity against tightly synchronized Plasmodium falciparum K1 assessed as parasite stage accumulation index at late ring stages at 10 uM treated at 18 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytolo | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID635241 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human type A-positive red blood cells assessed as parasite lactate dehydrogenase activity after 72 hrs by spectrophotometric analysis | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | A new class of antimalarial dioxanes obtained through a simple two-step synthetic approach: rational design and structure-activity relationship studies. |
| AID318192 | Reduced parasitemia in Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) at 10 mg/kg intraperitoneal dose after 4 days | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. |
| AID562271 | Antimalarial activity against Plasmodium falciparum isolates assessed as parasite growth inhibition after 72 hrs by ELISA based histidine-rich protein 2 in vitro drug susceptibility assay | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Antimalarial activity of tigecycline, a novel glycylcycline antibiotic. |
| AID268568 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR3 by pLDH reporter assay | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Exploration of a new type of antimalarial compounds based on febrifugine. |
| AID549613 | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 assessed as inhibition of [3H]hypoxanthine uptake in presence of 1 mM folinic acid | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones. |
| AID748228 | Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria. |
| AID26756 | DNA binding dissociation constant as KD | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics. |
| AID1699653 | Selectivity index, ratio of IC50 for cytotoxicity against human HEK293 cells to IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 ring stage | 2020 | Journal of natural products, 11-25, Volume: 83, Issue:11 | Antiplasmodial Alkaloids from the Australian Bryozoan |
| AID123194 | Number of Plasmodium berghei infected mice died on day 20 at 160 mg/kg | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines. |
| AID1145674 | Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID1355324 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as reduction in parasitemia at 20 mg/kg, po administered via gavage for 3 consecutive days post infection measured on day 7 post infection relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
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| AID1140209 | Binding affinity to haematin assessed as inhibition of beta-haematin formation after 5 to 6 hrs by pyridine-ferrichrome-based method | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis, β-haematin inhibition, and in vitro antimalarial testing of isocryptolepine analogues: SAR study of indolo[3,2-c]quinolines with various substituents at C2, C6, and N11. |
| AID1541968 | Binding affinity to monomeric heme assessed as binding constant in HEPES buffer in aqueous DMSO solution at pH 7.4 by UV-vis spectrophotometric titration analysis | 2020 | ACS medicinal chemistry letters, Feb-13, Volume: 11, Issue:2 | Functionalized Naphthalimide-4-aminoquinoline Conjugates as Promising Antiplasmodials, with Mechanistic Insights. |
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| AID510910 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 30 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
| AID725846 | Inhibition of Plasmodium falciparum recombinant DXR using DXP as substrate preincubated for 5 mins | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Antimalarial and Structural Studies of Pyridine-containing Inhibitors of 1-Deoxyxylulose-5-phosphate Reductoisomerase. |
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| AID452326 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 10 uM CuCl2 | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID404600 | Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense. |
| AID1254196 | Antiplasmodial activity against Plasmodium berghei ANKA expressing GFP infected in mouse assessed as means survival days at 30 mg/kg, po qd for 4 days | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
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| AID1156604 | Antiparasitic activity against Trypanosoma cruzi Tulahen LacZ/C4 amastigotes after 4 days by beta-galactosidase reporter gene assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups. |
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| AID1228553 | Antimalarial activity against Plasmodium falciparum 3D7A infected in red blood cells assessed as inhibition of parasite growth after 24 hrs by [3H]hypoxanthine incorporation assay | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides. |
| AID1405799 | Induction of autophagy in human HeLa cells assessed as increase in LC3-2 to LC3-1 ratio at 10 uM after 6 hrs by immunoblot analysis relative to control | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
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| AID763612 | Cmax in Sprague-Dawley rat at 5 mg/kg, po | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
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| AID1649415 | Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for multidrug resistant Plasmodium falciparum D6 infected in human erythrocytes | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
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| AID1533503 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring growth retardation up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
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| AID1808452 | Modulation of full length human Nurr1 expressed in SK-N-BE(2) cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by lucifera | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID480236 | Inhibition of CYP3A4 in human liver microsomes assessed as metabolite produced at 10 uM using testosterone as substrate by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID151360 | In vitro efficacy for chloroquine-resistant Plasmodium falciparum Thai | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24 | A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline. |
| AID341405 | Toxicity against human erythrocytes assessed as potentiation of heme-induced hemolysis at 10 uM in presence of heme | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | 2-tert-butyl-8-quinolinamines exhibit potent blood schizontocidal antimalarial activity via inhibition of heme crystallization. |
| AID499274 | Selectivity index, ratio of IC50 for human THP1 cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
| AID518571 | Antimalarial activity against Plasmodium berghei ANKA infected in perorally dosed NMRI mice (Mus musculus) assessed as reduction in parasitemia administered as single dose measured on day 3 postinfection | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. |
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| AID754530 | Inhibition of hemozoin formation in 8 M acetate buffer at pH 5 after 18 hrs by microtiter plate-based high-throughput assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID676998 | Selectivity index, ratio of CC50 for human HeLa cells to IC50 for VSV-G pseudotyped HIV1 lentiviral particles | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
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| AID703896 | Mutagenicity against Salmonella typhimurium TA98 assessed as revertants at 80 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1212341 | Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
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| AID636826 | Cytotoxicity against african green monkey Vero cells | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Structure and in vitro antiparasitic activity of constituents of Citropsis articulata root bark. |
| AID366962 | Selectivity index, ratio of IC50 for human KB cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Synthesis and structure-activity relationship of 3-phenylquinoxaline 1,4-di-N-oxide derivatives as antimalarial agents. |
| AID411378 | Antimalarial activity as reduced parasitaemia after 72 hrs against chloroquine-resistant Plasmodium falciparum FCB in human erythrocytes by DAPI stain | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum. |
| AID316965 | Antimalarial activity against Plasmodium falciparum D6 in parasite LDH assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Synthesis, thermal stability, antimalarial activity of symmetrically and asymmetrically substituted tetraoxanes. |
| AID343753 | Cytotoxicity against HMEC1 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Novel amodiaquine congeners as potent antimalarial agents. |
| AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID675405 | Resistant index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Synthesis and in vitro antimalarial activity of a series of bisquinoline and bispyrrolo[1,2a]quinoxaline compounds. |
| AID537630 | Inhibition of Schistosoma mansoni recombinant NAD+ glycohydrolase expressed in Pichia pastoris at up to 100 uM by continuous fluorometric method | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Identification by high-throughput screening of inhibitors of Schistosoma mansoni NAD(+) catabolizing enzyme. |
| AID623650 | Antiproliferative activity against human A2780 cells | 2011 | Journal of natural products, Oct-28, Volume: 74, Issue:10 | Antiplasmodial and antiproliferative pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest. |
| AID1378985 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcM29 infected in human red blood cells after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID275999 | Effect on survival of mice (Mus musculus) infected with Plasmodium berghei at 640 mg/kg, perorally | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | In vitro and in vivo efficacy and in vitro metabolism of 1-phenyl-3-aryl-2-propen-1-ones against Plasmodium falciparum. |
| AID1810596 | Antiplasmodial activity against asexual stage of chloroquine-sensitive Plasmodium falciparum D6 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | |||
| AID609328 | Antimalarial activity against chloroquine-resistant Plasmodium chabaudi infected in mouse assessed as parasitemia at 10 mg/kg, po administered for 3 consecutive days | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi. |
| AID1892262 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human RBC assessed as reduction in parasite growth after 72 hrs by LDH assay | 2022 | Bioorganic & medicinal chemistry, 07-15, Volume: 66 | New antimalarials identified by a cell-based phenotypic approach: Structure-activity relationships of 2,3,4,9-tetrahydro-1H-β-carboline derivatives possessing a 2-((coumarin-5-yl)oxy)alkanoyl moiety. |
| AID1648008 | Selectivity ratio of IC50 for HEK293 cells to IC50 for antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | A Meroisoprenoid, Heptenolides, and |
| AID319195 | Antimalarial activity against Plasmodium falciparum K1 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles. |
| AID158676 | In vivo antimalarial activity against Plasmodium berghei infected mice (Mus musculus) | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Potent antimalarial febrifugine analogues against the plasmodium malaria parasite. |
| AID159752 | Inhibition of Plasmodium falciparum K1 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker. |
| AID513850 | Antiplasmodial activity against Plasmodium falciparum FCB2 assessed as inhibition of merozoite invasion of human erythrocytes at 1.85 mg/mL after 18 hrs using hydroethidine staining by flow cytometry | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Well-defined regions of the Plasmodium falciparum reticulocyte binding protein homologue 4 mediate interaction with red blood cell membrane. |
| AID272518 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 by pLDH assay | 2006 | Journal of medicinal chemistry, Nov-30, Volume: 49, Issue:24 | Endoperoxide derivatives from marine organisms: 1,2-dioxanes of the plakortin family as novel antimalarial agents. |
| AID1380019 | Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis and antimalarial evaluation of artesunate-polyamine and trioxolane-polyamine conjugates. |
| AID493460 | Inhibition of maize ACC | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15 | Dimeric cyclohexane-1,3-dione oximes inhibit wheat acetyl-CoA carboxylase and show anti-malarial activity. |
| AID611751 | Antimalarial activity against Plasmodium berghei str. ANKA infected in NMRI mouse at 10 mg/kg/day, ip for three days measured on day 4 by Giemsa staining | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Synthesis and antimalarial activity of new heterocyclic hybrids based on chloroquine and thiazolidinone scaffolds. |
| AID1355323 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as reduction in parasitemia at 20 mg/kg, ip administered for 3 consecutive days post infection measured on day 5 post infection relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
| AID423746 | Apparent clearance with respect to bioavailability in human | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. |
| AID576575 | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax. |
| AID1743669 | Antiplasmodial activity against Plasmodium falciparum NF54 erythrocytic stages assessed as parasite growth inhibition preincubated overnight followed by [G-3H]hypoxanthine addition and measured after 24 hrs by liquid scintillation counting method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Palladium-catalysed synthesis of arylnaphthoquinones as antiprotozoal and antimycobacterial agents. |
| AID151350 | In vitro activity against drug-resistant Plasmodium falciparum W2 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Antiplasmodial activity and cytotoxicity of bis-, tris-, and tetraquinolines with linear or cyclic amino linkers. |
| AID1732466 | Antimalarial activity against asexual blood stage of Plasmodium knowlesi YHI assessed as reduction in cell viability after 48 hrs by EtBr staining based flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
| AID519979 | Antimalarial activity against Plasmodium falciparum 3D7 infected in erythrocyte assessed as increase in vesicle content after 8 hrs by immunofluorescence microscopy | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum. |
| AID1231848 | Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID1732335 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBC assessed as reduction in HRP2 level by ELISA | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization. |
| AID511098 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 10 mg/kg, perorally administered through 7% Tween80/3% Ethanol formulation 24 hrs post infection for 3 days measured 96 hrs post infecti | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
| AID1443526 | Antileishmanial activity against axenic amastigote form of Leishmania infantum MHOM/MA/67/ITMAP-263 assessed as parasite growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | New hydrazine and hydrazide quinoxaline 1,4-di-N-oxide derivatives: In silico ADMET, antiplasmodial and antileishmanial activity. |
| AID717065 | Antimalarial activity against schizonts of chloroquine-sensitive Plasmodium berghei ANKA 2.34 after 16 hrs | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Linear and cyclic dipeptides with antimalarial activity. |
| AID553546 | Drug level in malaria patient whole blood on day 14 | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID1408800 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Novel antimalarial chloroquine- and primaquine-quinoxaline 1,4-di-N-oxide hybrids: Design, synthesis, Plasmodium life cycle stage profile, and preliminary toxicity studies. |
| AID411983 | Antimalarial effect as schizonticidal activity against chloroquine-resistant Plasmodium falciparum 3D7 after 40 hrs | 2009 | Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1 | Search for new pharmacophores for antimalarial activity. Part I: synthesis and antimalarial activity of new 2-methyl-6-ureido-4-quinolinamides. |
| AID673344 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as [3H]hypoxanthine incorporation after 24 hrs by scintillation counting | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluation. |
| AID218536 | Inhibition of beta-hematin formation; active | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | In vitro antimalarial activity of a series of cationic 2,2'-bipyridyl- and 1,10-phenanthrolineplatinum(II) benzoylthiourea complexes. |
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| AID195084 | In vitro antiprotozoal activity against Plasmodium falciparum 3D7 infected erythrocytes at 20 uM | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 1. |
| AID1624365 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes measured after 72 hrs Malstat/NBT reagent based assay | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID389361 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum FcB1/Columbia to IC50 for chloroquine-sensitive Plasmodium falciparum FC32 | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: synthesis, and in vitro antimalarial activity. |
| AID1699563 | Selectivity ratio of IC50 for antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 to IC50 for antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and |
| AID406405 | Antiplasmodial activity as reduced parasitaemia at day 5 in Plasmodium vinckei petteri infected CD mice (Mus musculus) at 10 mg/kg/day intraperitoneal dose | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID606929 | Antimalarial activity against GFP-transfected Plasmodium berghei strain ANKA infected in NMRI mouse assessed as reduction in parasitemia at 10 mg/kg/day, ip administered for 4 consecutive days measured 24 hrs after last treatment by FACS analysis relative | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Antimalarial pyrido[1,2-a]benzimidazoles. |
| AID509183 | Inhibition of TLR7-mediated IFN-gamma production in aldrithiol-2-treated HIV1 Ada-stimulated human PBMC at 100 uM after 20 hrs by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID1272448 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBCs after 72 hrs by SYBR Green based parasite proliferation assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes. |
| AID356092 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs | 2003 | Journal of natural products, Jul, Volume: 66, Issue:7 | Antiparasitic alkaloids from Psychotria klugii. |
| AID666734 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as mean survival days of host at 30 mg/kg, po administered as 4 doses | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID1653745 | Antiplasmodial activity against Plasmodium falciparum NF54 measured after 24 hrs in presence of [3H] hypoxanthine by liquid scintillation counter analysis | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives. |
| AID554567 | Antimalarial activity against morfloquine-resistant Plasmodium falciparum TM91C235 assessed as [3H]hypoxanthine incorporation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID1378986 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 after 24 hrs by [G-3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID663059 | Antimalarial activity against Plasmodium berghei KBG173 infected in mouse assessed as decrease in parasitemia at 2.5 mg/kg, iv BID administered on day 3, 4 and 5 post infection measured on day 31 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin. |
| AID703712 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation incubated for 48 hrs prior to [3H]hypoxanthine addition measured after 48 hrs by liqui | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID158550 | In vitro growth inhibition against Plasmodium falciparum | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1 | Effects of bisphosphonates on the growth of Entamoeba histolytica and Plasmodium species in vitro and in vivo. |
| AID270224 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | A chloroquine-like molecule designed to reverse resistance in Plasmodium falciparum. |
| AID606570 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Optimization of 1,2,3,4-tetrahydroacridin-9(10H)-ones as antimalarials utilizing structure-activity and structure-property relationships. |
| AID768461 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as abnormal mitochondria at 1000 uM after 0.5 hrs by MitoTracker Red CMXRos-based fluorescence microscopic analysis relative to untreated con | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID688337 | n-octanol-KCl distribution coefficient, log D of the compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and antiplasmodial activity of new heteroaryl derivatives of 7-chloro-4-aminoquinoline. |
| AID637702 | Antimalarial activity against chloquine- and pyrimethamine-resistant Plasmodium falciparum K1 erythrocytic stage assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anti-protozoal activity of novel dihydropyrrolo[3,4-d][1,2,3]triazoles. |
| AID113170 | In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after subcutaneous administration | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides. |
| AID1426429 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
| AID1771329 | Antimalarial activity against Plasmodium falciparum Dd2 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting met | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials. |
| AID1880218 | Inhibition of autophagy in African green monkey Vero E6 cells assessed as fold increase in accumulation of LC3 puncta in cytoplasm at 10 uM measured after 4 hrs by DAPI staining based immunofluorescent confocal microscopic analysis | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
| AID401066 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected human erythrocytes as [3H]hypoxanthine uptake | 1998 | Journal of natural products, Jun-26, Volume: 61, Issue:6 | Novel quinone methides from Salacia kraussii with in vitro antimalarial activity. |
| AID553553 | Toxicity in malaria patient assessed as vomiting on day 1 after treatment at quartile 3 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID1324384 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by lactate dehydrogenase assay | 2016 | Bioorganic & medicinal chemistry, 12-01, Volume: 24, Issue:23 | Synthesis and antimalarial activity of N-benzylated (N-arylcarbamoyl)alkylphosphonic acid derivatives. |
| AID1810600 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured for 48 hrs by MTT assay | |||
| AID519200 | Antimicrobial activity against slow-growing synchronous Plasmodium vivax by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID543841 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected ICR mouse assessed as survival of mouse at 5 mg/kg/day, po for 4 days measured after 30 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID1858857 | Antimalarial activity against chloroquine resistant Plasmodium falciparum K1 incubated for 72 hrs by SYBR green staining based fluorescence reader method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Antimalarial application of quinones: A recent update. |
| AID469812 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as LDH activity after 72 hrs by malstat reagent method | 2009 | Journal of natural products, Dec, Volume: 72, Issue:12 | Biologically active tetranorditerpenoids from the fungus Sclerotinia homoeocarpa causal agent of dollar spot in turfgrass. |
| AID1462240 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum 3D7 | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | Synthesis of antimalarial amide analogues based on the plant serrulatane diterpenoid 3,7,8-trihydroxyserrulat-14-en-19-oic acid. |
| AID316604 | Antiplasmodial activity as survival against Plasmodium berghei ANKA infection in NMRI mice (Mus musculus) at 10 mg/kg intraperitoneal dose for 4 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity. |
| AID1552376 | Antimalarial activity against Plasmodium vinckei petteri 279BY infected in Swiss mouse assessed as reduction in parasitemia administered once daily via intraperitoneal route starting from day 1 to day 4 post infection measured on day 5 Giemsa staining bas | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Evaluation of amidoxime derivatives as prodrug candidates of potent bis-cationic antimalarials. |
| AID736792 | Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes after 24 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators. |
| AID1360912 | Cell cycle arrest in human KYSE410 cells assessed as accumulation at G1 phase at 5 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry (Rvb = 65.4%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma. |
| AID290013 | Cytotoxicity against MRC5 cells | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4 | Synthesis and antimalarial evaluation of a series of piperazinyl flavones. |
| AID1057258 | Cytotoxicity against human KB cells assessed as cell viability after 24 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers. |
| AID1688337 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1(CQR)Colombia incubated for 48 hrs by classical radioactive microdilution method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID1373909 | Antimalarial activity against chloroquine-susceptible Plasmodium berghei ANKA infected in Balb-C mouse assessed as mean survival days at 10 mg/kg, ip administered once daily for 4 days (Rvb = 8.4 +/- 0.15 day) | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
| AID538997 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds. |
| AID436170 | Antiplasmodial activity against Plasmodium falciparum W2 after 48 hrs | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Semisynthesis and antiplasmodial activity of the quinoline alkaloid aurachin E. |
| AID105690 | Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 8 uM concentration; No toxicity | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID1524712 | Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as increase in IFN-gamma level in spleen at 10 mg/kg, po administered for 4 days measured on day 10 by sandwich ELISA | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | Efficacy of TLR7 agonistic imidazoquinoline as immunochemotherapeutic agent against P. Berghei ANKA infected rodent host. |
| AID1638539 | Antimalarial activity against multidrug-resistant Plasmodium vivax clinical isolates assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | 3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity. |
| AID681130 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID428564 | Inhibition of CYP3A4 | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques. |
| AID1558334 | Antiviral activity against Zika virus MR 766 infected in HBMEC measured 5 days post infection by CellTiter Blue assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Drugs for the Treatment of Zika Virus Infection. |
| AID151196 | Antiparasitic activity against Plasmodium falciparum | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy. |
| AID558828 | Antimalarial activity against Plasmodium falciparum D6 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID1732475 | Antimalarial activity against Plasmodium falciparum NF54 late stage (1 to 3) expressing Pfs16-LUC-GFP assessed as growth inhibition at 20 uM by high content imaging assay relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
| AID545365 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro. |
| AID1204127 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as inhibition of parasitemia at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 7 post infection relative to | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1732393 | Antimalarial activity against Plasmodium falciparum W2 by parasite lactate dehydrogenase assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity. |
| AID768182 | Binding affinity to mu-oxodimericheme (unknown origin) in phosphate buffer at pH 5.8 at 1 to 25 uM by UV-visible spectrophotometry | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID502042 | Antimicrobial activity against epimastigotes form of Trypanosoma cruzi MHOM/MX/1994/Ninoa after 72 hrs | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas. |
| AID564291 | Antimalarial activity against Plasmodium falciparum 106/1 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID461599 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss Webster mice (Mus musculus) assessed as average parasitaemia at 200 mg/kg, perorally administered 1 day after infection measured after 5 days post infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID1433122 | Antimalarial activity against chloroquine-sensitive asexual intraerythrocytic stage of Plasmodium falciparum NF54 assessed as inhibition of parasite growth by lactate dehydrogenase assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID427287 | Antiplasmodial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum W2 in human erythrocytes by [3H]hypoxanthine uptake | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents. |
| AID1771305 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocyte assessed as intraerythrocytic growth inhibition incubated for 72 hrs by DAPI-staining based imaging analysis | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials. |
| AID419756 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
| AID410197 | Antimalarial activity after 72hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents. |
| AID272311 | Transcription of plasmid pGL3-CV upto 2.5 mM relative to control | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID1391503 | Inhibition of falcipain-2 in chloroquine resistant Plasmodium falciparum RKL9 schizont stage infected in human erythrocytes assessed as reduction in bacterial growth after 24 hrs by Giemsa staining based assay | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | Designing novel inhibitors against falcipain-2 of Plasmodium falciparum. |
| AID1457220 | Antimalarial activity against intraerythrocytic stage of Plasmodium falciparum assessed as parasite reduction ratio at 10 times IC50 preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID518558 | Toxicity in NMRI mice (Mus musculus) infected with Plasmodium berghei ANKA at 3 times 30 mg/kg, perorally measured up to 30 days postinfection | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. |
| AID1628532 | Antimalarial activity against CQ-sensitive Plasmodium falciparum D10 infected in human type O+ erythrocytes assessed as growth inhibition incubated for 48 hrs by LDH assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
| AID1368007 | Inhibition of bovine liver DHFR using FH2 as substrate preincubated for 2 mins followed by substrate addition | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Ionic liquid mediated stereoselective synthesis of alanine linked hybrid quinazoline-4(3H)-one derivatives perturbing the malarial reductase activity in folate pathway. |
| AID1779692 | Antiplasmodial activity against chloroquine-sensitive synchronized Plasmodium falciparum NF54 late trophozoite stage assessed as reduction in parasite survival incubated for 72 hrs under hypoxic condition by parasite lactate dehydrogenase based NBT microp | |||
| AID644368 | Antiprotozoal activity against erythrocytic stages chloroquine- and pyrimethamine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation pre-incubated for 48 hrs prior [3H]hypoxanthine addition measured after 24 hrs by | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis and antimalarial and antituberculosis activities of a series of natural and unnatural 4-methoxy-6-styryl-pyran-2-ones, dihydro analogues and photo-dimers. |
| AID647316 | Resistance index, ratio of IC50 for ring stage chloroquine-resistant Plasmodium falciparum INDO to IC50 for ring stage chloroquine-sensitive Plasmodium falciparum 3D7 | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Stilbene-chalcone hybrids: design, synthesis, and evaluation as a new class of antimalarial scaffolds that trigger cell death through stage specific apoptosis. |
| AID237474 | Percentage of drug bound in bovine plasma albumin | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16 | Contribution of ionization and lipophilicity to drug binding to albumin: a preliminary step toward biodistribution prediction. |
| AID740868 | Selectivity index, ratio of IC50 for human MCR5 cells to IC50 for Plasmodium falciparum K1 | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8 | Borrelidin analogues with antimalarial activity: design, synthesis and biological evaluation against Plasmodium falciparum parasites. |
| AID1548931 | Inhibition of autophagy in human MV4-11 cells assessed as LC3-II degradation at 5 uM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID412370 | Cytotoxicity against human KB cells by MTT assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID1810601 | Therapeutic index, ratio of IC50 for cytotoxicity against human HepG2 cells to IC50 for antiplasmodial activity against asexual blood stage of multidrug-resistant Plasmodium falciparum D6 infected in human erythrocytes | |||
| AID1169353 | Cytotoxicity against human Raji cells | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
| AID1524684 | Toxicity in Laca mouse infected with Plasmodium berghei ANKA assessed as death at 10 mg/kg, po administered for 4 days measured after 21 days | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | Efficacy of TLR7 agonistic imidazoquinoline as immunochemotherapeutic agent against P. Berghei ANKA infected rodent host. |
| AID537142 | Antimalarial activity against chloroquine-susceptible Plasmodium falciparum 3D7 infected in human A+ RBC assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs by scintillation counting | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | Synthesis and antimalarial activities of rhenium bioorganometallics based on the 4-aminoquinoline structure. |
| AID683371 | Cytotoxicity against pig LLC-PK11 cells up to 60 uM after 48 hrs by neutral red assay | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity. |
| AID354687 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 as [3H]hypoxanthine uptake | 1996 | Journal of natural products, Jun, Volume: 59, Issue:6 | Costaricine, a new antiplasmodial bisbenzylisoquinoline alkaloid from Nectandra salicifolia trunk bark. |
| AID544092 | Antimalarial activity against drug-resistant Plasmodium falciparum TM91C235 | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors. |
| AID1353878 | Binding affinity to monomeric heme at pH 7.4 by titration-based UV-vis spectrophotometric analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. |
| AID336324 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Indochina W2 after 24 to 60 hrs by [G-H3]hypoxanthine uptake | 1993 | Journal of natural products, Nov, Volume: 56, Issue:11 | A new antimalarial quassinoid from Simaba guianensis. |
| AID444052 | Hepatic clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID1439514 | Inhibition of bovine liver DHFR using FH2 as substrate preincubated for 2 mins followed by substrate addition in presence of NADPH | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Novel 2,3-disubstituted quinazoline-4(3H)-one molecules derived from amino acid linked sulphonamide as a potent malarial antifolates for DHFR inhibition. |
| AID355964 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Antimicrobial and antiparasitic (+)-trans-hexahydrodibenzopyrans and analogues from Machaerium multiflorum. |
| AID1195270 | Antimalarial activity against chloroquine and mefloquine-resistant Plasmodium falciparum Dd2 after 48 hrs by SYBR Green I assay | 2015 | Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10 | Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues. |
| AID1432054 | Anti-parasitic activity against CQ-resistant Plasmodium falciparum W2 assessed as growth inhibition by measuring increase in LDH release after 72 hrs by spectrophotometric method | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Accepting the Invitation to Open Innovation in Malaria Drug Discovery: Synthesis, Biological Evaluation, and Investigation on the Structure-Activity Relationships of Benzo[b]thiophene-2-carboxamides as Antimalarial Agents. |
| AID1439855 | Antiplasmodial activity against erythrocytic stage of GFP-fused Plasmodium berghei ANKA infected in NMRI mouse assessed as reduction in parasitaemia at 10 mg/kg, ip for 4 days measured at 24 hrs post last dose FACS analysis relative to control | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity. |
| AID1443734 | Binding affinity to haematin assessed as inhibition of NP40-mediated beta-haematin formation after 4 hrs by pyridine-ferrochrome method | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Docking, synthesis and antimalarial activity of novel 4-anilinoquinoline derivatives. |
| AID1433555 | Induction of autophagy in human HeLa cells assessed as effect on ratio of SQSTM1/p62 to actin at 15 uM after 2 hrs by immunoblot method relative to control | 2016 | Journal of natural products, 10-28, Volume: 79, Issue:10 | Chlorotheolides A and B, Spiroketals Generated via Diels-Alder Reactions in the Endophytic Fungus Pestalotiopsis theae. |
| AID1541832 | Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 infected in erythrocytes assessed as reduction in parasite growth incubated for 48 hrs under hypoxic condition by Hoechst 33342 staining based flow cytometry | |||
| AID1236479 | Antiplasmodial activity against asexual intraerythrocytic ring stage of chloroquine-sensitive Plasmodium falciparum 3D7 infected in human O+ erythrocytes assessed as inhibition of parasitic proliferation after 96 hrs by SYBR Green-1 based fluorescence ass | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites. |
| AID451287 | Antiplasmodial activity against Plasmodium yoelii infected in Swiss mice (Mus musculus) erythrocytes assessed as inhibition of beta-hematin formation after 16 hrs by fluorescence assay | 2009 | Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17 | Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity. |
| AID252849 | Resistance index in chloroquine-resistant Plasmodium falciparum K1 (K1 IC50/D10 IC50) | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15 | Application of multi-component reactions to antimalarial drug discovery. Part 1: Parallel synthesis and antiplasmodial activity of new 4-aminoquinoline Ugi adducts. |
| AID390346 | Antiplasmodial activity against Plasmodium falciparum FcB1 as [3H]hypoxanthine uptake after 24 hrs | 2008 | Journal of natural products, Dec, Volume: 71, Issue:12 | Antiplasmodial alkaloids from Desmos rostrata. |
| AID1188439 | Antimalarial activity against tightly synchronized Plasmodium falciparum HB3 assessed as parasite stage accumulation index at late ring stages at 10 uM treated at 18 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytol | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID1359634 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring forms infected in human RBC using compound encapsulated in to immunoliposome targeted to GPA incubated for 15 mins followed by compound removal and further incubation for | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID1404593 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based fluorescence assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Microthecaline A, a Quinoline Serrulatane Alkaloid from the Roots of the Australian Desert Plant Eremophila microtheca. |
| AID436271 | Cytotoxicity against african green monkey Vero cells by MTT assay | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Bioactive diterpenes and other constituents of Croton steenkampianus. |
| AID1304207 | Selectivity index, ratio of IC50 for human WI38 cells to IC50 chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13 | Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities. |
| AID1899008 | Antiplasmodial activity against CQ-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth measured after 48 hrs by SYBR Green 1 dye based fluorescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. |
| AID1437505 | Selectivity index, ratio of growth inhibitory effect against HEK293 cells at 40 uM to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC | |||
| AID1808460 | Modulation of full length human Nur77 expressed in HEK293 cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID522083 | Cmax in women at 450 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID404783 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum GCO3 after 72 hrs by SYBR green assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID573264 | Vacuolar accumulation ratio of the compound at pH 5.2 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID1201523 | Antiplasmodial activity against chloroquine-sensitive Plasmodium berghei NK65 infected in Swiss mouse assessed as reduction in parasitemia at 2.5 mg/kg, ip bid administered for 4 days measured on day 4 by Giemsa staining relative to control | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID1431679 | Cytotoxicity against African green monkey Vero cells after 72 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives, synthesized by thermal and ultrasonic means, are endowed with anti-Zika virus activity. |
| AID1533461 | Antiviral activity against Ebolavirus H. sapiens-wt/1995/Kikwit-9510621 infected in African green monkey Vero cells assessed as inhibition of viral infection pretreated for 2 hrs followed by viral infection and measured after 48 hrs by EboV GP immunostain | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID277605 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore. |
| AID417937 | Cytotoxicity against african green monkey Vero cells up to 16.72 uM after 72 hrs by neutral red assay | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Iodine-catalyzed one-pot synthesis and antimalarial activity evaluation of symmetrically and asymmetrically substituted 3,6-diphenyl[1,2,4,5]tetraoxanes. |
| AID731502 | Cytocidal antimalarial activity against chloroquine/mefloquine-resistant Plasmodium falciparum Dd2 intraerythrocytic stage | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3 | Antiproliferative and antiplasmodial dimeric phloroglucinols from Mallotus oppositifolius from the Madagascar Dry Forest (1). |
| AID504271 | Inhibition of beta-hematin formation assessed as molar equivalents by BHIA assay relative to hemin | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID158877 | In vitro inhibition of parasite development of Plasmodium falciparum W2 in human erythrocytes | 2002 | Bioorganic & medicinal chemistry letters, May-20, Volume: 12, Issue:10 | Synthesis and evaluation of new antimalarial analogues of quinoline alkaloids derived from Cinchona ledgeriana Moens ex Trimen. |
| AID275997 | Antimalarial activity against Plasmodium falciparum D6 | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | In vitro and in vivo efficacy and in vitro metabolism of 1-phenyl-3-aryl-2-propen-1-ones against Plasmodium falciparum. |
| AID404782 | Selectivity for chloroquine-resistant Plasmodium falciparum Dd2 over chloroquine-sensitive Plasmodium falciparum HB3 as IC50 ratio by SYBR green assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID323376 | Growth inhibition of Plasmodium vivax isolate 3 assessed as parasite LDH synthesis after 48 hrs by double-site Plasmodium LDH antigen capture enzyme-linked immunosorbent assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Improved assessment of plasmodium vivax response to antimalarial drugs by a colorimetric double-site plasmodium lactate dehydrogenase antigen capture enzyme-linked immunosorbent assay. |
| AID1162949 | Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides: a new class of antiplasmodial compounds. |
| AID358251 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of natural products, Oct, Volume: 64, Issue:10 | Antimalarial (+)-trans-hexahydrodibenzopyran derivatives from Machaerium multiflorum. |
| AID673144 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as reduction of parasite level in blood at 100 mg/kg, po administered 24 hrs post infection measured after 72 hrs post infection by flow cytometry | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
| AID734082 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis, cytotoxicity and antiplasmodial activity of novel ent-kaurane derivatives. |
| AID1814041 | Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at pH 7 in presence of glucose measured after 48 hrs by visual analysis | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH. |
| AID530577 | Antileishmanial activity against Leishmania infantum promastigotes overexpressing LiABCG6 assessed as cell viability after 72 hrs by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement. |
| AID1188449 | Antimalarial activity against tightly synchronized Plasmodium falciparum W2 assessed as parasite stage accumulation index at trophozoites stages at 10 uM treated at 18 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cyt | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID1688341 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Palo Alto(CQR)Ouganda incubated for 48 hrs by classical radioactive microdilution method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID482877 | Inhibition of Plasmodium falciparum recombinant falcipain-2 expressed in Escherichia coli at 100 uM after 20 min by spectrofluorometry | 2009 | Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18 | On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences. |
| AID1175720 | Antigametocytocidal activity against Plasmodium falciparum NF54-pfs16-GPF early (1 to 3) gametocyte assessed as viability after 72 hrs by MitoTracker Red CM-H2XRos/micro-plate confocal imaging system | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2 | The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs. |
| AID325971 | Antiprotozoal activity against Plasmodium falciparum | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and anti-protozoal activity of C2-substituted polyazamacrocycles. |
| AID768470 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as nonviable parasite at 0.005 uM after 0.5 hrs by SYTO 61 staining-based flow cytometric analysis relative to untreated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1457206 | Antimalarial activity against Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting m | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID619709 | Dissociation constant, pKa of the compound with quinoline heteroaromatic N atom by pH titration method | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). |
| AID442261 | Therapeutic index, ratio of IC50 for concanavalin-stimulated BALB/c mice (Mus musculus) splenocytes to IC50 for Plasmodium falciparum 3D7 | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID1188443 | Antimalarial activity against tightly synchronized Plasmodium falciparum HB3 assessed as parasite stage accumulation index at schizonts stages at 10 uM treated at 30 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytol | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID278817 | Antimalarial activity against Plasmodium falciparum FAC8 | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Synergistic interactions of the antiretroviral protease inhibitors saquinavir and ritonavir with chloroquine and mefloquine against Plasmodium falciparum in vitro. |
| AID361154 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FCB1-R/Colombia by [3H]hypoxanthine uptake | 2002 | Journal of natural products, Oct, Volume: 65, Issue:10 | Antiplasmodial activity of alkaloids from various strychnos species. |
| AID434591 | Resistance factor, ratio of IC50 for Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. |
| AID1714098 | Antiplasmodial activity against Plasmodium berghei ANKA infected in NMRI mouse model assessed as reduction in parasitemia at 30 mg/kg, po qd for 4 consecutive days measured at day 7 post infection by flow cytometry analysis | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle. |
| AID636365 | Antimalarial activity against Plasmodium falciparum PH3 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID259766 | Antimalarial activity against Plasmodium yoelii in Swiss mice (Mus musculus) model at 96 mg/kg peroral dose | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | 8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro (4.5) decane, a new 1,2,4-trioxane effective against rodent and simian malaria. |
| AID402130 | Antimalarial activity as reduced parasitaemia against Plasmodium berghei infected Swiss albino mice (Mus musculus) at 5 mg/kg/day peroral dose for 4 days | 1997 | Journal of natural products, Jul, Volume: 60, Issue:7 | In vitro and in vivo antiplasmodial activity of cryptolepine and related alkaloids from Cryptolepis sanguinolenta. |
| AID730535 | Cytotoxicity against african green monkey Vero C1008 cells after 72 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Synthesis and insight into the structure-activity relationships of chalcones as antimalarial agents. |
| AID451289 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N67 infected in Swiss mice (Mus musculus) assessed as inhibition of parasitaemia at 10 mg/kg, perorally administered for 4 days measured on day 4 post-infection | 2009 | Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17 | Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity. |
| AID530576 | Antileishmanial activity against GFP-tagged at NH2 terminus Leishmania infantum promastigotes overexpressing LiABCG6 assessed as cell viability after 72 hrs by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10 | Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement. |
| AID774913 | Inhibition of beta-hematin formation after overnight incubation by NP-40 detergent-mediated spectroscopic analysis | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Synthesis, characterization, antiparasitic and cytotoxic evaluation of thioureas conjugated to polyamine scaffolds. |
| AID337534 | Selectivity index, ratio of ED50 for human LUC1 cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1764059 | Cytotoxicity against HUVEC cells assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Anti-protozoal and anti-fungal evaluation of 3,5-disubstituted 1,2-dioxolanes. |
| AID274297 | Selectivity index, IC50 for L6 cells/IC50 for chloroquine-sensitive Plasmodium falciparum | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
| AID323671 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum T996 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID402294 | Antimalarial activity against Plasmodium falciparum infected erythrocytes | 2005 | Journal of natural products, Jun, Volume: 68, Issue:6 | Triterpenoid saponin anthranilates from Albizia grandibracteata leaves ingested by primates in Uganda. |
| AID667393 | Inhibition of heme polymerization at 1 mM after 48 hrs by spectrophotometry relative to chloroquine | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Novel cinnamic acid/4-aminoquinoline conjugates bearing non-proteinogenic amino acids: towards the development of potential dual action antimalarials. |
| AID118016 | The compound was tested in vivo antimalarial response against multidrug-resistant Plasmodium yoelii in Swiss mice (Mus musculus) at a dose of 48 (mg/kg/day) after 10 days | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Photo-oxygenation of geraniol: synthesis of a novel series of hydroxy-functionalized anti-malarial 1,2,4-trioxanes. |
| AID1378995 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in human red blood cells assessed as reduction in parasitic LDH activity by Malstat reagent based spectrophotometric method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID117999 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium berghei N. activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4-day test at a concentration of 1 mg/kg in experiment 1 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID1415895 | Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation cou | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening. |
| AID361155 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2/Indochina by [3H]hypoxanthine uptake | 2002 | Journal of natural products, Oct, Volume: 65, Issue:10 | Antiplasmodial activity of alkaloids from various strychnos species. |
| AID1404598 | Cytotoxicity against HEK293 cells assessed as inhibition of cell growth at 10 uM after 72 hrs by alamar blue assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Microthecaline A, a Quinoline Serrulatane Alkaloid from the Roots of the Australian Desert Plant Eremophila microtheca. |
| AID1552379 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum Nigerian infected in human blood after 48 hrs by [3H]-hypoxanthine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Evaluation of amidoxime derivatives as prodrug candidates of potent bis-cationic antimalarials. |
| AID404787 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID1524682 | Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as parasitemia at 10 mg/kg, po administered for 4 days measured on day 17 by Giemsa-staining based assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | Efficacy of TLR7 agonistic imidazoquinoline as immunochemotherapeutic agent against P. Berghei ANKA infected rodent host. |
| AID247058 | Effective dose against chloroquine-resistant, pyrimethamine-resistant, mefloquine-sensitive Plasmodium falciparum K1 | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID1391091 | Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 42 residues) production measured after 24 hrs by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | New phenylaniline derivatives as modulators of amyloid protein precursor metabolism. |
| AID1649905 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Triazole derivatives and their antiplasmodial and antimalarial activities. |
| AID515065 | Antiplasmodial activity against synchronized chloroquine-resistant Plasmodium falciparum Dd2 infected in NMRI mice (Mus musculus) RBC assessed as inhibition of hemozoin formation at 1000 nM after 24 hrs by colorimetric analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID1168875 | Selectivity index, ratio of CC50 for HMEC1 to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID151990 | Inhibitory activity against chloroquine-resistant Plasmodium falciparum FcB1R | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID337526 | Cytotoxicity against mouse P388 cells after 2 days by sulforhodamine B assay | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID748433 | Antiplasmodial activity against erythrocytic stage of Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6 | New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi. |
| AID1515767 | Antimalarial activity against synchronized ring stage Plasmodium falciparum 3D7 transfected with nano-luciferase assessed as parasite growth inhibition after 72 hrs by Nano-Glo luciferase assay | 2019 | MedChemComm, Sep-01, Volume: 10, Issue:9 | Repositioning Salirasib as a new antimalarial agent. |
| AID725847 | Inhibition of Escherichia coli recombinant DXR using DXP as substrate preincubated for 5 mins | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Antimalarial and Structural Studies of Pyridine-containing Inhibitors of 1-Deoxyxylulose-5-phosphate Reductoisomerase. |
| AID1571717 | Inhibition of beta-hematin formation assessed as reduction in hemozoin formation incubated for 5 hrs by NP40 detergent-based assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles. |
| AID753996 | Antimalarial activity against chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 infected in human red blood cells assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Synthesis and antimalarial testing of neocryptolepine analogues: addition of ester function in SAR study of 2,11-disubstituted indolo[2,3-b]quinolines. |
| AID1191210 | Antimicrobial activity against Plasmodium falciparum Dd2 | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Reemergence of chloroquine (CQ) analogs as multi-targeting antimalarial agents: a review. |
| AID1059804 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12 | Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
| AID1688340 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2(CQR)Indo-China incubated for 48 hrs by classical radioactive microdilution method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID482883 | Antiplasmodial activity against Plasmodium falciparum W2 by fluorometric method | 2009 | Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18 | On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences. |
| AID1732468 | Antimalarial activity against asexual blood stage of Mefloquine-resistant Plasmodium falciparum W2mef assessed as reduction in cell viability after 72 hrs by EtBr staining based flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
| AID377698 | Antileishmanial activity against Leishmania donovani after 72 hrs by alamar blue assay | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID257593 | Antimalarial activity as reduced schizont maturation against chloroquine-sensitive Plasmodium falciparum FDL-B after 24 hrs | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Anti-malarial activity of Baylis-Hillman adducts from substituted 2-chloronicotinaldehydes. |
| AID284269 | Antimalarial activity against Plasmodium falciparum D6 | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID576507 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay. |
| AID407854 | Cytotoxicity against mouse FM3A cells assessed as inhibition of increase in cell density after 48 hrs | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Pyridinium cationic-dimer antimalarials, unlike chloroquine, act selectively between the schizont stage and the ring stage of Plasmodium falciparum. |
| AID453258 | Toxicity against rat L6 cells | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues. |
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| AID346872 | Binding affinity to heme in 20 mM CTAB surfactant assessed as equilibrium constant by UV-visible spectrophotometry | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
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| AID1585806 | Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 asynchronous cultures infected in human erythrocytes | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis of isatin based N |
| AID1457222 | Antimalarial activity against intraerythrocytic stage of Plasmodium falciparum assessed as time required to clear 99.9% of initial parasite population at 10 times IC50 preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
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| AID760220 | Cytotoxicity against human KB cells after 72 hrs by Alamar blue assay | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids. |
| AID268407 | Antimalarial activity against Plasmodium falciparum W2 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Probing the role of the covalent linkage of ferrocene into a chloroquine template. |
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| AID298581 | Antimalarial activity against Plasmodium falciparum TM91C235 | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1). |
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| AID480221 | Mutagenic activity in Salmonella Typhimurium TA98 assessed as number of revertants after 48 hrs by Ames test | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
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| AID157850 | Growth inhibition of chloroquine-sensitive Plasmodium falciparum D10 | 2001 | Bioorganic & medicinal chemistry letters, Aug-20, Volume: 11, Issue:16 | Synthesis, antimalarial activity and inhibition of haem detoxification of novel bisquinolines. |
| AID1717743 | Selectivity index, ratio of CC50 for human Huh-7 cells to EC50 for HCoV-229E harboring GFP infected in human Huh-7 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
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| AID356098 | Cytotoxicity against african green monkey Vero cells at 10 ug/ml | 2003 | Journal of natural products, Jul, Volume: 66, Issue:7 | Antiparasitic alkaloids from Psychotria klugii. |
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| AID1409610 | Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
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| AID330907 | Displacement of quinaldine red from human AAG by fluorescence method | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein. |
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| AID400312 | Cytotoxicity against human SKOV3 cells after 2 to 7 days by neutral red assay | 1996 | Journal of natural products, Jan, Volume: 59, Issue:1 | A new quassinoid from Castela texana. |
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| AID1733524 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Identification of two novel thiophene analogues as inducers of autophagy mediated cell death in breast cancer cells. |
| AID1174541 | Binding affinity to monomeric heme (unknown origin) assessed as binding constant at pH 7.4 | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | 4-Aminoquinoline-pyrimidine hybrids: synthesis, antimalarial activity, heme binding and docking studies. |
| AID1288232 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as inhibition of parasite growth after 48 hrs by parasite lactate dehydrogenase assay | 2016 | European journal of medicinal chemistry, May-23, Volume: 114 | Indolyl-3-ethanone-α-thioethers: A promising new class of non-toxic antimalarial agents. |
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| AID625277 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
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| AID211647 | Compound was evaluated for toxicity on Human kidney epithelial (Graham cells) at a dose of 100 ug/mL; Not toxic | 2002 | Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16 | Antimalarial compounds from Parinari capensis. |
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| AID644262 | Cytotoxicity against human NFF assessed as growth inhibition after 3 days by sulforhodamine B assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis and antiplasmodial evaluation of novel chromeno[2,3-b]chromene derivatives. |
| AID1265979 | Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and bio-evaluation of novel quinolino-stilbene derivatives as potential anticancer agents. |
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| AID1143192 | Water-lipid distribution coefficient, log D of the compound at pH 5.2 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity. |
| AID1179402 | Association constant, log K of the compound in aqueous DMSO at pH 7.5 assessed as complex formation by UV spectrophotometry | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Antiplasmodial activity of new 4-aminoquinoline derivatives against chloroquine resistant strain. |
| AID565416 | Antimalarial activity against Plasmodium falciparum PfV1S0176/N10 infected in immunodeficient HM-IL2Rgamma null mouse after 7 days | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rgammanull mice engrafted with human erythrocytes. |
| AID418747 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
| AID442353 | Selectivity index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for human K562 cells | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Original quinazoline derivatives displaying antiplasmodial properties. |
| AID580699 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of schizont stage parasite growth at IC50 after 6 hr by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID1204131 | Toxicity in Plasmodium berghei NK65 infected Swiss albino mouse assessed as mouse survival at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 7 post infection relative to untreated control | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID343600 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM6 in human erythrocytes by [3H]hypoxanthine uptake | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors. |
| AID768458 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as abnormal mitochondria at 0.005 uM after 0.5 hrs by MitoTracker Red CMXRos-based fluorescence microscopic analysis relative to untreated co | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1894308 | Inhibition of Beta-hematin assessed as bis-pyridyl-Fe(III)PPIX complex formation incubated for 5 hrs by NP40 detergent-mediated colorimetric assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID404786 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 by [3H]hypoxanthine uptake | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID1204118 | Cytotoxic activity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID666488 | Selectivity ratio of IC50 for human HepG2 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7A | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
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| AID586609 | Antimalarial activity against ring stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. |
| AID343750 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 as LDH activity | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Novel amodiaquine congeners as potent antimalarial agents. |
| AID421653 | Antiplasmodial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum W2 infected human erythrocytes by [3H]hypoxanthine uptake | 2009 | Journal of natural products, Feb-27, Volume: 72, Issue:2 | Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity. |
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| AID659132 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected Swiss mouse assessed as suppression of parasitemia at 20 mg/kg/day, po qd for 4 days measured on day 6 | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Antiplasmodial activity of novel keto-enamine chalcone-chloroquine based hybrid pharmacophores. |
| AID774916 | Antiplasmodial activity against chloroquine-sensitive erythrocyte stages of Plasmodium falciparum NF54 by parasite lactate dehydrogenase assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Synthesis, characterization, antiparasitic and cytotoxic evaluation of thioureas conjugated to polyamine scaffolds. |
| AID334844 | Selectivity index, ratio of ED50 for human KB cells to ED50 for Plasmodium falciparum D6 | 1993 | Journal of natural products, Aug, Volume: 56, Issue:8 | Cytotoxic and antimalarial alkaloids from the bulbs of Crinum amabile. |
| AID1667185 | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Synthesis and efficacy of pyrvinium-inspired analogs against tuberculosis and malaria pathogens. |
| AID318212 | Cytotoxicity against human KB cells by MTT assay | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
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| AID625398 | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3. |
| AID378979 | Antimalarial activity after 48 hrs against Plasmodium falciparum D6 by [3H]hypoxanthine uptake | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | Lupeol long-chain fatty acid esters with antimalarial activity from Holarrhena floribunda. |
| AID1530047 | Antimalarial activity against Plasmodium yoelii nigeriensis infected in mouse | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Quinoline and quinolone dimers and their biological activities: An overview. |
| AID323375 | Growth inhibition of Plasmodium vivax isolate 2 assessed as parasite LDH synthesis after 48 hrs by double-site Plasmodium LDH antigen capture enzyme-linked immunosorbent assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Improved assessment of plasmodium vivax response to antimalarial drugs by a colorimetric double-site plasmodium lactate dehydrogenase antigen capture enzyme-linked immunosorbent assay. |
| AID390619 | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | New chimeric antimalarials with 4-aminoquinoline moiety linked to a tetraoxane skeleton. |
| AID458585 | Cytotoxicity against human MDA-MB-468 cells after 48 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4 | Design and synthesis of anti-breast cancer agents from 4-piperazinylquinoline: a hybrid pharmacophore approach. |
| AID1829856 | Cytotoxicity against human HEK293 cells assessed as cell viability measured for 24 hrs by MTT assay | |||
| AID636366 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID152139 | In vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2003 | Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23 | Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials. |
| AID1808466 | Modulation of full length human NOR1 expressed in HEK293T cells co-transfected with with RXRalpha luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter gene assa | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID457732 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum MRC-02 in human B+ erythrocytes assessed as inhibition of schizont maturation after 24 hrs by conventional parasite culture method | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Gomphostenins: two new antimalarial compounds from the leaves of Gomphostemma niveum. |
| AID1433157 | Binding affinity to monomeric heme (unknown origin) assessed as association constant at pH 5.6 by UV-visible absorption spectrophotometry | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID477938 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum D6 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID284263 | Antibacterial activity against methicillin-resistant Staphylococcus aureus | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID673594 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcM29 assessed as [3H]hypoxanthine incorporation after 48 hrs | 2012 | Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15 | Short synthesis and antimalarial activity of fagaronine. |
| AID700948 | Antiplasmodial activity against Plasmodium falciparum assessed as pyknotic phenotype after 24 hrs by Giemsa-staining method | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5 | A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. |
| AID434595 | Antimalarial activity as mean survival time against Plasmodium yoelii N67 infected Swiss mice (Mus musculus) | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. |
| AID461348 | Cytotoxicity against african green monkey Vero cells after 48 hrs by neutral red assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID157863 | In vitro inhibitory activity against Plasmodium falciparum | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14 | Design, synthesis, and biological evaluation of a series of simple and novel potential antimalarial compounds. |
| AID1808456 | Modulation of full length human NOR1 expressed in SK-N-BE(2) cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID740867 | Selectivity index, ratio of IC50 for human MCR5 cells to IC50 for Plasmodium falciparum FCR-3 | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8 | Borrelidin analogues with antimalarial activity: design, synthesis and biological evaluation against Plasmodium falciparum parasites. |
| AID1166277 | Antimalarial activity against Plasmodium falciparum FCR3 after 48 hrs by parasite lactate dehydrogenase assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Preparation and antimalarial activity of a novel class of carbohydrate-derived, fused thiochromans. |
| AID346864 | Binding affinity to heme in DMSO assessed as equilibrium constant by UV-visible spectrophotometry | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID449198 | Antimalarial activity against Plasmodium falciparum W2mef ring form by hoechst 33342-thiazole orange stain based flow cytometry assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials. |
| AID1433152 | Cytotoxicity against MDCK cells assessed as alteration of normal cell morphology by microscopic analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID256080 | Antiplasmodial activity for Plasmodium falciparum F32 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities. |
| AID336446 | Antileishmanial activity against Leishmania donovani (MHOM/ET/67/L82) promastigotes | 2002 | Journal of natural products, Oct, Volume: 65, Issue:10 | Assessment of the antiprotozoal activity of Galphimia glauca and the isolation of new nor-secofriedelanes and nor-friedelanes. |
| AID762745 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as inhibition of parasitemia at 10 mg/kg, po qd for 4 days measured on day 5 to 7 of after infection relative to control | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16 | In vivo antimalarial activity of novel 2-hydroxy-3-anilino-1,4-naphthoquinones obtained by epoxide ring-opening reaction. |
| AID1473366 | Antimalarial activity against erythrocyte stage of Plasmodium falciparum 3D7 preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1239629 | Antiplasmodial activity against CQ-sensitive Plasmodium falciparum D6 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Quinoline-based antimalarial hybrid compounds. |
| AID509191 | Inhibition of TLR7/TLR9-mediated upregulation of indoleamine 2,3-dioxygenase expression in aldrithiol-2-treated HIV1 Ada-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID513851 | Antiplasmodial activity against Plasmodium falciparum FCB2 assessed as inhibition of merozoite invasion of human erythrocytes at 0.93 mg/mL after 18 hrs using hydroethidine staining by flow cytometry | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Well-defined regions of the Plasmodium falciparum reticulocyte binding protein homologue 4 mediate interaction with red blood cell membrane. |
| AID522086 | Cmax in Papua new Guinean pregnant women at 750 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID337523 | Cytotoxicity against human Col1 cells after 3 days by sulforhodamine B assay | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID425020 | Antiplasmodial activity against Plasmodium falciparum D6 | 2009 | Journal of natural products, May-22, Volume: 72, Issue:5 | Biologically active cannabinoids from high-potency Cannabis sativa. |
| AID607060 | Antimalarial activity against Plasmodium falciparum HB3 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Antimalarial pyrido[1,2-a]benzimidazoles. |
| AID235325 | Selectivity ratio of cytotoxicity against FM3A cells to antimalarial activity against Plasmodium falciparum FCR3 | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Potent antimalarial febrifugine analogues against the plasmodium malaria parasite. |
| AID576511 | Antiplasmodial activity against Plasmodium falciparum 3D7 by SYBR Green 1-based fluorescence assay | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay. |
| AID323680 | Reduction of [3H]chloroquine uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID504259 | Lipid accumulation ratio of the compound at pH 7.4 | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID72977 | Ability to associate with ferriprotoporphyrin IX | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | In vitro antimalarial activity of a series of cationic 2,2'-bipyridyl- and 1,10-phenanthrolineplatinum(II) benzoylthiourea complexes. |
| AID1487408 | Antiplasmodial activity against chloroquine-resistant erythrocyte stage of Plasmodium falciparum FcM29-Cameroon infected in human RBC assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition mea | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16 | Structure-activity relationship studies on thiaplidiaquinones A and B as novel inhibitors of Plasmodium falciparum and farnesyltransferase. |
| AID1885207 | Agonist activity at Nurr1 ligand binding domain (unknown origin) measured by Gal4-based reporter gene assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Medicinal Chemistry and Chemical Biology of Nurr1 Modulators: An Emerging Strategy in Neurodegeneration. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID275996 | Antimalarial activity against Plasmodium falciparum W2 | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | In vitro and in vivo efficacy and in vitro metabolism of 1-phenyl-3-aryl-2-propen-1-ones against Plasmodium falciparum. |
| AID1196101 | Antiplasmodial activity against chloroquine-sensitive asexual erythrocytic stage of Plasmodium falciparum NF54 assessed as [3H]-hypoxanthine incorporation by lactate dehydrogenase assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Synthesis of functionalized 3-, 5-, 6- and 8-aminoquinolines via intermediate (3-pyrrolin-1-yl)- and (2-oxopyrrolidin-1-yl)quinolines and evaluation of their antiplasmodial and antifungal activity. |
| AID768488 | Resistant index, ratio of IC50 for Plasmodium falciparum K1 to IC50 for Plasmodium falciparum 3D7 | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID461346 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 after 72 hrs by LDH assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID1699657 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability at 4 uM after 72 hrs by resazurin dye based assay relative to control | 2020 | Journal of natural products, 11-25, Volume: 83, Issue:11 | Antiplasmodial Alkaloids from the Australian Bryozoan |
| AID317957 | Antiparasitic activity against chloroquine-resistant Plasmodium falciparum K1 | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum. |
| AID499813 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum W2 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
| AID1161928 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human O positive erythrocyte after 72 hrs | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18 | Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax. |
| AID1426428 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
| AID1533486 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as mortality up to 120 hrs post fertilization | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1849759 | Antimalarial activity against multidrug resistant Plasmodium falciparum Dd2 incubated for 72 hrs by malaria SYBR green I nucleic acid staining dye based fluorescence assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
| AID378977 | Antimalarial activity after 48 hrs against Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2006 | Journal of natural products, Jan, Volume: 69, Issue:1 | Lupeol long-chain fatty acid esters with antimalarial activity from Holarrhena floribunda. |
| AID1433133 | Cytotoxicity against african green monkey Vero cells assessed as alteration of normal cell morphology by microscopic analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID1593289 | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials. |
| AID1168867 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID1542990 | Selectivity index, ratio of IC50 for human HMEC1 cells to IC50 for antimalarial activity against CQ-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Covalent Inhibitors of |
| AID1858890 | In vivo antiplasmodial activity against Plasmodium berghei ANKA infected in CD-1 mouse assessed as decrease in parasitaemia at 50 mg/kg, ip measured after 4 days relative to control | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Antimalarial application of quinones: A recent update. |
| AID1181515 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in erythrocytes assessed as [3H]hypoxanthine incorporation after 24 hrs by microbeta scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Kojic acid derived hydroxypyridinone-chloroquine hybrids: synthesis, crystal structure, antiplasmodial activity and β-haematin inhibition. |
| AID564233 | Antiplasmodial activity against Plasmodium falciparum harboring wild type pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID1125280 | Antimicrobial activity against blood-stage Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP). |
| AID118003 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS. activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4-day test at a concentration of 10 mg/kg in experiment 2 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID636373 | Antimalarial activity against blood stage of Plasmodium berghei NK65 infected in po dosed rat assessed as inhibition of parasite growth | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Febrifugine analogue compounds: synthesis and antimalarial evaluation. |
| AID1272515 | Antiplasmodial activity against chloroquine, quinine and pyrimethamine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs by liquid scintillation counting analysis | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | In vitro efficacy of 2,N-bisarylated 2-ethoxyacetamides against Plasmodium falciparum. |
| AID1899028 | Antiplasmodial activity CQ-resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite growth measured after 72 hrs by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. |
| AID1574649 | Growth inhibition of HEK293 cells at 40 uM after 72 hrs by resazurin dye based assay relative to control | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases. |
| AID1906561 | Induction of autophagy in human SCC-4 cells assessed as increase in LC3-II to LC3-I ratio at 10 uM in absence of EBSS measured after 3 hrs by Western blot analysis | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Design and synthesis of multifunctional microtubule targeting agents endowed with dual pro-apoptotic and anti-autophagic efficacy. |
| AID406711 | Toxicity in Plasmodium vinckei petteri infected CD mice (Mus musculus) assessed as mortality at 10 mg/kg/day, intraperitoneally measured on day 5 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID1682558 | Selectivity index, ratio of CC50 for African green monkey Vero cells infected with SARS-CoV-2 betaCoV/KOR/KCDC03/2020 to IC50 for SARS-CoV-2 betaCoV/KOR/KCDC03/2020 | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Discovery of cyclic sulfonamide derivatives as potent inhibitors of SARS-CoV-2. |
| AID723298 | Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents. |
| AID219087 | Association constant with ferriprotoporphyrin IX. | 2000 | Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2 | Structure-function relationships in aminoquinolines: effect of amino and chloro groups on quinoline-hematin complex formation, inhibition of beta-hematin formation, and antiplasmodial activity. |
| AID479151 | Antiplasmodial activity against Plasmodium falciparum FCB2 assessed as inhibition of merozoite invasion of human RBCs at 1.85 mg/mL after 18 hrs using hydroethidine staining by flow cytometry | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Conserved high activity binding peptides are involved in adhesion of two detergent-resistant membrane-associated merozoite proteins to red blood cells during invasion. |
| AID304044 | Antiplasmodial activity against Plasmodium falciparum in human red blood cells after 4 hrs | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Synthesis and pharmacological evaluation of fluorescent and photoactivatable analogues of antiplasmodial naphthylisoquinolines. |
| AID600090 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition. |
| AID351889 | Antimalarial activity after 72 hrs against chloroquine-resistant transporter 106/1'76T mutant Plasmodium falciparum infected human erythrocytes by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
| AID480232 | Inhibition of CYP2C9 in human liver microsomes assessed as metabolite produced at 10 uM by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID366982 | Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for chloroquine-resistant Plasmodium falciparum FcB1R/Colombia | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline. |
| AID1518839 | Resistance ratio of IC50 for antimalarial activity against ring stage Plasmodium falciparum K1 to IC50 for antimalarial activity against ring stage Plasmodium falciparum 3D7 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
| AID619713 | Antimalarial activity against erythrocyte stages of chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes by lactate dehydrogenase assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). |
| AID683353 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as suppression in parasitemia at 100 mg/kg, po administered QD for 3 days measured on day 7 relative to control | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity. |
| AID564294 | Antimalarial activity against Plasmodium falciparum IMT A4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID619712 | Antimalarial activity against erythrocyte stages of chloroquine-sensitive Plasmodium falciparum D10 infected in human erythrocytes by lactate dehydrogenase assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT). |
| AID1636114 | Inhibition of beta-haematin formation after 12 to 14 hrs by microplate assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials. |
| AID1204116 | Cytotoxic activity against human HeLa cells assessed as cell viability at 0.1 ug/ml incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1437632 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2017 | Journal of natural products, 01-27, Volume: 80, Issue:1 | Octaminomycins A and B, Cyclic Octadepsipeptides Active against Plasmodium falciparum. |
| AID1188438 | Antimalarial activity against tightly synchronized Plasmodium falciparum HB3 assessed as parasite stage accumulation index at schizonts stages at 10 uM treated at 6 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytolo | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID1155447 | Antiplasmodial activity against Plasmodium berghei ANKA expressing GFP infected in BALB/c mouse assessed as host survival days at 30 mg/kg, po qd for 4 days | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Aminoazabenzimidazoles, a novel class of orally active antimalarial agents. |
| AID667437 | Antiplasmodial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as decrease in parasitemia measured on day 1 post-treatment by geimsa staining (Rvb = 0.65 +/- 02%) | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain. |
| AID659134 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected Swiss mouse assessed as suppression of parasitemia at 10 mg/kg/day, po qd for 4 days measured on day 6 | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Antiplasmodial activity of novel keto-enamine chalcone-chloroquine based hybrid pharmacophores. |
| AID1188914 | Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR Green fluorescence assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents. |
| AID1167555 | Cytotoxicity against human HepG2 cells incubated for 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | New series of monoamidoxime derivatives displaying versatile antiparasitic activity. |
| AID549610 | Resistance index, ratio of IC50 for Plasmodium falciparum multidrug-resistant TM91C235 to IC50 for mefloquine-resistant, chloroquine-sensitive Plasmodium falciparum D6 | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones. |
| AID406404 | Toxicity in Plasmodium vinckei petteri infected CD mice (Mus musculus) assessed as mortality at 1 mg/kg/day, intraperitoneally measured on day 15 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID334845 | Selectivity index, ratio of ED50 for human KB cells to ED50 for Plasmodium falciparum W2 | 1993 | Journal of natural products, Aug, Volume: 56, Issue:8 | Cytotoxic and antimalarial alkaloids from the bulbs of Crinum amabile. |
| AID441597 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as inhibition of schizont maturation at 0.50 ug/ml after 36-40 hrs relative to control | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Synthesis of new chalcone derivatives containing acridinyl moiety with potential antimalarial activity. |
| AID1518827 | Antimalarial activity against ring stage Plasmodium falciparum 3D7 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
| AID700786 | Antiplasmodial activity against Plasmodium falciparum Dd2 assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to [3H]hypoxanthine addition measured after 24 hrs by beta scintillation counting | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5 | A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. |
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| AID1405800 | Induction of autophagy in human HeLa cells assessed as increase in LC3-2 to LC3-1 ratio at 50 uM after 6 hrs by immunoblot analysis relative to control | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
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| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
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| AID1880207 | Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero E6 cells to EC50 for antiviral activity against SARS-CoV-2 infected in eGFP expressing African green monkey Vero E6 cells | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
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| AID780246 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 to 72 hrs by SYBR green-1 assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | New route to the 5-((arylthio- and heteroarylthio)methylene)-3-(2,2,2-trifluoroethyl)-furan-2(5H)-ones--key intermediates in the synthesis of 4-aminoquinoline γ-lactams as potent antimalarial compounds. |
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| AID1530565 | Antiplasmodial activity against asynchronous form of Plasmodium falciparum W2 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
| AID1238799 | Antiplasmodial activity against chloroquine and sulfadoxine-resistant and mefloquine-sensitive Plasmodium falciparum W2 infected in human erythrocytes by anti-HRP2 assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Anti-Plasmodium falciparum activity of quinoline-sulfonamide hybrids. |
| AID1538875 | Antiplasmodial activity against Plasmodium falciparum infected in human RBC assessed as reduction in virus-induced cytopathicity by MTT assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway. |
| AID1883297 | Selectivity index, ratio of IC50 for cytotoxicity against human MRC5 cells to IC50 for antimalarial activity against chloroquine-resistant Plasmodium falciparum FCR3 | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Sattahipmycin, a Hexacyclic Xanthone Produced by a Marine-Derived |
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| AID1555162 | Antimalarial activity against Plasmodium berghei ANKA infected in specific pathogen-free C57BL/6 mouse assessed as reduction in disease severity at 100 mg/kg, po administered once daily for 4 days measured up to 35 days post-infection by rapid staining-ba | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials. |
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| AID1555161 | Antimalarial activity against Plasmodium berghei ANKA infected in specific pathogen-free C57BL/6 mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily for 4 days measured up to 35 days post-infection by rapid staining-based m | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials. |
| AID446182 | Inhibition of beta-hematin formation assessed as biocrystallization by UV-visible assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and antiplasmodial activity of new indolone N-oxide derivatives. |
| AID771679 | Antiplasmodial activity against chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 assessed as growth inhibition after 24 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Design, synthesis, and biological and crystallographic evaluation of novel inhibitors of Plasmodium falciparum enoyl-ACP-reductase (PfFabI). |
| AID1808272 | Modulation of full length human Nurr1 expressed in SKNBE(2) cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene as | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1633709 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as host survival at 11.1 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 28 post infection relative to untreated control | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID411374 | Antimalarial activity as reduced parasitaemia after 72 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 in human erythrocytes by DAPI stain | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum. |
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| AID1373925 | Induction of apoptosis in human Jurkat E6-1 cells assessed as early apoptotic cells at 100 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 0.5 +/- 0.07 %) | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
| AID736789 | Selectivity index, ratio of GI50 for human HL60 cells to GI50 for Trypanosoma brucei TC211 | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators. |
| AID663124 | Antimalarial activity against Plasmodium berghei NS infected in po dosed CD1 mouse assessed as decrease in parasitemia measured on day 4 | 2012 | Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5 | Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2). |
| AID666735 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as reduction in parasitemia at 100 mg/kg, po administered as single dose measured on day 3 post-infection by flow cytometry | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID1829870 | Antimalarial activity against Plasmodium berghei ANKA infected in Balb/c mouse assessed as suppression of parasitemia at 50 mg/kg, ip administered for 4 days by microscopic analysis | |||
| AID1558338 | Cytotoxicity against HBMEC after 5 days by CellTiter Blue assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Drugs for the Treatment of Zika Virus Infection. |
| AID558058 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as Plasmodium lactate dehydrogenase release after 48 hrs by colorimetry | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Statins as potential antimalarial drugs: low relative potency and lack of synergy with conventional antimalarial drugs. |
| AID1530563 | Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of novel quinazoline derivatives as potent antiplasmodial agents. |
| AID1327393 | Cytotoxicity against CHO cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin. |
| AID1541834 | Antimalarial activity against asexual stage of Plasmodium falciparum NF54 assessed as reduction in parasite growth incubated for 96 hrs by SYBR Green I dye-based fluorescence assay | |||
| AID1647633 | Cytotoxicity against HEK293 cells incubated for 72 hrs by resazurin dye based assay | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Orthoscuticellines A-E, β-Carboline Alkaloids from the Bryozoan |
| AID683339 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells after 72 hrs by parasitic LDH assay | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity. |
| AID1533501 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring yolk absorption up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1484922 | Antimalarial activity against chloroquine resistant Plasmodium falciparum K1 after 72 hrs by SYBR green 1 dye based fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Cinnamoylated chloroquine analogues: A new structural class of antimalarial agents. |
| AID763609 | AUC (0 to t) in Sprague-Dawley rat at 5 mg/kg, po | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID212184 | Number of survivals against Plasmodium yoelii in mice (Mus musculus) (out of 5) at 48 mg/kg/day orally on day 28 | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Orally active amino functionalized antimalarial 1,2,4-trioxanes. |
| AID158821 | Inhibition of Plasmodium berghei infection in mice (Mus musculus) at 25 mg/kg peroral dose (experiment 3); Not determined | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID389358 | Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for chloroquine-sensitive Plasmodium falciparum FC32 | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: synthesis, and in vitro antimalarial activity. |
| AID347218 | Antimalarial schizonticidal activity against Plasmodium falciparum 3D7 infected erythrocytes at 0.19 ug/ml after 30-39 hrs | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials. |
| AID478227 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by fluorescence assay | 2010 | Journal of natural products, May-28, Volume: 73, Issue:5 | Antimalarial bromotyrosine derivatives from the Australian marine sponge Hyattella sp. |
| AID1233725 | Antiparasite activity against Plasmodium falciparum D6 assessed as growth inhibition incubated for 72 hrs by SYBR green fluorescence assay | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery. |
| AID361514 | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Novel 4-aminoquinolines active against chloroquine-resistant and sensitive P. falciparum strains that also inhibit botulinum serotype A. |
| AID1808478 | Modulation of full length human NOR1 expressed in PC12 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1649411 | Antimalarial activity against multidrug resistant Plasmodium falciparum Dd2 infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
| AID427289 | Toxicity in Plasmodium berghei infected ICR mice (Mus musculus) dosed intraperitoneally once daily for 4 days by Thompson test | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents. |
| AID1236486 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth after 48 hrs by LDH assay | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites. |
| AID1887441 | Antimalarial activity against blood stage chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in parasite growth incubated for 72 hrs by SYBR Green dye based fluorescence assay | |||
| AID1229886 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 20 post infection by Giemsa st | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID427681 | Antimalarial activity as reduced parasitaemia after 48 hrs against chloroquine, pyrimethamine and proguanil-resistant Plasmodium falciparum W2 infected in type A+ human erythrocytes by flow cytometry | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines. |
| AID272309 | Uptake of CDP/plasmid pGL3-CV polyplexes in HepG2 cells after 30 mins | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID536138 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by SYBR Green I fluorescence based method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies. |
| AID279388 | Growth inhibition of Plasmodium falciparum Dd2 ring stage infected erythrocytes after 72 hrs by DAPI fluorimetry | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | High-throughput Plasmodium falciparum growth assay for malaria drug discovery. |
| AID519267 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum K1AM by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
| AID1067547 | Antimalarial activity against chloroquine and mefloquine-resistant Plasmodium falciparum Dd2 assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria. |
| AID1167554 | Antiplasmodial activity against chloroquine, pyrimethamine and proguanil-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in Parasitemia incubated for 72 hrs by SYBR Green I fluorescence-based method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | New series of monoamidoxime derivatives displaying versatile antiparasitic activity. |
| AID158035 | Inhibitory concentration against Plasmodium falciparum D6 infected erythrocytes | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Synthesis and in vitro evaluation of 9-anilino-3,6-diaminoacridines active against a multidrug-resistant strain of the malaria parasite Plasmodium falciparum. |
| AID1829874 | Anticancer activity against human BEAS-2B cells assessed as cell growth inhibition measured for 72 hrs by MTT assay | |||
| AID366988 | Toxicity in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus) | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline. |
| AID289760 | Antimalarial activity against Plasmodium falciparum FCM29 | 2007 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3 | Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives. |
| AID655667 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 24 hrs by microbeta counter | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11 | Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS). |
| AID696503 | Antimalarial activity against Plasmodium berghei NK-65 infected in ICR mouse assessed as survival rate at 50 mg/kg, po administered day 3, 4 and 5 post infection | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | Lead optimization of antimalarial propafenone analogues. |
| AID1433136 | Antiviral activity against Vaccinia virus infected in human HEL cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID529757 | Antimicrobial activity against Plasmodium vivax at ring stage | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Stronger activity of human immunodeficiency virus type 1 protease inhibitors against clinical isolates of Plasmodium vivax than against those of P. falciparum. |
| AID554566 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as [3H]hypoxanthine incorporation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID630867 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse assessed as reduction in parasitemia at 30 mg/kg, po administered as quadruple dose regimen after 4 days by flow cytometry | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID1706809 | Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH inhibitors. |
| AID517482 | Cytotoxicity index, ratio of EC50 for mice (Mus musculus) J774 cells to EC50 for chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. |
| AID586606 | Antimalarial activity against trophozoites stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. |
| AID1163792 | Antiplasmodial activity against Plasmodium falciparum 3D7 late ring stages and early trophozoites forms infected in human erythrocytes assessed as parasite growth inhibition by LDH release assay | 2014 | Journal of natural products, Sep-26, Volume: 77, Issue:9 | MDN-0104, an antiplasmodial betaine lipid from Heterospora chenopodii. |
| AID1323835 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
| AID1694947 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human Erythrocyte assessed as reduction in plasmodial growth incubated for 48 hrs by FACS analysis | 2020 | RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1 | Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles. |
| AID1135020 | Antimalarial activity against Plasmodium falciparum Malayan Camp CH/Q infected in po once daily dosed Owl monkey assessed as curative dose compound treated for 7 days | 1979 | Journal of medicinal chemistry, Oct, Volume: 22, Issue:10 | Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity. |
| AID515042 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 after 72 hrs by SYBR green 1 fluorescence-based method | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID1433159 | Binding affinity to mu-oxo-heme (unknown origin) assessed as association constant at pH 5.8 by UV-visible absorption spectrophotometry | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID405079 | Antiplasmodial activity growth inhibition of chloroquine-resistant Plasmodium falciparum BHz 26/86 after 72 hrs | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Antiplasmodial activity of aryltetralone lignans from Holostylis reniformis. |
| AID417167 | Cytotoxicity against human A2780 cells | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Antiproliferative and antimalarial anthraquinones of Scutia myrtina from the Madagascar forest. |
| AID1633700 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as suppression in parasitemia at 33.3 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 5 post infection relative to untreated control | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID568778 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as reduction of parasite infection at 2 mg/kg, sc qd for 4 days relative to control | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen". |
| AID18984 | Lipophilicity at pH 7.4; ND = Not determined | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. |
| AID157860 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum | 2002 | Bioorganic & medicinal chemistry letters, Jul-08, Volume: 12, Issue:13 | Antimalarial activities of ring-substituted bioimidazoles. |
| AID1443525 | Selectivity index, ratio of CC50 for human HepG2A16 cells to IC50 for chloroquine/cycloguanil-resistant Plasmodium falciparum FCR3 | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | New hydrazine and hydrazide quinoxaline 1,4-di-N-oxide derivatives: In silico ADMET, antiplasmodial and antileishmanial activity. |
| AID1883296 | Selectivity index, ratio of IC50 for cytotoxicity against human MRC5 cells to IC50 for antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Sattahipmycin, a Hexacyclic Xanthone Produced by a Marine-Derived |
| AID346548 | Cytotoxicity against african green monkey Vero cells after 48 hrs by neutral red assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Synthesis and evaluation of dihydroartemisinin and dihydroartemisitene acetal dimers showing anticancer and antiprotozoal activity. |
| AID327132 | Selectivity for chloroquine-resistant Plasmodium falciparum Dd2 over chloroquine-sensitive Plasmodium falciparum HB3 as IC50 ratio by SYBR green assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines. |
| AID648237 | Antimalarial activity against Plasmodium falciparum 3D7 0087/N9 infected in human RBC engrafted NOD-SCID IL-2Rgamma-null mouse assessed as reduction in parasitemia administered orally 3 days post infection qd for 4 days measured 24 hrs after final dose by | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential. |
| AID255857 | In vitro antimalarial activity for Plasmodium falciparum D6 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives. |
| AID1467027 | Induction of autophagy in HEK293 cells assessed as increase in p62 level at 10 uM after 8 hrs by immunoblot analysis | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy. |
| AID158049 | Growth inhibition of chloroquine-sensitive Plasmodium falciparum K1 | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID570293 | Antiplasmodial activity against chloroquine-resistant ring stage Plasmodium falciparum W2 infected in human red blood cells after 48 hrs | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Incorporation of basic side chains into cryptolepine scaffold: structure-antimalarial activity relationships and mechanistic studies. |
| AID676993 | Antiplasmodial activity against drug resistant Plasmodium falciparum Dd2 ring stage cells assessed as reduction parasitemia by Malstat assay | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID1188460 | Antimalarial activity against tightly synchronized Plasmodium falciparum K1 assessed as parasite stage accumulation index at trophozoites stages at 10 uM treated at 30 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cyt | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID248406 | In vitro antimalarial activity as schizont maturation in chemo-sensitive Plasmodium falciparum | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Design, synthesis and biological evaluation of novel bicyclic beta-lactams as potential antimalarials. |
| AID1221956 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID540242 | Phospholipidosis-positive literature compound observed in Rhesus monkey | |||
| AID1700298 | Antimalarial activity against Plasmodium falciparum CQR (W2 clone) infected in human erythrocyte assessed as reduction in parasite growth incubated for 48 hrs by SYBR assay | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission. |
| AID586607 | Antimalarial activity against ring stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. |
| AID318198 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID327135 | Selectivity index for chloroquine-resistant Plasmodium falciparum FCB to chloroquine-sensitive Plasmodium falciparum GCO3 by SYBR green IC50 ratio | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines. |
| AID401640 | Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2005 | Journal of natural products, May, Volume: 68, Issue:5 | Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound. |
| AID1201515 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for chloroquine-sensitive Plasmodium falciparum K1 infected in human erythrocytes | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID158699 | In vitro inhibitory concentration against chloroquine-resistant Plasmodium falciparum K1 | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of new diamine containing analogues. |
| AID631173 | Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as reduction in parasitemia measured between day 1 and day 2 relative to control | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21 | The anti-malarial activity of bivalent imidazolium salts. |
| AID1221963 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID647315 | Antimalarial activity against ring stage chloroquine-resistant Plasmodium falciparum INDO infected in human O positive erythrocytes after 48 hrs by SYBR green 1 fluorescence assay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Stilbene-chalcone hybrids: design, synthesis, and evaluation as a new class of antimalarial scaffolds that trigger cell death through stage specific apoptosis. |
| AID351790 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 after 48 hrs as [3H]hypoxanthine uptake | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10 | Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids. |
| AID118001 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS., activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4 day test at a concentration of 1 mg/kg in experiment 2 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID1188464 | Antimalarial activity against Plasmodium falciparum HB3 by automated image mining based cytological profiling assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID442256 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID1234852 | Cytotoxicity against HMEC1 assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Modified quaternary ammonium salts as potential antimalarial agents. |
| AID1169350 | Selectivity index, ratio of cytotoxic EC50 against human cells to EC50 for Plasmodium falciparum 3D7 | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
| AID688315 | Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and comparison of antiplasmodial activity of (+), (-) and racemic 7-chloro-4-(N-lupinyl)aminoquinoline. |
| AID1234849 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Modified quaternary ammonium salts as potential antimalarial agents. |
| AID323677 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum 34-1/E | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID774789 | Antiprotozoal activity against Plasmodium falciparum assessed as parasite growth inhibition | 2013 | Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18 | Natural product derived antiprotozoal agents: synthesis, biological evaluation, and structure-activity relationships of novel chromene and chromane derivatives. |
| AID427682 | Cytotoxicity against human K562 cells after 72 hrs by flow cytometry | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines. |
| AID683365 | Antimalarial activity Plasmodium berghei infected in mouse assessed as cure from infection at 100 mg/kg, po administered QD for 3 days measured on day 28 | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity. |
| AID1846637 | Antiprotozoal activity against Chloroquine-resistant Plasmodium falciparum K1 assessed as parasite growth inhibition | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9 | Synthesis and Biological Evaluation of Natural-Product-Inspired, Aminoalkyl-Substituted 1-Benzopyrans as Novel Antiplasmodial Agents. |
| AID159735 | Compound was tested in vivo for antimalarial activity against Plasmodium berghei in mice (Mus musculus) after 6 days of administration (ED90 is the dose necessary to reduce the percentage of infected cells to 10% of the level found in the infected untreat | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials. |
| AID673598 | Antiplasmodial activity Plasmodium vinckei petteri infected in CD mouse assessed as suppression of parasitaemia at 10 mg/kg/day, ip administered from day 0 to day 3 and measured on day 4 by Giemsa staining relative to control | 2012 | Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15 | Short synthesis and antimalarial activity of fagaronine. |
| AID1732469 | Antimalarial activity against asexual blood stage of chloroquine-resistant Plasmodium falciparum Dd2 assessed as reduction in cell viability after 72 hrs by EtBr staining based flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
| AID372463 | Antimalarial activity as 2nd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by flow cytometry | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast. |
| AID519583 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Potent antimalarial activity of histone deacetylase inhibitor analogues. |
| AID1070210 | Antiplasmodial activity chloroquine-resistant Plasmodium falciparum Dd2 by lactate dehydrogenase assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4 | Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity. |
| AID338767 | Antimalarial activity against Plasmodium falciparum D6 in human erythrocytes after 24 hrs by [3H]hypoxanthine uptake | |||
| AID663063 | Antimalarial activity against Plasmodium berghei KBG173 infected in mouse assessed as decrease in parasitemia at 2.5 mg/kg, ip BID administered on day 3, 4 and 5 post infection measured on day 31 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin. |
| AID469810 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as LDH activity after 72 hrs by malstat reagent method | 2009 | Journal of natural products, Dec, Volume: 72, Issue:12 | Biologically active tetranorditerpenoids from the fungus Sclerotinia homoeocarpa causal agent of dollar spot in turfgrass. |
| AID598736 | Antimalarial malarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human A positive erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 24 hrs | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | 2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads. |
| AID269375 | Inhibition of scrapie prion formation in mouse ScN2a cell line | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17 | Similar structure-activity relationships of quinoline derivatives for antiprion and antimalarial effects. |
| AID309396 | Cytotoxicity against human HeLa cells assessed as cell survival after 7 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential antimalarial and anticancer agents. |
| AID1633696 | Resistance index, ratio of IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 incubated for 48 hrs by parasite lactate dehydrogenase assay to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium f | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID1140159 | Antimalarial activity against Plasmodium yoelii MR4 MRA-428 infected in mouse CF1 assessed as dose required to achieve cure measured as 30 days survival administered through oral gavage once daily for 4 days | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers. |
| AID1202797 | Selectivity ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-resistant Plasmodium falciparum C235 | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives. |
| AID1915888 | Antiplasmodial activity against chloroquine-sensitive asexual blood stage Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 1 hr by HRP2-ELISA | |||
| AID519194 | Antimicrobial activity against Plasmodium vivax at the trophozoites by microscopy treated during ring stage | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID499808 | Antileishmanial activity against Leishmania donovani promastigotes after 72 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
| AID620096 | Resistance ratio of IC50 for Plasmodium falciparum W2 to IC50 for Plasmodium falciparum 3D7 | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities. |
| AID1177594 | Antiparasitic activity against Plasmodium falciparum NF54 | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 | Xenortide Biosynthesis by Entomopathogenic Xenorhabdus nematophila. |
| AID626324 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Biological evaluation of glycosyl-isoindigo derivatives against the pathogenic agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis). |
| AID1072851 | Antiplasmodial activity against Plasmodium berghei ANKA infected in mouse assessed as mean survival time at 3 mg/kg, po administered 4 times per day | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity. |
| AID377694 | Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 in erythrocytes by LDH reporter assay | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID421657 | Cytotoxicity against human erythrocytes | 2009 | Journal of natural products, Feb-27, Volume: 72, Issue:2 | Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity. |
| AID732337 | Antimalarial activity against multidrug-resistant and atovaquone-sensitive Plasmodium falciparum TM91C235 | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID105843 | Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 8 uM concentration | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID1830497 | Cytotoxicity against human Mahlavu cells assessed as cell viability by MTT assay | |||
| AID284375 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. |
| AID480231 | Inhibition of CYP2B6 in human liver microsomes assessed as metabolite produced at 10 uM by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1494310 | Half life in Sprague-Dawley rat liver microsomes at 100 uM up to 180 mins by HPLC-UV analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1699652 | Selectivity index, ratio of IC50 for cytotoxicity against human HEK293 cells to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring stage | 2020 | Journal of natural products, 11-25, Volume: 83, Issue:11 | Antiplasmodial Alkaloids from the Australian Bryozoan |
| AID461170 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum W2 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. |
| AID158026 | In vitro antimalarial activity against Plasmodium falciparum SGE2 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID1808473 | Modulation of full length human Nur77 expressed in PC12 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID269379 | Toxicity against ScN2a cell line at 10 uM | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17 | Similar structure-activity relationships of quinoline derivatives for antiprion and antimalarial effects. |
| AID1688344 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR3 infected in human erythrocytes incubated for 48 hrs by [3H]-hypoxanthine incorporation assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID1859900 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID359665 | Cytotoxicity against human KB cells | 1992 | Journal of natural products, Dec, Volume: 55, Issue:12 | Antimalarial activity of sesquiterpenes from the marine sponge Acanthella klethra. |
| AID319199 | Antimalarial activity against Plasmodium falciparum PH3 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles. |
| AID731060 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Synthesis of 2-aminomethyl-4-phenyl-1-azabicyclo[2.2.1]heptanes via LiAlH₄-induced reductive cyclization of 2-(4-chloro-2-cyano-2-phenylbutyl)aziridines and evaluation of their antimalarial activity. |
| AID151220 | In vitro growth inhibition of Plasmodium falciparum D6 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Antiplasmodial activity and cytotoxicity of bis-, tris-, and tetraquinolines with linear or cyclic amino linkers. |
| AID316375 | Binding affinity to heme in aqueous solution | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Synthesis and heme-binding correlation with antimalarial activity of 3,6-bis-(omega-N,N-diethylaminoamyloxy)-4,5-difluoroxanthone. |
| AID1494357 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as increase in number of virtual platform crossing at 30 mg/kg/day, po for 80 days by Morris water maze test | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID377696 | Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum W2 in erythrocytes by LDH reporter assay | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7 | Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID72010 | Antiproliferative activity against Mouse mammary tumor FM3A cells | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | Cholic acid derivatives as 1,2,4,5-tetraoxane carriers: structure and antimalarial and antiproliferative activity. |
| AID1880211 | Selectivity index, ratio of CC50 for cytotoxicity against HEL 299 cells to EC50 for antiviral activity against HCoV-OC43 infected in HEL 299 cells | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
| AID1201511 | Cytotoxicity against CHO cells assessed as cell viability after 24 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID158191 | In vitro anti-protozoal activity against Plasmodium falciparum Ghana strain | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Biological evaluation of substituted quinolines. |
| AID389360 | Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for chloroquine-resistant Plasmodium falciparum PFB | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: synthesis, and in vitro antimalarial activity. |
| AID622797 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in parasitemia after 72 hrs by spectrophotometry | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | Synthesis and evaluation of 7-substituted 4-aminoquinoline analogues for antimalarial activity. |
| AID644817 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A-positive erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 48 hrs by semi-automated microdilution technique | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents. |
| AID678318 | Inhibition of beta hematin formation assessed as ratio of molar equivalents of compound to molar equivalents of hematin for 50% inhibition after 18 hrs | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID1167708 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by Malaria SYBR Green I-nucleic acid staining based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis of chiral chloroquine and its analogues as antimalarial agents. |
| AID722368 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for chloroquine-susceptible Plasmodium falciparum D10 | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Synthesis, characterization and antimalarial activity of quinoline-pyrimidine hybrids. |
| AID580316 | Antimalarial activity against chloroquine-susceptible Plasmodium berghei ANKA assessed as inhibition of trophozoite extract-mediated mouse hemoglobin hydrolysis at 10 mM after 18 hrs by SDS-PAGE | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents. |
| AID600553 | Toxicity in human RBC assessed as hemolysis at 100 uM after 48 hrs | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Antiprotozoal activity of chloroquinoline based chalcones. |
| AID1405078 | Resistance index, ratio of IC50 for synchronized ring stage of chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes to IC50 for synchronized ring stage of chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythroc | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Facile synthesis of vanillin-based novel bischalcones identifies one that induces apoptosis and displays synergy with Artemisinin in killing chloroquine resistant Plasmodium falciparum. |
| AID453363 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID317956 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum. |
| AID375467 | Antiplasmodial activity after 48 hrs against chloroquine-sensitive Plasmodium falciparum D10 infected human erythrocytes by LDH reporter assay | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Synthesis of novel 2-alkoxy-3-amino-3-arylpropan-1-ols and 5-alkoxy-4-aryl-1,3-oxazinanes with antimalarial activity. |
| AID1810599 | Antiplasmodial activity against asexual blood stage of multidrug-resistant Plasmodium falciparum TM90C2B infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | |||
| AID1701749 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in po dosed NSG mouse assessed as blood AUC level require to show 90% reduction in parasitemia administered once daily for 4 consecutive days starting from day 3 post-infection and measure | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity. |
| AID318187 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. |
| AID670966 | Antimalarial activity against chloroquine sensitive Plasmodium falciparum FCR-3 | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Synthesis and antimalarial activity of calothrixins A and B, and their N-alkyl derivatives. |
| AID477959 | Lipophilicity, log D at pH 7.4 | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID232455 | Selectivity ratio between cytotoxicity to antimalarial activity was determined | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20 | Metabolites of febrifugine and its synthetic analogue by mouse liver S9 and their antimalarial activity against Plasmodium malaria parasite. |
| AID473014 | Antitrypanosomal activity against Trypanosoma brucei brucei | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids. |
| AID564240 | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 and wild type pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID597175 | Partition coefficient, log D of the compound at pH 3 by HPLC analysis | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies. |
| AID768455 | Ratio of IC50 for trophozoite stage of Plasmodium falciparum 3D7 infected in RBC after 5 hrs to IC50 for Plasmodium falciparum 3D7 infected in RBC after 48 hrs | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID446175 | Antimalarial activity against Plasmodium berghei ANKA infected Swiss mice (Mus musculus) assessed as reduction in parasitemia treated intraperitoneally for 3 days measured on day 4 | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and antiplasmodial activity of new indolone N-oxide derivatives. |
| AID1073349 | Antiviral activity against Chikungunya virus | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Chikungunya virus: emerging targets and new opportunities for medicinal chemistry. |
| AID1439482 | Resistance index, ratio of IC50 for Plasmodium falciparum W2 infected in red blood cells to IC50 for Plasmodium falciparum D6 infected in red blood cells | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Synthesis, antimalarial activity, heme binding and docking studies of N-substituted 4-aminoquinoline-pyrimidine molecular hybrids. |
| AID158037 | Inhibitory concentration against Plasmodium falciparum W2 infected erythrocytes | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10 | Synthesis and in vitro evaluation of 9-anilino-3,6-diaminoacridines active against a multidrug-resistant strain of the malaria parasite Plasmodium falciparum. |
| AID1664917 | Binding affinity to monomeric heme after 24 hrs by UV-Visible Spectroscopic analysis | 2020 | ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7 | Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity. |
| AID536139 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum Dd2 to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies. |
| AID1404595 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based fluorescence assay | 2018 | Journal of natural products, 04-27, Volume: 81, Issue:4 | Microthecaline A, a Quinoline Serrulatane Alkaloid from the Roots of the Australian Desert Plant Eremophila microtheca. |
| AID99863 | In vitro anti protozoal activity against Leishmania amazonensis strain MHOM/ET/L82/LV9 was determined; ND = Not determined | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Biological evaluation of substituted quinolines. |
| AID1887442 | Antimalarial activity against blood stage chloroquine-resistant Plasmodium falciparum Dd2 assessed as reduction in parasite growth incubated for 72 hrs by SYBR Green dye based fluorescence assay | |||
| AID1128659 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as mean survival days at 30 mg/kg, po qd for 4 days | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1. |
| AID754527 | Inhibition of hemozoin formation in 12.9 M acetate buffer at pH 4.5 at 60 degC after 1 hr by microtiter-based high-throughput assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID1380020 | Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Synthesis and antimalarial evaluation of artesunate-polyamine and trioxolane-polyamine conjugates. |
| AID740869 | Cytotoxicity against human MCR5 cells after 7 days by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8 | Borrelidin analogues with antimalarial activity: design, synthesis and biological evaluation against Plasmodium falciparum parasites. |
| AID337535 | Selectivity index, ratio of ED50 for human LUC1 cells to ED50 for chloroquine-resistant Plasmodium falciparum W2 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID718288 | Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay | 2012 | Journal of natural products, Dec-28, Volume: 75, Issue:12 | Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication. |
| AID267108 | Antimalarial activity against Plasmodium falciparum W2 | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Tetraoxane antimalarials and their reaction with Fe(II). |
| AID1625413 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 infected in human RBC incubated for 18 to 20 hrs by microdilution radioisotope method | 2016 | Journal of natural products, Apr-22, Volume: 79, Issue:4 | Antimalarial Oxoprotoberberine Alkaloids from the Leaves of Miliusa cuneata. |
| AID1444636 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | Synthesis and antiplasmodial activity of novel indoleamide derivatives bearing sulfonamide and triazole pharmacophores. |
| AID1255801 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum 3D7 infected in human O+ erythrocytes after 72 hrs by SYBR Green based parasite proliferation assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22 | Synthesis and preliminary biological evaluation of a small library of hybrid compounds based on Ugi isocyanide multicomponent reactions with a marine natural product scaffold. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID580694 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of trophozoite stage parasite growth at 100 times IC50 after 1 hr by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID628228 | Antimalarial activity against chloroquine- and mefloquine-resistant Plasmodium falciparum W2-Mef infected in human O-positive erythrocytes assessed as inhibition of ring-stage parasite growth after 48 hrs | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | 3-bromohomofascaplysin A, a fascaplysin analogue from a Fijian Didemnum sp. ascidian. |
| AID720845 | Antimalarial activity against erythrocytic stage of Plasmodium falciparum NF54 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Aminoalkyl derivatives of guanidine diaromatic minor groove binders with antiprotozoal activity. |
| AID434585 | Resistance factor, ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum HB3 | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. |
| AID284270 | Antimalarial activity against Plasmodium falciparum W2 | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID451286 | Selectivity index, ratio of CC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2009 | Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17 | Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with potent antiplasmodial activity. |
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| AID509194 | Inhibition of TLR7/TLR9-mediated indoleamine 2,3-dioxygenase activation in aldrithiol-2-treated HIV1 MN-stimulated human PBMC assessed as decrease in kynurenine to tryptophan level at 100 uM after 20 hrs by fluorometric assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
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| AID1335175 | Inhibition of beta-hematin formation incubated for 5 to 6 hrs by NP40 detergent-mediated assay | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active against |
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| AID272301 | Exclusion of picogreen dye from plasmid pGL3-CV at 0.5 mM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
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| AID1808442 | Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as decrease in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by luciferase reporter gene a | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
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| AID1405715 | Induction of mitotic arrest in human HeLa cells assessed as formation of misaligned chromosomes at 15 to 25 uM after 6 hrs by DAPI staining-based immunofluorescence analysis | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
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| AID543644 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected in ICR mouse assessed as parasitemia at 5 mg/kg/day, po pretreated for 4 days before infection and measured after 72 hrs (Rvb = 4.6+/-0.21 %) | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID414511 | Lipid accumulation ratio in pH 5.2 digestive vacuole | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
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| AID272310 | Uptake of CDP/plasmid pGL3-CV polyplexes in HepG2 cells after 2 hrs | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID406392 | Inhibition of rat PFTase | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
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| AID1203064 | Ratio of hydroxychloroquine IC50 to compound IC50 for human HCC827 cells | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID564287 | Antimalarial activity against Plasmodium falciparum FCM29 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID1494361 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as time spent in correct quadrant at 30 mg/kg/day, po for 80 days by Morris water maze test (Rvb = 20.6 +/- 4.4 sec) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1713578 | Hemolytic activity in human erythrocytes measured after 1 hr by microtiter plate method | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents. |
| AID412364 | Antimalarial activity after 24 hrs against chloroquine-resistant synchronous Plasmodium falciparum K1 infected human A+ erythrocytes by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID598734 | Antimalarial malarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A positive erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 24 hrs | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | 2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads. |
| AID453368 | Binding affinity to synthetic hematin by spectrophotometry | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID1808437 | Cytotoxicity against human SKNBE2 cells assessed as reduction in cell viability at 125 uM incubated for 18 hrs by Cell Titer Glo assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID314181 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Cryptolepine analogues containing basic aminoalkyl side-chains at C-11: synthesis, antiplasmodial activity, and cytotoxicity. |
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| AID701110 | Mutagenicity against Salmonella typhimurium TA100 assessed as revertants at 20 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
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| AID1755248 | Disaggregation of copper-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 50 uM measured after 24 hrs by transmission electron microscopic analysis | |||
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| AID1581635 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 erythrocytic stage measured after 3 days by HRP2 assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Harmicines - harmine and cinnamic acid hybrids as novel antiplasmodial hits. |
| AID1494325 | Induction of cell proliferation in C57BL/6 mouse hippocampal neurons in CA1 region assessed as BrdU-incorporation at 0.5 uL/hr, icv for 7 days by immunohistochemical analysis (Rvb = 3.2%) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
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| AID458586 | Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4 | Design and synthesis of anti-breast cancer agents from 4-piperazinylquinoline: a hybrid pharmacophore approach. |
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| AID553562 | Toxicity in malaria patient assessed as duration of vomiting at quartile 4 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID1433129 | Selectivity index, ratio of IC50 for human HeLa cells to IC50 for chloroquine-resistant asexual intraerythrocytic stage of Plasmodium falciparum Dd2 | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID1726765 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as growth inhibition after 48 hrs by flow cytometer | 2021 | RSC medicinal chemistry, Jun-23, Volume: 12, Issue:6 | Design, synthesis, crystal structure and anti-plasmodial evaluation of tetrahydrobenzo[4,5]thieno[2,3- |
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| AID320713 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum Thai after 24 hrs | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents. |
| AID558842 | Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID158674 | Effective dose ED90 against Plasmodium berghei N in mice (Mus musculus) malaria model after subcutaneous administration | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID1776189 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse model assessed as reduction in parasitemia at 30 mg/kg, po dosed 4 times relative to control | |||
| AID1070249 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for chloroquine-resistant and mefloquine-sensitive Plasmodium falciparum W2 | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | 7-Chloroquinolinotriazoles: synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies. |
| AID452323 | Growth inhibition of human CE81T cells after 48 hrs by MTT assay in presence of 10% FBS supplemented DMEM medium | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID1168869 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID1706810 | Selectivity index, ratio of IC50 for cytotoxicity against human HepG2 cells to IC50 for antimalarial activity against Plasmodium falciparum 3D7 | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comparative study between the anti-P. falciparum activity of triazolopyrimidine, pyrazolopyrimidine and quinoline derivatives and the identification of new PfDHODH inhibitors. |
| AID780280 | Antimalarial activity against ring stage of chloroquine-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
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| AID419116 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 molecules of heme to 1 equivalent of drug in presence of 40% DMSO by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
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| AID480233 | Inhibition of CYP2C19 in human liver microsomes assessed as metabolite produced at 10 uM by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID611750 | Cytotoxicity against human HepG2 cells at 19 uM after 24 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Synthesis and antimalarial activity of new heterocyclic hybrids based on chloroquine and thiazolidinone scaffolds. |
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| AID1440398 | Disruption of biofilm of Candida albicans ATCC 90028 after 48 hrs in presence of voriconazole by XTT assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Tackling Fungal Resistance by Biofilm Inhibitors. |
| AID1404704 | Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Enhanced antimalarial activity of plasmepsin V inhibitors by modification of the P |
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| AID1275779 | Inhibition of voltage-gated calcium channel in Wistar rat synaptoneurosomes after 30 mins by fluorescent ratiometric indicator method | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
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| AID517481 | Cytotoxicity against mouse J774 cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. |
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| AID392459 | Cytotoxicity against rat L6 cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity. |
| AID660169 | Inhibition of beta-hematin formation after 16 hrs at pH 5.6 by microplate reader | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Investigating the activity of quinine analogues versus chloroquine resistant Plasmodium falciparum. |
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| AID1829876 | Selectivity ratio of IC50 for anticancer activity against human BEAS-2B cells to IC50 for anticancer activity against human A549 cells | |||
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| AID1405798 | Induction of autophagy in human HeLa cells assessed as increase in LC3-2 to LC3-1 ratio at 2.5 uM after 6 hrs by immunoblot analysis relative to control | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131). |
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| AID1494358 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as increase in number of effective region crossing at 30 mg/kg/day, po for 80 days by Morris water maze test | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
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| AID620101 | Cytotoxicity against human HepG2 cells after 48 hrs by lactate dehydrogenase assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities. |
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| AID1057134 | Apparent permeability from apical to basolateral side in MDCK cells at 10 uM after 1 hr by LC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum. |
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| AID1733523 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Identification of two novel thiophene analogues as inducers of autophagy mediated cell death in breast cancer cells. |
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| AID1439849 | Antiplasmodial activity against erythrocytic stage of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity. |
| AID1624376 | Antimalarial activity against Plasmodium berghei ANKA infected in Swiss mouse assessed as mean survival days at 10 mg/kg, ip administered once daily for 5 days (Rvb = 11.2 day) | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID525491 | Antigametocyte activity against ring stage Plasmodium falciparum D10 assessed as inhibition of parasite growth at 50 nM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID480229 | Inhibition of CYP3A4 in human liver microsomes assessed as metabolite produced at 1 uM using midazolam as substrate by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID608682 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives. |
| AID1177973 | Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by XTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Amino derivatives of indolone-N-oxide: preparation and antiplasmodial properties. |
| AID1457208 | Antimalarial activity against Plasmodium falciparum HB3 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID597184 | Ratio of compound IC50 to hematin IC50 for inhibition of beta-hematin formation | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies. |
| AID666877 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as reduction in parasitemia at 10 mg/kg, po administered as single dose measured on day 3 post-infection by flow cytometry | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID775659 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Design, synthesis, and in vitro cancer cell growth inhibition evaluation and antimalarial testing of trioxanes installed in cyclic 2-enoate substructures. |
| AID477960 | Binding affinity to pUC18 DNA at pH 7.5 by UV-Vis spectrophotometry analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID1140204 | Antimalarial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF54 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis, β-haematin inhibition, and in vitro antimalarial testing of isocryptolepine analogues: SAR study of indolo[3,2-c]quinolines with various substituents at C2, C6, and N11. |
| AID731868 | Antimalarial activity against Plasmodium berghei str. ANKA infected in NMRI mouse assessed as mean survival days at 10 mg/kg, po qd for 4 days (Rvb = 5.7 days) | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID422744 | Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 by pLDH activity | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1 | Indolizidine, antiinfective and antiparasitic compounds from Prosopis glandulosa var. glandulosa. |
| AID573261 | Toxicity in human RBC assessed as hemolysis pretreated at 50 uM for 30 mins followed by washing and incubated with 40 uM ferriprotoporphyrin 9 for 2hrs | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID158846 | Inhibitory activity against Plasmodium falciparum NF54 | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID1191135 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I-based fluorescence method | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters. |
| AID337531 | Selectivity index, ratio of ED50 for human BCA1 cells to ED50 for chloroquine-resistant Plasmodium falciparum W2 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID701115 | Half life in po dosed human plasma | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1359643 | Antiplasmodial activity against Plasmodium falciparum 3D7 late stage forms infected in human non-washed human RBC containing full drug dosages by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID1808484 | Modulation of Gal4-fused VP16 expressed in SKNBE(2) cells co-transfected with UAS repoter gene assessed as increase in luciferase activity upto 15 uM incubated for 18 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1533160 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 measured after 48 hrs by SYBR green1 dye based fluorescence assay | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12 | Potent Antimalarial 2-Pyrazolyl Quinolone |
| AID768721 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as quantal survival at 51.5 mg/kg, ip administered 4 times per day for 3 days measured on day 10 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives. |
| AID780278 | Cytotoxicity against human NFF cells after 3 days by SRB assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment. |
| AID1808467 | Modulation of full length human NOR1 expressed in SK-N-BE(2) cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1076159 | Inhibition of beta-hematin formation at 2.5 mM after 24 hrs by spectrophotometry | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents. |
| AID1204107 | Cytotoxic activity against human HepG2 cells assessed as cell viability at 1000 ug/ml incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID382474 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Thai after 24 hrs by semiautomated micro dilution assay | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2 | Synthesis and antimalarial activity of new analogues of amodiaquine. |
| AID359999 | Selectivity index, ratio of IC50 of african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha. |
| AID1494356 | Toxicity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as swimming speed at 30 mg/kg/day, po for 80 days by Morris water maze test (Rvb = 17.8 +/- 2.5 cm/sec) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1494303 | Inhibition of Cu2+ - induced amyloid beta (1 to 42) (unknown origin) aggregation assessed as small-sized nonfibrillar amorphos amyloid beta at compound/amyloid beta/Cu2+ ratio of 2:1:1 after 48 hrs by TEM analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID553550 | Volume of distribution in malaria patient | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID1483950 | Antiprotozoal activity against erythrocytic stage of Plasmodium falciparum NF54 after 48 hrs by [3H]- hypoxanthine incorporation assay | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Dioncophyllines C |
| AID723629 | Antiplasmodial activity against erythrocyte form of chloroquine-sensitive Plasmodium falciparum D10 by parasite lactate dehydrogenase assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis and antiplasmodial evaluation of novel (4-aminobutyloxy)quinolines. |
| AID118017 | The compound was tested in vivo antimalarial response against multidrug-resistant Plasmodium yoelii in Swiss mice (Mus musculus) at a dose of 48 (mg/kg/day) after 4 day | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Photo-oxygenation of geraniol: synthesis of a novel series of hydroxy-functionalized anti-malarial 1,2,4-trioxanes. |
| AID1332920 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as mean survival days at 5 mg/kg, po administered 4 hrs post infection for 4 days measured up to 30 days (Rvb = 7.2 days) | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 4, 5-Dihydrooxazole-pyrazoline hybrids: Synthesis and their evaluation as potential antimalarial agents. |
| AID366981 | Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum K1/Thailand by [3H]hypoxanthine uptake | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline. |
| AID480217 | Antimalarial activity against Plasmodium falciparum 3D7 by FACS assay | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID274218 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains. |
| AID543843 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected ICR mouse assessed as survival of mouse at 10 mg/kg/day, po for 4 days measured after 27 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID1585802 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 asynchronous cultures infected in human erythrocytes after 72 hrs by SYBR green1 staining based fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis of isatin based N |
| AID159738 | Inhibition of Plasmodium falciparum FCM29 | 2000 | Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14 | Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker. |
| AID243143 | Binding constant dissolved in DMSO against hematin receptor at pH 7.4 (HEPES Buffer) upon incubation at 42 degree C | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: design, construction, characterization, and pharmacology of metaquine. |
| AID212502 | Compound was tested for antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS, activity is expressed as the mortality rate at a concentration of 1 mg/kg. in experiment 2; 5 out of 5 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID1182790 | Antiplasmodial activity against Plasmodium falciparum W2 harboring mutations conferring drug-resistance by SYBR-green based assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
| AID358965 | Antiplasmodial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum FCA10/GHA as LDH activity | 2002 | Journal of natural products, May, Volume: 65, Issue:5 | The antiplasmodial activity of isolates from Ajuga remota. |
| AID1433158 | Binding affinity to monomeric heme (unknown origin) assessed as association constant at pH 7.5 by UV-visible absorption spectrophotometry | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID624628 | Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID158865 | Antimalarial activity against Plasmodium falciparum Dd2 in erythrocytes | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | Structure-activity relationships of novel anti-malarial agents. Part 3: N-(4-acylamino-3-benzoylphenyl)-4-propoxycinnamic acid amides. |
| AID1639290 | Selectivity ratio of IC50 for Plasmodium falciparum Dd2 ring stage forms to IC50 for Plasmodium falciparum 3D7 ring stage forms | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens. |
| AID1713581 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as decrease in parasitemia at 50 mg/kg, po qd administered via gavage for 4 consecutive days and measured up to 8 days by optical microscopy analysis | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents. |
| AID393075 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Pharmacodynamics and pharmacokinetics studies of phenoxazinium derivatives for antimalarial agent. |
| AID726920 | Antimalarial activity against Plasmodium falciparum C235 containing mdr1 transporter gene assessed as growth inhibition after 72 hrs by SYBR Green 1-based fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | From a cytotoxic agent to the discovery of a novel antimalarial agent. |
| AID266644 | Antimalarial activity against multidrug-resistant Plasmodium falciparum W2 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug-resistant P. falciparum. |
| AID736793 | Antitrypanosomal activity against Trypanosoma brucei TC211 after 24 hrs by alamar blue assay | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators. |
| AID519974 | Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum. |
| AID525281 | Antimicrobial activity against Plasmodium falciparum harboring HFP-tagged Pfs16 protein after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID775982 | Antiplasmodial activity against ring stage of chloroquine-resistant Plasmodium falciparum W2 infected in human RBC after 48 hrs by flow cytometric analysis | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Squaric acid/4-aminoquinoline conjugates: novel potent antiplasmodial agents. |
| AID419755 | Antiplasmodial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum K1 infected human erythrocytes by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
| AID1533502 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring liver morphology and color up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1572679 | Antimalarial activity against chloroquine-resistant and mefloquine-sensitive Plasmodium falciparum W2 ring stage form infected in human erythrocytes by spectrophotometric analysis | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | New hybrid trifluoromethylquinolines as antiplasmodium agents. |
| AID1332923 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells assessed as inhibition of schizont stage parasite growth measured after 24 hrs by giemsa staining based assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 4, 5-Dihydrooxazole-pyrazoline hybrids: Synthesis and their evaluation as potential antimalarial agents. |
| AID1585803 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 asynchronous cultures infected in human erythrocytes after 72 hrs by SYBR green1 staining based fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis of isatin based N |
| AID1706561 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 incubated for 48 hrs by parasite lactate dehydrogenase assay | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities. |
| AID268571 | Selectivity for L929 cells over Plasmodium falciparum FCR3 as EC50 ratio | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Exploration of a new type of antimalarial compounds based on febrifugine. |
| AID518336 | Antimalarial activity against Plasmodium berghei ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitemia at 100 mg/kg, perorally administered as single dose measured on day 3 postinfection | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. |
| AID388305 | Antimalarial activity against Plasmodium berghei infected mice (Mus musculus) | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Carbonic anhydrase inhibitors: inhibition of Plasmodium falciparum carbonic anhydrase with aromatic/heterocyclic sulfonamides-in vitro and in vivo studies. |
| AID558838 | Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID423747 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1 | Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. |
| AID1179401 | Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Plasmodium falciparum | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14 | Antiplasmodial activity of new 4-aminoquinoline derivatives against chloroquine resistant strain. |
| AID1738755 | Resistance index, ratio of IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis and biological evaluation of novel quinoline-piperidine scaffolds as antiplasmodium agents. |
| AID574873 | Antiplasmodial activity against Plasmodium cynomolgi sporozoites infected in Rhesus monkey assessed as relapse time at 10 mg/kg/day, po administered for 7 consecutive days before infection | 2011 | Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4 | New imidazolidinedione derivatives as antimalarial agents. |
| AID710073 | Resistant index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents. |
| AID452329 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 100 uM ZnCl2 | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID570294 | Antiplasmodial activity against chloroquine-sensitive ring stage Plasmodium falciparum 3D7 infected in human red blood cells after 48 hrs | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Incorporation of basic side chains into cryptolepine scaffold: structure-antimalarial activity relationships and mechanistic studies. |
| AID298580 | Antimalarial activity against Plasmodium falciparum D6 | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1). |
| AID775957 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | In vitro antimalarial activity, β-haematin inhibition and structure-activity relationships in a series of quinoline triazoles. |
| AID419178 | Toxicity in po dosed mouse assessed as maximal nonlethal dose administered as single dose | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID453385 | Antiplasmodial activity against Plasmodium falciparum W2 infected in RBCs by parasitic LDH release assay | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers. |
| AID267113 | Effect on survival of CD1 mice (Mus musculus) infected with Plasmodium berghei KBG173 at 4 mg/kg/day, peroral | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Tetraoxane antimalarials and their reaction with Fe(II). |
| AID1808461 | Modulation of full length human Nur77 expressed in HEK293 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID158025 | In vitro antimalarial activity against Plasmodium falciparum FG4 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID675166 | Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for Plasmodium falciparum | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum. |
| AID1191138 | Selectivity index, ratio of IC50 for human WI38 cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters. |
| AID349012 | Selectivity index, ratio of IC50 for human KB cells to IC50 for Plasmodium falciparum 3D7 | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. |
| AID404785 | Selectivity for chloroquine-resistant Plasmodium falciparum FCB over chloroquine-sensitive Plasmodium falciparum GCO3 as IC50 ratio by SYBR green assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID1518830 | Selectivity index, ratio of EC50 for human MDA-MB-231 cells to IC50 for ring stage Plasmodium falciparum K1 | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor. |
| AID404450 | Antimalarial activity against Plasmodium falciparum TM91C235 by hypoxanthine uptake | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum. |
| AID334013 | Antiplasmodial activity against Plasmodium falciparum schizonts assessed as [3H]hypoxanthine incorporation by liquid scintillation counting | 1997 | Journal of natural products, Oct, Volume: 60, Issue:10 | Antiprotozoal compounds from Asparagus africanus. |
| AID1167717 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67infected in Swiss Albino mouse assessed as mouse cured on day 28 at 20 mg/kg, po once daily for 4 days measured on day 4 post infection | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis of chiral chloroquine and its analogues as antimalarial agents. |
| AID1204123 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as parasitemia level at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 7 post infection (Rvb = 5.42 +/- 0.7 | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1530038 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Quinoline and quinolone dimers and their biological activities: An overview. |
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| AID523426 | Antiplasmodial activity against Plasmodium falciparum F32-Tanzania assessed as time required to reach 5% parasitaemia at 0.2 uM treated for 48 hrs | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 | Increased tolerance to artemisinin in Plasmodium falciparum is mediated by a quiescence mechanism. |
| AID1373910 | Cytotoxicity against human lymphocytes after 24 to 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
| AID157699 | Antimalarial activity against Plasmodium falciparum D6 in vitro. | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines. |
| AID1808457 | Modulation of full length human NOR1 expressed in SK-N-BE(2) cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1064729 | Cytotoxicity against human WI38 cells after 48 hrs by SRB assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Synthesis, in vitro antimalarial activity and cytotoxicity of novel 4-aminoquinolinyl-chalcone amides. |
| AID355962 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 | 2003 | Journal of natural products, Jun, Volume: 66, Issue:6 | Antimicrobial and antiparasitic (+)-trans-hexahydrodibenzopyrans and analogues from Machaerium multiflorum. |
| AID158197 | In vitro antimalarial activity against Plasmodium falciparum FCR3 | 2003 | Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1 | Synthesis and antimalarial activity of 2-methoxyprop-2-yl peroxides derivatives. |
| AID1161920 | Cytotoxicity against human HepG2 cells assessed as cell death after 48 hrs by Cell Titer-Glo assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18 | Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax. |
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| AID158530 | In vitro antiparasitic activity against chloroquine-sensitive Plasmodium falciparum Haiti 135 | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Parallel solution-phase synthesis of conformationally restricted congeners of pentamidine and evaluation of their antiplasmodial activities. |
| AID1221965 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
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| AID1829854 | Antiplasmodial activity against artemisinin-resistant Plasmodium falciparum Cam 3.1 R539 assessed as growth inhibition by SYBER green 1 dye based fluorescence assay | |||
| AID401065 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected human erythrocytes as [3H]hypoxanthine uptake | 1998 | Journal of natural products, Jun-26, Volume: 61, Issue:6 | Novel quinone methides from Salacia kraussii with in vitro antimalarial activity. |
| AID157698 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1 | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID434586 | Antimalarial activity against Plasmodium falciparum 3D7 | 2009 | European journal of medicinal chemistry, Aug, Volume: 44, Issue:8 | Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation. |
| AID482593 | Antimalarial activity against Plasmodium berghei ANKA infected in NMRI mice (Mus musculus) assessed as host survival time at 100 mg/kg, perorally administered as single dose (Rvb = 6 to 7 days) | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria. |
| AID732346 | Antimalarial activity against erythrocytic stage of chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]-hypoxanthine incorporation incubated for 48 hrs prior to [3H]-hypoxanthine addition measured after 24 hrs b | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID545359 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro. |
| AID731865 | Antimalarial activity against Plasmodium berghei str. ANKA infected in NMRI mouse assessed as mean survival days at 10 mg/kg, po qd for 4 days (Rvb = 7 days) | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID468923 | Selectivity index, ratio of antimicrobial activity against Plasmodium falciparum 3D7 over cytotoxicity against human HEK293 cells | 2009 | Journal of natural products, Aug, Volume: 72, Issue:8 | Antimalarial benzylisoquinoline alkaloid from the rainforest tree Doryphora sassafras. |
| AID469817 | Cytotoxicity against african green monkey Vero cells at 4760 ng/ml after 48 hrs by neutral red dye staining | 2009 | Journal of natural products, Dec, Volume: 72, Issue:12 | Biologically active tetranorditerpenoids from the fungus Sclerotinia homoeocarpa causal agent of dollar spot in turfgrass. |
| AID1203046 | Induction of apoptosis in human H460 cells at 25 to 75 uM after 24 hrs by annexin-V staining-based flow cytometry | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID351792 | Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10 | Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids. |
| AID768183 | Binding affinity to monomeric heme (unknown origin) in MES buffer at pH 5.6 at 1 to 25 uM by UV-visible spectrophotometry | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID247971 | In vitro antimalarial activity against Plasmodium falciparum resistant W-2 | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | Synthesis of novel 10-deoxoartemisinins. |
| AID517478 | Antimalarial activity against chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B infected in human A+ erythrocytes after 72 hrs by SYBR Green I assay | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19 | Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. |
| AID549912 | Inhibition of beta-hematin formation | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis, antiprotozoal, antimicrobial, β-hematin inhibition, cytotoxicity and methemoglobin (MetHb) formation activities of bis(8-aminoquinolines). |
| AID580677 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID620103 | Selectivity index, ratio of GI50 for human HepG2 cells to IC50 for Plasmodium falciparum 3D7 | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities. |
| AID311093 | Hemolytic activity in human erythrocytes at 100 ug/mL after 48 hrs relative to 0.2% saponin | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Transformations of manool. tri- and tetracyclic norditerpenoids with in vitro activity against Plasmodium falciparum. |
| AID1171540 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials. |
| AID1720813 | Inhibition of quorum sensing in violacein-negative Chromobacterium violaceum CV026 mini-Tn5 mutant assessed as quorum quenching by measuring violacein production at 400 uM in presence of C6-HSL relative to control | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16 | Chloroquine fumardiamides as novel quorum sensing inhibitors. |
| AID279387 | Growth inhibition of Plasmodium falciparum HB3 ring stage in infected erythrocytes after 72 hrs in DAPI fluorimetry | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | High-throughput Plasmodium falciparum growth assay for malaria drug discovery. |
| AID1160927 | Antimalarial activity against multi-drug-resistant Plasmodium falciparum W2 infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
| AID1445944 | Cytotoxicity against human HepG2 cells by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally. |
| AID1624383 | Toxicity in Swiss mouse infected with Plasmodium berghei ANKA assessed as change in body weight at 10 mg/kg, ip administered once daily for 5 days measured on 11 days post infection (Rvb = 81%) | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID454712 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as SYBR Green 1 fluorescence emission after 72 hrs | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18 | Synthesis and antimalarial activity of new chloroquine analogues carrying a multifunctional linear side chain. |
| AID1193543 | Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities. |
| AID1673519 | Plasma concentration in NIH mouse infected with Plasmodium chabaudi ASS at 10 mg/kg, po qd for 4 days starting from 4 hrs post-parasite inoculation and measured at 6 hrs post-dosing on day 4 by LC/MS analysis | |||
| AID468921 | Cytotoxicity against human HEK293 cells at 2 uM after 72 hrs by Alamar blue assay | 2009 | Journal of natural products, Aug, Volume: 72, Issue:8 | Antimalarial benzylisoquinoline alkaloid from the rainforest tree Doryphora sassafras. |
| AID1533490 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as lethal effect on heart beat up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID763627 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by MSF assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID256009 | In vitro antimalarial activity for Plasmodium falciparum D6 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives. |
| AID675415 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 ring stage after 72 hrs by SYBP Green fluorescence-based assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Tandem synthesis and in vitro antiplasmodial evaluation of new naphtho[2,1-d]thiazole derivatives. |
| AID158845 | Inhibitory activity against Plasmodium falciparum K1 | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID1859902 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
| AID272304 | Transfection of CDP/plasmid pGL3-CV in HepG2 cells at 200 uM after 48 hrs by luciferase assay | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID436172 | Inhibition of respiration in bovine heart submitochondrial particles assessed as NADH oxidation | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Semisynthesis and antiplasmodial activity of the quinoline alkaloid aurachin E. |
| AID1085762 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hr by plasmodial LDH assay | 2012 | Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Oct, Volume: 21, Issue:10 | Antimicrobial and antiprotozoal activities of secondary metabolites from the fungus Eurotium repens. |
| AID159033 | Concentration required for 50% decrease in IC50 for chloroquine; Not determined | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
| AID539293 | Selectivity index, ratio of IC50 for CHO cells to IC50 of chloroquine-sensitive Plasmodium falciparum D10 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity. |
| AID347211 | Antimalarial schizonticidal activity against Plasmodium falciparum 3D7 infected erythrocytes at 5 ug/ml after 30-39 hrs | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials. |
| AID1201808 | Antimalarial activity against CQ-resistant Plasmodium falciparum W2 assessed as parasite growth inhibition after 48 hrs by YOYO-1 dye based flow cytometry | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Synthesis and in vitro antiplasmodial evaluation of 7-chloroquinoline-chalcone and 7-chloroquinoline-ferrocenylchalcone conjugates. |
| AID522093 | Cmax in Papua new Guinean pregnant women assessed as monodesethychloroquine at 600 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID740948 | Cytotoxicity against african green monkey Vero cells | 2013 | Journal of natural products, Mar-22, Volume: 76, Issue:3 | 8,8-dialkyldihydroberberines with potent antiprotozoal activity. |
| AID1360911 | Cell cycle arrest in human KYSE410 cells assessed as accumulation at G2 phase at 1 uM after 24 to 48 hrs by propidium iodide staining based flow cytometry (Rvb = 12.2%) | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and biological evaluation of novel 2-oxo-1,2-dihydroquinoline-4-carboxamide derivatives for the treatment of esophageal squamous cell carcinoma. |
| AID748224 | Inhibition of heme crystallization to hemozoin | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria. |
| AID221568 | Percent of infected erythrocytes in Blood schizonticidal activity against Plasmodium chabaudi in mice at a concentration of 10 mg/kg/day on day 1 | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
| AID1336738 | Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity. |
| AID1483956 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for erythrocytic stage of Plasmodium falciparum NF54 | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Dioncophyllines C |
| AID158827 | Inhibition of Plasmodium berghei infection in mice (Mus musculus) at 15 mg/kg subcutaneous dose (experiment 2) | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID449274 | Antimalarial activity against Plasmodium falciparum W2mef schizont form by hoechst 33342-thiazole orange stain based flow cytometry assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials. |
| AID1056373 | Antimicrobial activity against mid-ring stage Plasmodium falciparum 3D7 infected in erythrocytes assessed as reduction in trophozoite stage development at 500 nM after 16 to 24 hrs by Giemsa-staining based microscopy relative to control | 2013 | ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11 | Adamantyl derivative as a potent inhibitor of Plasmodium FK506 binding protein 35. |
| AID1174527 | Cytotoxicity against African green monkey Vero cells up to 20 uM after 72 hrs by neutral red assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | 4-Aminoquinoline-pyrimidine hybrids: synthesis, antimalarial activity, heme binding and docking studies. |
| AID1537213 | Antiviral activity against Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells assessed as protection against virus-induced cytopathic effect after 5 days by MTS assay | 2019 | Journal of natural products, 02-22, Volume: 82, Issue:2 | Antiviral Compounds from Codiaeum peltatum Targeted by a Multi-informative Molecular Networks Approach. |
| AID360366 | Antimalarial activity after 96hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake | 2007 | The Journal of biological chemistry, Jan-26, Volume: 282, Issue:4 | In vitro efficacy, resistance selection, and structural modeling studies implicate the malarial parasite apicoplast as the target of azithromycin. |
| AID278586 | Reduced apicoplast DNA/nuclear DNA ratio in Plasmodium falciparum FCK2 at 100 nM after 72 hrs by competitive PCR | 2007 | Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1 | Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum. |
| AID1764062 | Selectivity index, ratio of CC50 for cytotoxicity against HUVEC cells to IC50 for antileishmanial activity against axenic amastigote form of Leishmania donovani LV9 | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Anti-protozoal and anti-fungal evaluation of 3,5-disubstituted 1,2-dioxolanes. |
| AID570296 | Antiplasmodial activity against chloroquine-sensitive, mefloquine-resistant ring stage Plasmodium falciparum D6 infected in human red blood cells after 48 hrs | 2011 | Journal of medicinal chemistry, Feb-10, Volume: 54, Issue:3 | Incorporation of basic side chains into cryptolepine scaffold: structure-antimalarial activity relationships and mechanistic studies. |
| AID1880209 | Selectivity index, ratio of CC50 for cytotoxicity against HEL 299 cells to EC50 for antiviral activity against HCoV-229E infected in HEL 299 cells | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
| AID656213 | Antiplasmodial activity against Plasmodium falciparum W2 infected in human erythrocytes | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8 | Phosphonium lipocations as antiparasitic agents. |
| AID1649917 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Triazole derivatives and their antiplasmodial and antimalarial activities. |
| AID444053 | Renal clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID284273 | Antimicrobial activity against Mycobacterium intracellular | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID311934 | Dissociation constant, pKa of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
| AID1229881 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 12 post infection by Giemsa st | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID1181599 | Antimicrobial activity against erythrocytic stage of Plasmodium falciparum NF54 infected in human washed RBC assessed as [3H]-hypoxanthine incorporation incubated for 48 hrs prior to [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei. |
| AID401643 | Antiplasmodial activity against Plasmodium berghei ANKA S infected NMRI mice (Mus musculus) as reduced parasitaemia at 50 mg/kg subcutaneous dose for 4 days | 2005 | Journal of natural products, May, Volume: 68, Issue:5 | Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound. |
| AID737064 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum ItG after 72 hrs by lactate dehydrogenase assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Antimalarial activities of 6-iodouridine and its prodrugs and potential for combination therapy. |
| AID1439847 | Antiplasmodial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity. |
| AID1883294 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR3 assessed as parasite growth inhibition and measured after 72 hrs by ELISA | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Sattahipmycin, a Hexacyclic Xanthone Produced by a Marine-Derived |
| AID417168 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by SYBR green assay | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Antiproliferative and antimalarial anthraquinones of Scutia myrtina from the Madagascar forest. |
| AID765718 | Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
| AID549607 | Antimalarial activity against mefloquine-resistant, chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine uptake | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones. |
| AID1359613 | Antiplasmodial activity against Plasmodium berghei ANKA infected in mouse assessed as mouse survival time at 3 mg/kg/day, po for 4 consecutive days starting from 2 hrs post infection by MSF assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID396984 | Antimalarial activity as survival at day 4 in Peter's assay against Plasmodium berghei ANKA infected NIH mice (Mus musculus) at 25 mg/kg intraperitoneal dose 2 hrs post infection then daily for 4 days | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities. |
| AID656018 | Antagonist activity at TLR7 in human PBMC assessed as inhibition of gardiquimod-induced IL-1beta release after 12 hrs by bead array assay | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Toll-like receptor (TLR)-7 and -8 modulatory activities of dimeric imidazoquinolines. |
| AID1457198 | Antimalarial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival rate at 30 mg/kg administered once daily via oral gavage for 4 consecutive days beginning 1 hr after infection measured from day 4 to day 20 post i | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID152000 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 Sierra Leone | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20 | Structure-activity relationships of the antimalarial agent artemisinin. 8. design, synthesis, and CoMFA studies toward the development of artemisinin-based drugs against leishmaniasis and malaria. |
| AID1439510 | Antimalarial activity against Plasmodium falciparum | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Novel 2,3-disubstituted quinazoline-4(3H)-one molecules derived from amino acid linked sulphonamide as a potent malarial antifolates for DHFR inhibition. |
| AID1247015 | Selectivity index, ratio of EC50 for human HepG2A16 cells to EC50 for chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocyte | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype. |
| AID436268 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Bioactive diterpenes and other constituents of Croton steenkampianus. |
| AID93346 | The compound was tested for survival of the ICR mice (infected with Plasmodium berghei) as a symptom indicative of toxicity on day 4, at a dose of 0.1 mg/kg/day | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID117998 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium berghei N. activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4-day test at a concentration of 10 mg/kg in experiment 1 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID667439 | Antiplasmodial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as decrease in parasitemia measured on day 3 post-treatment by geimsa staining (Rvb = 2.18 +/- 0.17%) | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain. |
| AID768460 | Antimalarial activity against mid to late trophozoite stage of Plasmodium falciparum 3D7 infected in RBC assessed as abnormal mitochondria at 200 uM after 0.5 hrs by MitoTracker Red CMXRos-based fluorescence microscopic analysis relative to untreated cont | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID286712 | Ratio of EC50 for rat L6 cells to EC50 for Plasmodium falciparum K1 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and antimalarial property of orally active phenoxazinium salts. |
| AID461605 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss Webster mice (Mus musculus) assessed as average parasitaemia at 200 mg/kg, perorally administered 1 day after infection measured after 10 days post infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID585011 | Antimalarial activity against Plasmodium ovale trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia. |
| AID673147 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase of mouse survival at 30 mg/kg, po administered 24 hrs post infection (Rvb = 6 to 7 days) | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
| AID1808483 | Modulation of Gal4-fused VP16 expressed in SKNBE(2) cells co-transfected with UAS repoter gene assessed as decrease in luciferase activity at 125 uM incubated for 18 hrs by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID157680 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
| AID666491 | Antibacterial activity against Streptococcus pyogenes isolate 3565 by broth microdilution method | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
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| AID419114 | Antimalarial activity as minimal concentration for parasite elimination at day 23 against Plasmodium yoelii 17X peroral inoculated CD1 mice (Mus musculus) dosed 1 hrs post infection then daily for 4 days | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID1676922 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in microbial growth after 72 hrs by SYBR green I staining based fluorescence assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines. |
| AID384957 | Antimalarial activity against Plasmodium falciparum T9-96 infected Rhesus positive human erythrocytes by [3H]hypoxanthine uptake | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9 | Synthesis and structure-activity relationships of 4-pyridones as potential antimalarials. |
| AID1433141 | Antiviral activity against Coxsackievirus B4 infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID1815837 | Selectivity index, ratio of LD50 for cytotoxicity against Chinese hamster V79 cells to IC50 for antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Indole-Containing Pyrazino[2,1- |
| AID119887 | In vivo antimalarial activity against Plasmodium yoelii in mice (Mus musculus) at 48 mg/kg/day orally on day 4 expressed as percent suppression | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2 | Orally active amino functionalized antimalarial 1,2,4-trioxanes. |
| AID441655 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities. |
| AID419183 | Distribution coefficient, log D at pH 7.4 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID524787 | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by 96-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID400318 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs as LDH activity by Makler assay | 1996 | Journal of natural products, Jan, Volume: 59, Issue:1 | A new quassinoid from Castela texana. |
| AID730533 | Selectivity index, ratio of CC50 for african green monkey Vero C1008 cells to IC50 for Plasmodium falciparum 3D7 | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Synthesis and insight into the structure-activity relationships of chalcones as antimalarial agents. |
| AID1431584 | Antimalarial activity against synchronous culture of Plasmodium falciparum 3D7 ring stage parasite infected in human erythrocytes incubated for 3 hrs followed by compound wash out and measured after 24 hrs by NanoGlo-reagent based bioluminescence assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity. |
| AID1167707 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by Malaria SYBR Green I-nucleic acid staining based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis of chiral chloroquine and its analogues as antimalarial agents. |
| AID278900 | Inhibition of Tween 20-induced beta-hematin formation by colorimetric assay | 2007 | Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1 | Simple colorimetric inhibition assay of heme crystallization for high-throughput screening of antimalarial compounds. |
| AID1720811 | Inhibition of quorum sensing system in Chromobacterium violaceum ATCC 31532 assessed as reduction in violacein production at 400 uM relative to control | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16 | Chloroquine fumardiamides as novel quorum sensing inhibitors. |
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| AID538443 | Antimalarial activity against Plasmodium falciparum NF 54 assessed as inhibition of maturation into schizont stage after 36 to 40 hrs | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents. |
| AID1199044 | Cytotoxicity against African green monkey Vero cells assessed as inhibition of overall cell metabolism after 6 to 7 days by MTS assay | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID84652 | Inhibitory activity against proliferation of HTLV-1 transformed cell lines (HUT-102) at 10 uM; ND = Not determined | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Biological evaluation of substituted quinolines. |
| AID522097 | AUC (0 to infinity) in Papua new Guinean pregnant women assessed as monodesethychloroquine at 600 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID673592 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as [3H]hypoxanthine incorporation after 48 hrs | 2012 | Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15 | Short synthesis and antimalarial activity of fagaronine. |
| AID358248 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 by LDH reporter assay | 2001 | Journal of natural products, Oct, Volume: 64, Issue:10 | Antimalarial (+)-trans-hexahydrodibenzopyran derivatives from Machaerium multiflorum. |
| AID611741 | Cytotoxicity against mouse macrophage J774 cells at 19 uM after 24 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Synthesis and antimalarial activity of new heterocyclic hybrids based on chloroquine and thiazolidinone scaffolds. |
| AID1808278 | Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID573270 | Drug uptake in human RBC at 50 uM in absence of 10 um ferriprotoporphyrin 9 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID497156 | Antimalarial activity against Plasmodium vinckei petteri infected in CD mice (Mus musculus) assessed as inhibition of parasitaemia at 1 mg/kg, intraperitoneal daily for 4 days measured on day 5 | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15 | 1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs. |
| AID1624381 | Toxicity in Swiss mouse infected with Plasmodium berghei ANKA assessed as change in body weight at 10 mg/kg, ip administered once daily for 5 days measured on 7 days post infection (Rvb = 89%) | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID515029 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mice (Mus musculus) assessed as parasitaemia level at 30 mg/kg, perorally administered as single dose measured after 3 days relative to control | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID1494327 | Induction of cell proliferation in C57BL/6 mouse hippocampal neurons in CA3 region assessed as BrdU-incorporation at 0.5 uL/hr, icv for 7 days by immunohistochemical analysis (Rvb = 1.4%) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID381965 | Antiparasitic activity as survival days against chloroquine-sensitive Plasmodium berghei ANKA infected NIH mice (Mus musculus) at 20 mg/kg intraperitoneal dose | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs. |
| AID671317 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FLD-B assessed as inhibition of total parasite growth | 2012 | Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13 | Morita-Baylis-Hillman adducts: biological activities and potentialities to the discovery of new cheaper drugs. |
| AID1829879 | Selectivity ratio of IC50 for anticancer activity against human L02 cells to IC50 for anticancer activity against human HepG2 cells | |||
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| AID725845 | Antimalarial activity against Plasmodium falciparum 3D7 after 3 days by SYBR green I assay | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Antimalarial and Structural Studies of Pyridine-containing Inhibitors of 1-Deoxyxylulose-5-phosphate Reductoisomerase. |
| AID372461 | Antimalarial activity as 2nd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs by flow cytometry | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast. |
| AID540236 | Phospholipidosis-positive literature compound observed in human | |||
| AID736791 | Antileishmanial activity against Leishmania infantum MHOM/BR/1972/LD promastigotes after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators. |
| AID449197 | Antimalarial activity against Plasmodium falciparum W2mef by hypoxanthine uptake assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials. |
| AID509453 | Antiproliferative activity against human p53, pRB mutant and estrogen receptor deficient MDA-MB-231 cells after 48 hrs by SRB assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of chloroquine analogs with anti-breast cancer property. |
| AID519195 | Antimicrobial activity against Plasmodium vivax trophozoites measured after 30 hrs by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID227387 | Antiplasmodial potency relative to chloroquine | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | The imidazo[2,1-a]isoindole system. A new skeletal basis for antiplasmodial compounds. |
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| AID151221 | In vitro growth inhibition of Plasmodium falciparum FcB1R | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Antiplasmodial activity and cytotoxicity of bis-, tris-, and tetraquinolines with linear or cyclic amino linkers. |
| AID519191 | Antimicrobial activity against Plasmodium falciparum at the ring stage by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID1353870 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. |
| AID333070 | Antimalarial activity against Plasmodium falciparum D6 | 2004 | Journal of natural products, Aug, Volume: 67, Issue:8 | Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases. |
| AID504265 | Cytotoxicity against HMEC1 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID1241107 | Cytotoxicity against CHO cells by MTT assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. |
| AID1494360 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as time spent in effective region at 30 mg/kg/day, po for 80 days by Morris water maze test (Rvb = 9.0 +/- 3.8 sec) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID247035 | Effective dose against chloroquine-resistant, pyrimethamine-resistant, mefloquine-resistant Plasmodium falciparum Dd2 | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11 | Protein farnesyltransferase inhibitors exhibit potent antimalarial activity. |
| AID1633704 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as suppression in parasitemia at 33.3 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 7 post infection relative to untreated control | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID1353869 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by LDH release assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity. |
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| AID1445952 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mouse assessed as reduction in parasitemia at 30 mg/kg, po administered at 4, 24, 48, 72 hrs post infection measured on day 4 by Peter's test relative to control | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally. |
| AID377917 | Antiplasmodial activity against Plasmodium falciparum K1 in human erythrocytes by [3H]hypoxanthine uptake | 2000 | Journal of natural products, Nov, Volume: 63, Issue:11 | Ancistroealaines A and B, two new bioactive naphthylisoquinolines, and related naphthoic acids from Ancistrocladus ealaensis. |
| AID480218 | Antimalarial activity against Plasmodium falciparum W2 by FACS assay | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID1201512 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 72 hrs by SYBR Green I dye-based fluorescence assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID482597 | Antimalarial activity against Plasmodium berghei ANKA infected in NMRI mice (Mus musculus) assessed as host survival time at 30 mg/kg, perorally administered once daily for 3 days (Rvb = 6 to 7 days) | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria. |
| AID1628558 | Resistance index, ratio of IC50 for CQ-resistant Plasmodium falciparum K1 infected in human type O+ erythrocytes to IC50 for CQ-sensitive Plasmodium falciparum NF54 infected in human type O+ erythrocytes | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
| AID621151 | Antimalarial activity against Plasmodium falciparum K1 at pH 7.4 by microplate assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives. |
| AID1125529 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR-3 assessed as growth inhibition | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | The chemistry and biology of febrifugine and halofuginone. |
| AID1894270 | Antiplasmodial activity against Plasmodium falciparum NF54 expressing transgenic luciferase assessed as parasite kill rate at trophozoite stage incubated for 6 hrs by bioluminescence relative rate of kill (BRRoK) assay | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID284274 | Antifungal activity against Aspergillus fumigatus | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Antiprotozoal and antimicrobial activities of O-alkylated and formylated acylphloroglucinols. |
| AID1462233 | Selectivity ratio of IC50 for Plasmodium falciparum Dd2 to IC50 for Plasmodium falciparum 3D7 | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | Synthesis of antimalarial amide analogues based on the plant serrulatane diterpenoid 3,7,8-trihydroxyserrulat-14-en-19-oic acid. |
| AID597501 | Antimalarial activity against Plasmodium berghei NK-65 infected in ICR mouse assessed as survival days at 100 mg/kg, po administered as single dose (Rvb = 6 days) | 2010 | ACS medicinal chemistry letters, Oct-14, Volume: 1, Issue:7 | Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria. |
| AID1155330 | Cytotoxicity against human HepG2 cells after 48 hrs | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
| AID617828 | Antimalarial activity against chloroquine-resistant and mefloquine-sensitive Plasmodium falciparum W2 | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against Plasmodium falciparum. |
| AID1306835 | Inhibition of beta-hematin formation in acetate solution at pH 4.5 measured after 60 mins by pyridine-based spectrophotometric assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Bistacrine derivatives as new potent antimalarials. |
| AID1355325 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as reduction in parasitemia at 20 mg/kg, ip administered for 3 consecutive days post infection measured on day 7 post infection relative to control | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
| AID562553 | Antiplasmodial activity against Plasmodium vinckei petteri infected in po dosed CD mouse assessed as mean survival time at 10 mg/kg/day, ip for 4 days measured upto day 21 post-infection | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID157870 | Growth inhibition of chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Antimalarial activity of ferrocenyl chalcones. |
| AID663064 | Antimalarial activity against Plasmodium berghei KBG173 infected in mouse assessed as decrease in parasitemia at 1.25 mg/kg, ip BID administered on day 3, 4 and 5 post infection measured on day 31 relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin. |
| AID158683 | In vitro inhibitory activity against multidrug-resistant Plasmodium falciparum W2 Indochina | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1433139 | Antiviral activity against Adenovirus infected in human HEL cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID337524 | Cytotoxicity against human KB cells after 3 days by sulforhodamine B assay | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1808273 | Modulation of full length human Nurr1 expressed in SKNBE(2) cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1156603 | Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups. |
| AID406402 | Toxicity in Plasmodium vinckei petteri infected CD mice (Mus musculus) assessed as mortality at 1 mg/kg/day, intraperitoneally measured on day 1 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID1228728 | Antiviral activity against Sindbis virus strain HRsp infected in african green monkey Vero cells assessed as inhibition of virus induced cell death measured after 7 days | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID1140206 | Antimalarial activity against erythrocytic stage of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis, β-haematin inhibition, and in vitro antimalarial testing of isocryptolepine analogues: SAR study of indolo[3,2-c]quinolines with various substituents at C2, C6, and N11. |
| AID247016 | Effective dose required to reduce the parasitemia in mice when compound administered with Tween-80 after 3 day postinfection | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. |
| AID1533537 | Induction of lysosomotropism in human HeLa cells infected with Ebolavirus assessed as increase in lysosome concentration in juxtanuclear region at 10 uM for 2 hrs by acridine orange staining based assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
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| AID768177 | Binding affinity to calf thymus DNA at 30 uM by fluorescence assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
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| AID158383 | In vitro antimalarial activity for Plasmodium falciparum HB3 | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
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| AID212376 | Compound was tested for antimalarial activity in mice (Mus musculus), infected with Plasmodium berghei N., activity is expressed as the mortality rate at a concentration of 1 mg/kg. in experiment 1; 5 out of 5 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
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| AID1373921 | Induction of apoptosis in human Jurkat E6-1 cells assessed as late apoptotic cells at 100 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 0.73 +/- 0.14 %) | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
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| AID159175 | Percent reversal against Plasmodium falciparum W2 at 1 uM DEEA | 2002 | Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15 | Synthesis and effects on chloroquine susceptibility in Plasmodium falciparum of a series of new dihydroanthracene derivatives. |
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| AID619752 | Antimalarial activity against transgenic Plasmodium falciparum 3D7 infected in human A positive erythrocytes after 72 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs. |
| AID1738751 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | Synthesis and biological evaluation of novel quinoline-piperidine scaffolds as antiplasmodium agents. |
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| AID1859903 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
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| AID1486840 | Inhibition of bovine liver DHFR pre-incubated 2 mins before dihydrofolic acid substrate addition and measured over 10 mins in presence of NADPH | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | 1,2,4-Triazole and 1,3,4-oxadiazole analogues: Synthesis, MO studies, in silico molecular docking studies, antimalarial as DHFR inhibitor and antimicrobial activities. |
| AID225003 | In vivo antimalarial activity against Plasmodium chabaudi in mice (Mus musculus) and its survival was reported | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
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| AID595215 | Antimalarial activity against Plasmodium falciparum W2 | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus. |
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| AID1140750 | Inhibition of Clostridium botulinum recombinant BoNT/A light chain using N-terminal acetylated, C-terminal aminated SNAP-25 (187-203) as substrate at 20 uM by reverse-phase HPLC analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Second generation steroidal 4-aminoquinolines are potent, dual-target inhibitors of the botulinum neurotoxin serotype A metalloprotease and P. falciparum malaria. |
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| AID1808472 | Modulation of full length human Nur77 expressed in PC12 cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
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| AID1126850 | Cytotoxicity against human MCF7 cells after 48 hrs by XTT reduction assay | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | 2-Aryl-3H-indol-3-ones: synthesis, electrochemical behaviour and antiplasmodial activities. |
| AID1533498 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as teratogenic effect by measuring effect on blood circulation up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
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| AID628227 | Antimalarial activity against chloroquine- and mefloquine-resistant Plasmodium falciparum W2-Mef infected in human O-positive erythrocytes after 48 hrs | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | 3-bromohomofascaplysin A, a fascaplysin analogue from a Fijian Didemnum sp. ascidian. |
| AID1457210 | Antimalarial activity against Plasmodium falciparum TM90C2B infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation count | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
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| AID1883295 | Cytotoxicity against human MRC5 cells assessed as cell growth inhibition and measured after 2 days by WST-8 assay | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Sattahipmycin, a Hexacyclic Xanthone Produced by a Marine-Derived |
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| AID382483 | Antimalarial activity as increased MST in Plasmodium berghei ANKA 65 infected Swiss CD1 at 10 mg/kg initial oral followed by intraperitoneal dose after 4 days | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2 | Synthesis and antimalarial activity of new analogues of amodiaquine. |
| AID525168 | Antimicrobial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mice (Mus musculus) at 2.5 mg/kg, perorally administered after 72 hrs post inoculation measured on day 4 post infection | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
| AID754535 | Inhibition of hemozoin formation in 0.5 M acetate buffer at pH 4.8 after 12 hrs by microtiter plate-based high-throughput assay in presence of trophozoite lysate | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID1204840 | Cytotoxicity against pig LLC-PK1 cells assessed as cell growth inhibition after 48 hrs by neutral red assay | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID1439477 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 infected in red blood cells | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Synthesis, antimalarial activity, heme binding and docking studies of N-substituted 4-aminoquinoline-pyrimidine molecular hybrids. |
| AID1865619 | Antiparasitic activity against Plasmodium falciparum 3D7 infected in erythrocytes assessed as inhibition of parasite growth at 50 uM incubated for 48 hrs by SYBR Green I dye based fluorescence assay relative to control | 2022 | Journal of natural products, 12-23, Volume: 85, Issue:12 | Dactylosporolides: Glycosylated Macrolides from |
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| AID247908 | In vitro antimalarial activity against Plasmodium falciparum (Ghana) | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10 | Synthesis of novel 10-deoxoartemisinins. |
| AID576572 | Antimalarial activity against Plasmodium falciparum trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax. |
| AID151062 | In vivo antimalarial activity against Plasmodium berghei infected mice (Mus musculus) at 160 mg/kg | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11 | Bisquinolines. 1. N,N-bis(7-chloroquinolin-4-yl)alkanediamines with potential against chloroquine-resistant malaria. |
| AID1676950 | Inhibition of beta-hematin formation at 12.5 to 200 uM after 16 hrs by inverted microscopic analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Synthesis, Structure-Activity Relationship, and Antimalarial Efficacy of 6-Chloro-2-arylvinylquinolines. |
| AID322132 | In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. |
| AID675401 | Aqueous solubility of the compound in phosphate buffer at pH 5.5 after 24 hrs by HPLC analysis | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | Synthesis and in vitro antimalarial activity of a series of bisquinoline and bispyrrolo[1,2a]quinoxaline compounds. |
| AID678038 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 by SYBR green I-based assay | 2012 | Journal of natural products, Jul-27, Volume: 75, Issue:7 | Busseihydroquinones A-D from the roots of Pentas bussei. |
| AID427684 | Selectivity index, ratio of IC50 for human K562 cells to IC50 for chloroquine, pyrimethamine and proguanil-resistant Plasmodium falciparum W2 | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines. |
| AID393074 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Pharmacodynamics and pharmacokinetics studies of phenoxazinium derivatives for antimalarial agent. |
| AID105835 | Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 25 uM concentration | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID412369 | Cytotoxicity against PHA-stimulated human lymphocytes by MTT assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID635308 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2mef infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by beta liquid scintillation counting method | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives. |
| AID558054 | Antimicrobial activity against Plasmodium falciparum harboring SVMNT genotype after 72 hrs by SYBR green I assay | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Dynamics of malaria drug resistance patterns in the Amazon basin region following changes in Peruvian national treatment policy for uncomplicated malaria. |
| AID734226 | In vitro antimalarial activity against ring stage of chloroquine-resistant Plasmodium falciparum W2 cultured in medium containing 10% human serum assessed as inhibition of parasite growth after 48 hrs by YOYO-1 dye based flow cytometry | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Azide-alkyne cycloaddition en route to 1H-1,2,3-triazole-tethered 7-chloroquinoline-isatin chimeras: synthesis and antimalarial evaluation. |
| AID479487 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by flow-cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID1433140 | Antiviral activity against Vesicular stomatitis virus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID282996 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum 3D7 in erythrocytes | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate. |
| AID1176092 | Selectivity index, ratio of IC50 for HMEC1 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Clofazimine analogs with antileishmanial and antiplasmodial activity. |
| AID1639283 | Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Acrotrione: An Oxidized Xanthene from the Roots of Acronychia pubescens. |
| AID395328 | Lipophilicity, log P of the compound | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID442257 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID159899 | Effective subcutaneous dose ED50 against Plasmodium yoelii sspNS | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID406389 | Selectivity index ratio of IC50 for human MCF7 cells to IC50 for chloroquine-resistant Plasmodium falciparum FcB1 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID703715 | Resistance ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum NF54 | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1732392 | Antimalarial activity against Plasmodium falciparum D10 by parasite lactate dehydrogenase assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity. |
| AID1188458 | Antimalarial activity against tightly synchronized Plasmodium falciparum K1 assessed as parasite stage accumulation index at trophozoites stages at 10 uM treated at 18 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cyt | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID1524691 | Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as reduction in CD3+ cell level in brain at 10 mg/kg, po administered for 4 days measured on day 10 by flow cytometry | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | Efficacy of TLR7 agonistic imidazoquinoline as immunochemotherapeutic agent against P. Berghei ANKA infected rodent host. |
| AID406712 | Toxicity in Plasmodium vinckei petteri infected CD mice (Mus musculus) assessed as mortality at 10 mg/kg/day, intraperitoneally measured on day 15 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID580317 | Inhibition of beta-hematin formation assessed as inhibition of flavoprotein polymerization at 5 to 100 mM after 48 hrs | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents. |
| AID1433127 | Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation by Coulter counter analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID558825 | Antimicrobial activity against Plasmodium falciparum 3D7 by DAPI growth inhibition assay | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Colorimetric high-throughput screen for detection of heme crystallization inhibitors. |
| AID1124791 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected after 72 hrs by Malaria SYBR Green I-staining based fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7 | Synthesis and evaluation of new diaryl ether and quinoline hybrids as potential antiplasmodial and antimicrobial agents. |
| AID736788 | Selectivity index, ratio of GI50 for human HL60 cells to GI50 for Trypanosoma cruzi trypomastigotes | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators. |
| AID1176087 | Antileishmanial activity against Leishmania tropica MHOM/IT/2012/ISS3130 promastigotes assessed as inhibition of parasite growth after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Clofazimine analogs with antileishmanial and antiplasmodial activity. |
| AID1434597 | Inhibition of Escherichia coli DNA topisomerase-1 assessed as reduction in enzyme-mediated relaxation of supercoiled pBlueScript 2 KS+ DNA substrate at 100 uM after 1 hr by agarose gel electrophoresis method | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3 | Synthesis and biological evaluation of naphthoquinone-coumarin conjugates as topoisomerase II inhibitors. |
| AID732424 | Antimalarial activity against Plasmodium falciparum K1 assessed as inhibition of [3H] hypoxanthine uptake by liquid scintillation counting | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1 | Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives. |
| AID1433138 | Antiviral activity against acyclovir-resistant TK-negative Herpes simplex virus 1 KOS infected in human HEL cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID1587111 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation pretreated for 24 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by | 2019 | ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1 | Synthesis, Profiling, and in Vivo Evaluation of Cyclopeptides Containing |
| AID453386 | Selectivity index, ratio of TC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum W2 | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers. |
| AID732335 | Antimalarial activity against Plasmodium berghei str. ANKA infected in NMRI mouse assessed as reduction in parasitemia at 100 mg/kg, po qd for 4 days measured on day 4 by FACS analysis relative to control | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID1402366 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in red blood cells incubated for 72 hrs by parasite LDH release based colorimetric assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Bioactive products from singlet oxygen photooxygenation of cannabinoids. |
| AID1433123 | Antimalarial activity against chloroquine-resistant asexual intraerythrocytic stage of Plasmodium falciparum Dd2 assessed as inhibition of parasite growth by lactate dehydrogenase assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID158032 | Effective concentration for gametocidal activity against Plasmodium falciparum FDL-HD; No data | 2002 | Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24 | Isolation and antimalarial activity of peroxydisulfate oxidation products of primaquine. |
| AID1808451 | Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as decrease in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by luciferase reporter gene | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1291843 | Selectivity index, ratio of MLD50 for African green monkey BGM cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | New pentasubstituted pyrrole hybrid atorvastatin-quinoline derivatives with antiplasmodial activity. |
| AID72859 | In vitro inhibitory concentration against ferriprotoporphyrin in biomineralisation assay (FBIT) | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | The imidazo[2,1-a]isoindole system. A new skeletal basis for antiplasmodial compounds. |
| AID1466469 | Anti-plasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes after 50 hrs by SYBR green dye based fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Synthesis and evaluation of anti-plasmodial and cytotoxic activities of epoxyazadiradione derivatives. |
| AID1649414 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
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| AID382113 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by LDH reporter assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Structural insights into the Plasmodium falciparum histone deacetylase 1 (PfHDAC-1): A novel target for the development of antimalarial therapy. |
| AID159766 | In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum W2 Indochina | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Mixed steroidal 1,2,4,5-tetraoxanes: antimalarial and antimycobacterial activity. |
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| AID333756 | Antiplasmodial activity against Plasmodium falciparum K1 | 2004 | Journal of natural products, Dec, Volume: 67, Issue:12 | Ancistrobenomine a, the first naphthylisoquinoline oxygenated at Me-3, and related 5,1'-coupled alkaloids, from the "new" plant species ancistrocladusbenomensis. |
| AID285470 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum Nigeria | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
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| AID88264 | Hematin binding affinity of compound was determined as a measure of inhibiting hematin polymerization | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Carbon isosteres of the 4-aminopyridine substructure of chloroquine: effects on pK(a), hematin binding, inhibition of hemozoin formation, and parasite growth. |
| AID318195 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 by [3H]hypoxanthine incorporation | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID711163 | Antimalarial activity against Plasmodium falciparum K1 infected in human O positive erythrocytes under low oxygen atmosphere after 72 hrs by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors. |
| AID93351 | The compound was tested for survival of the ICR mice (infected with Plasmodium berghei) as a symptom indicative of toxicity on day 4, at a dose of 2 mg/kg/day | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID1373372 | Antiviral activity against Chikungunya virus Indian Ocean 889 infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTS/PMS method | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents. |
| AID159840 | Compound was evaluated for its antimalarial activity in vitro on Plasmodium falciparum | 2002 | Bioorganic & medicinal chemistry letters, Aug-19, Volume: 12, Issue:16 | Antimalarial compounds from Parinari capensis. |
| AID1204117 | Cytotoxic activity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID152132 | In vitro antimalarial activity against Plasmodium falciparum FCR3 | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20 | Metabolites of febrifugine and its synthetic analogue by mouse liver S9 and their antimalarial activity against Plasmodium malaria parasite. |
| AID1275775 | Selectivity index, ratio of IC50 for CHO cells to IC50 for chloroquine sensitive Plasmodium falciparum NF54 | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
| AID480240 | Hepatotoxicity in Sprague-Dawley rat hepatocytes after 20 to 24 hrs by MTT assay | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
| AID768716 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei NK-173 infected in Swiss albino mouse assessed as quantal survival at 51.5 mg/kg, ip administered 4 times per day for 3 days measured on day 14 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives. |
| AID1504885 | Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12 | Pimentelamines A-C, Indole Alkaloids Isolated from the Leaves of the Australian Tree Flindersia pimenteliana. |
| AID1199048 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Sindbis virus HRsp infected in African green monkey Vero cells | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6 | Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID1624368 | Antimalarial activity against Plasmodium berghei ANKA infected in Swiss mouse assessed as suppression of parasitaemia at 10 mg/kg, ip administered once daily for 5 days measured on 4 days post infection by flow cytometry relative to control | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID352675 | Antiplasmodial activity as inhibition of beta-hematin against Plasmodium yoelii N67 infected Swiss mice (Mus musculus) erythrocytes | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9 | Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials. |
| AID123189 | Number of Plasmodium berghei infected mice died on day 16 at 40 mg/kg | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines. |
| AID764879 | Antiprotozoal activity against bloodstream form of chloroquine- and pyrimethamine-resistant Plasmodium falciparum K1 infected in NMRI mouse assessed as mean survival time at 50 mg/kg, ip qd for administered 3 days post-inoculation for 4 consecutive days ( | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom. |
| AID515050 | Drug level in NMRI mice (Mus musculus) erythrocytes infected with chloroquine-resistant Plasmodium falciparum Dd2 after 1 hr | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID726099 | Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP-Luc infected in HuH7 cells incubated at 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured after 48 hrs by Alamar blue assay | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | In vitro efficiency of 9-(N-cinnamoylbutyl)aminoacridines against blood- and liver-stage malaria parasites. |
| AID1780630 | Antileishmanial activity against Leishmania infantum (MHOM/TN/80/IPTI) promastigotes assessed as reduction in parasite viability measured after 72 hrs by MTT assay | 2021 | ACS medicinal chemistry letters, Nov-11, Volume: 12, Issue:11 | Development of Potent 3-Br-isoxazoline-Based Antimalarial and Antileishmanial Compounds. |
| AID1247274 | Antimalarial activity against Plasmodium berghei NK65 infected in BALB/c mouse assessed as mean survival time at 5 mg/kg, po qd for 4 days (Rvb = 22 +/- 3 days) | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents. |
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| AID1255358 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by microculture radioisotope technique | 2015 | Journal of natural products, Oct-23, Volume: 78, Issue:10 | Antimalarial and Antiproliferative Cassane Diterpenes of Caesalpinia sappan. |
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| AID377198 | Antiplasmodial activity against Plasmodium falciparum NF54 | 2000 | Journal of natural products, Aug, Volume: 63, Issue:8 | Pelorol from the tropical marine sponge Dactylospongia elegans. |
| AID600551 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H] hypoxanthine incorporation after 24 hrs by scintillation counting | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Antiprotozoal activity of chloroquinoline based chalcones. |
| AID780245 | Resistant index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | New route to the 5-((arylthio- and heteroarylthio)methylene)-3-(2,2,2-trifluoroethyl)-furan-2(5H)-ones--key intermediates in the synthesis of 4-aminoquinoline γ-lactams as potent antimalarial compounds. |
| AID1593252 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in human erythrocytes by SYBR green 1-based fluorescence assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials. |
| AID1059805 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12 | Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds. |
| AID477942 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum PA infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
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| AID400306 | Cytotoxicity against human K562 cells after 2 to 7 days by neutral red assay | 1996 | Journal of natural products, Jan, Volume: 59, Issue:1 | A new quassinoid from Castela texana. |
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| AID407144 | Antiplasmodial activity against Plasmodium falciparum 3D7 | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13 | Sucutiniranes A and B, new cassane-type diterpenes from Bowdichia nitida. |
| AID221570 | Percent of infected erythrocytes in Blood schizonticidal activity against Plasmodium chabaudi in mice at a concentration of 10 mg/kg/day on day 3 | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
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| AID553555 | Toxicity in malaria patient assessed as diarrhea on day 1 after treatment at quartile 1 of compound concentration | 2009 | Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1 | Chloroquine is grossly overdosed and overused but well tolerated in Guinea-bissau. |
| AID247005 | Effective dose required to reduce the parasitemia in mice when compound administered with SSV after 3 day postinfection | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. |
| AID1894311 | Inhibition of hemozoin formation in sorbitol-synchronized early ring stage plasmodium falciparum NF54 trophozoites assessed as decrease in free hemozoin level at 0.5 to 3 times EC50 incubated for 32 hrs by flow cytometry analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in |
| AID1664911 | Antimalarial activity against CQ-resistant Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by SYBR Green1 dye based fluorescence assay | 2020 | ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7 | Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity. |
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| AID1915904 | Inhibition of hemozoin formation in sorbitol-synchronized early ring stage plasmodium falciparum NF54 trophozoites assessed as reduction in hemozoin level at 1 to 2.5 times IC50 incubated for 28 hrs by flow cytometry analysis | |||
| AID113169 | In vivo antimalarial activity in mice (Mus musculus) against chloroquine-sensitive Plasmodium berghei N after oral administration | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides. |
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| AID419682 | Antibacterial activity against intraerythrocytic form of Plasmodium falciparum | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase. |
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| AID319196 | Antimalarial activity against Plasmodium falciparum GC03 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles. |
| AID544213 | Antiplasmodial activity against Plasmodium falciparum F32 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | In vitro and in vivo properties of ellagic acid in malaria treatment. |
| AID509188 | Inhibition of TLR7-mediated IFN-gamma production in aldrithiol-2-treated HIV1 MN-stimulated human PBMC after 20 hrs by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID274296 | Antiprotozoal activity against chloroquine-sensitive Plasmodium falciparum | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
| AID673143 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as reduction of parasite level in blood at 30 mg/kg, po administered 24 hrs post infection measured after 72 hrs post infection by flow cytometry | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
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| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID701116 | Volume of distribution in po dosed human measured in plasma | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
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| AID666487 | Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides. |
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| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1228730 | Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell metabolism after 72 hrs by MTS assay | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID1649410 | Antimalarial activity against multidrug resistant Plasmodium falciparum D6 infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | 2020 | Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11 | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials. |
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| AID1694948 | Inhibition of beta-hematin formation assessed as reduction in hemozoin formation incubated for 20 hrs by NP40 detergent-mediated assay | 2020 | RSC medicinal chemistry, Jan-01, Volume: 11, Issue:1 | Insights into structural and physicochemical properties required for β-hematin inhibition of privileged triarylimidazoles. |
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| AID1717746 | Selectivity index, ratio of CC50 for African green monkey Vero E6 cells to EC50 for SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
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| AID609558 | Cytotoxicity against mouse peritoneal macrophages after 48 hrs by trypan blue exclusion method | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities. |
| AID418857 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum K1 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
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| AID1457205 | Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
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| AID442260 | Cytotoxicity against concanavalin-stimulated BALB/c mouse splenocytes after 72 hrs by resazurin dye reduction method | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
| AID1155471 | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR I method | 2014 | Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13 | Aminoazabenzimidazoles, a novel class of orally active antimalarial agents. |
| AID406403 | Toxicity in Plasmodium vinckei petteri infected CD mice (Mus musculus) assessed as mortality at 1 mg/kg/day, intraperitoneally measured on day 5 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID1265980 | Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Synthesis and bio-evaluation of novel quinolino-stilbene derivatives as potential anticancer agents. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1193241 | n-octanol-phosphate buffer partition coefficient, log D in CH3CN-MeOH-phosphate buffer at pH 7.4 by HPLC-UV analysis | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity. |
| AID543836 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei ATCC 50175 infected in ICR mouse assessed as chemosuppression of parasitemia at 5 mg/kg/day, po pretreated for 4 days before infection and measured after 72 hrs | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice. |
| AID432028 | Antimalarial activity against Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2. |
| AID1377528 | Cytotoxicity against African green monkey Vero A cells assessed as reduction in cell viability after 6 to 7 days by MTS assay | 2017 | Journal of natural products, 07-28, Volume: 80, Issue:7 | Isolation of Premyrsinane, Myrsinane, and Tigliane Diterpenoids from Euphorbia pithyusa Using a Chikungunya Virus Cell-Based Assay and Analogue Annotation by Molecular Networking. |
| AID518550 | Antimalarial activity against Plasmodium berghei ANKA infected in NMRI mice (Mus musculus) assessed as cure rate at 3 times 30 mg/kg, perorally measured on day 3 postinfection | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Preclinical evaluation of the antifolate QN254, 5-chloro- N'6'-(2,5-dimethoxy-benzyl)-quinazoline-2,4,6-triamine, as an antimalarial drug candidate. |
| AID1391093 | Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as increase in AICD level at 3 uM measured after 24 hrs by Western blot analysis relative to chloroquine | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | New phenylaniline derivatives as modulators of amyloid protein precursor metabolism. |
| AID603024 | Antimalarial activity against Plasmodium falciparum D6 assessed as plasmodial LDH activity after 72 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates. |
| AID1422834 | Inhibition of Plasmodium falciparum FCR-3 HDP expressed in Escherichia coli assessed as reduction in hemazoin formation | 2018 | ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10 | Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme. |
| AID722360 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 asexual erythrocyte forms after 48 hrs by parasite LDH assay | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Synthesis, characterization and antimalarial activity of quinoline-pyrimidine hybrids. |
| AID1197877 | Antimalarial activity against Plasmodium falciparum infected in SCID mouse engrafted with human erythrocytes assessed as reduction in parasitemia at 5 mg/kg, po qd for 4 days relative to control | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Prodrugs of reverse fosmidomycin analogues. |
| AID461602 | Antiplasmodial activity against Plasmodium berghei NK65 infected in Swiss Webster mice (Mus musculus) assessed as average parasitaemia at 200 mg/kg, perorally administered 1 day after infection measured after 7 days post infection | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections. |
| AID477966 | Binding affinity to polydAdT DNA containing 100% AT assessed as middle of the peak at half height melting temperature at 1 uM by spectrophotometry analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
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| AID436267 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum D6 | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Bioactive diterpenes and other constituents of Croton steenkampianus. |
| AID372493 | Tmax in patient with kidney disease at 300 mg, po | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast. |
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| AID71872 | Cytotoxicity against FM3A mouse mammary cells | 2003 | Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20 | Metabolites of febrifugine and its synthetic analogue by mouse liver S9 and their antimalarial activity against Plasmodium malaria parasite. |
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| AID1494355 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as decrease in escape latency at 30 mg/kg/day, po for 80 days by Morris water maze test | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
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| AID1351179 | Growth inhibition of CQ-sensitive GFP-fused Plasmodium falciparum D10 after 90 hrs by ethidium bromide staining based flow cytometry | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Broad activity of diphenyleneiodonium analogues against Mycobacterium tuberculosis, malaria parasites and bacterial pathogens. |
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| AID1182794 | Resistance index, ratio of IC50 for Plasmodium falciparum 7G8 to IC50 for Plasmodium falciparum NF54 | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
| AID1494364 | Cognition enhancement activity in double APP/PS1 transgenic Alzheimer's disease mouse model assessed as swimming path length in correct quadrant at 30 mg/kg/day, po for 80 days by Morris water maze test (Rvb = 295.3 +/- 46.9 cm) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID515041 | Cytotoxicity against mouse spleen lymphocytes | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
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| AID1405623 | Antiprotozoal activity against erythrocytic stage of chloroquine and pyrimethamine resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents. |
| AID158373 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Antimalarial activities of (+)-deoxoartemisitene and its novel C-11, 13 derivatives. |
| AID158029 | In vitro antimalarial activity against Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Antimalarial and antitumor evaluation of novel C-10 non-acetal dimers of 10beta-(2-hydroxyethyl)deoxoartemisinin. |
| AID1732338 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss mouse assessed as parasitemia at 10 mg/kg, po administered for 4 days and measured on day 9 post infection by Giemsa staining based microscopic analysis (Rvb = 100 %) | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization. |
| AID1335800 | Cytotoxicity against African green monkey Vero cells at 10 uM after 4 days by fluorescence assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors. |
| AID1904098 | Induction of autophagy in human LNCaP cells assessed as increase in GABARAP2 level at 10 uM preincubated for 2 hrs followed by medium change into aminoacid free medium for 3 hrs by immunoblotting analysis | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery and Structure-Based Optimization of Novel Atg4B Inhibitors for the Treatment of Castration-Resistant Prostate Cancer. |
| AID311096 | Effect on erythrocyte shape in human erythrocytes assessed as echinocytes at 100 ug/mL after 48 hrs | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Transformations of manool. tri- and tetracyclic norditerpenoids with in vitro activity against Plasmodium falciparum. |
| AID587701 | Inhibition of Plasmodium falciparum falcipain 2 incubated with compound for 10 mins before addition of 25 uM Z-Leu-Arg-AMC substrate by fluorescence spectrophotometry | 2011 | European journal of medicinal chemistry, Mar, Volume: 46, Issue:3 | Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials. |
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| AID1427499 | Inhibition of beta-hematin formation assessed as reduction in acetate buffer-initiated hemozoin formation after 18 hrs by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Synthesis of 1,3,5-trisubstituted pyrazolines as potential antimalarial and antimicrobial agents. |
| AID519977 | Antimalarial activity against schizont-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as inhibition of horseradish peroxidase(HRP) uptake after 10 hrs by colorimetric peroxidase assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum. |
| AID268408 | Lipophilicity, Log D at pH 5.2 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Probing the role of the covalent linkage of ferrocene into a chloroquine template. |
| AID676994 | Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID1467028 | Induction of autophagy in HEK293 cells assessed as increase in LC3-2 level at 10 uM after 8 hrs by immunoblot analysis | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy. |
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| AID768181 | Inhibition of beta-hematin formation at 1 mg/ml | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID1859905 | Resistance index, ratio of IC50 for antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 to IC50 for antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of harmiquins, harmine and chloroquine hybrids as potent antiplasmodial agents. |
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| AID1542986 | Inhibition of recombinant His-tagged Plasmodium falciparum GAPDH expressed in Escherichia coli assessed as reduction in NADH formation by measuring Kinact/Ki ratio in presence of NAD+, DL-glyceraldehyde 3-phosphate and GAPDH by spectrophotometry based Fer | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Covalent Inhibitors of |
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| AID1858891 | In vivo antiplasmodial activity against Plasmodium berghei ANKA infected in CD-1 mouse assessed as decrease in parasitaemia at 50 mg/kg, ip measured after 7 days relative to control | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Antimalarial application of quinones: A recent update. |
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| AID411379 | Antimalarial activity as reduced parasitaemia after 72 hrs against chloroquine-resistant Plasmodium falciparum 106/1 in human erythrocytes by DAPI stain | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum. |
| AID1544800 | Antimicrobial activity against Pseudomonas aeruginosa assessed as zone of inhibition at 1 uM/disk after 24 hrs by disk diffusion method | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13 | Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones. |
| AID322074 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hrs | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro. |
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| AID1533488 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as lethal effect on somite formation up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1732470 | Antimalarial activity against asexual blood stage of chloroquine-resistant Plasmodium falciparum 7G8 assessed as reduction in cell viability after 72 hrs by EtBr staining based flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
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| AID1182776 | Cmax in Plasmodium berghei infected mouse at 30 mg/kg treated with four once daily doses | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
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| AID1431575 | Antimalarial activity against Plasmodium falciparum 3D7 asexual blood stage infected in human erythrocytes incubated for 72 hrs by LDH assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity. |
| AID303243 | Cytotoxicity against rat L6 cells | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations. |
| AID1383225 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as reduction in parasitemia at 5 mg/kg, po treated up to day 3 measured at day 4 by Giemsa-staining based microscopic analysis relative to control | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study. |
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| AID454077 | Cytotoxicity against human MCF10A cells after 48 hrs by SRB assay | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | Hybrid pharmacophore design and synthesis of isatin-benzothiazole analogs for their anti-breast cancer activity. |
| AID516848 | Inhibition of beta-hematin formation | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19 | Bis-alkylamine quindolone derivatives as new antimalarial leads. |
| AID1057257 | Therapeutic index, ratio of IC50 for human KB cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers. |
| AID538331 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human O+ erythrocytes after 72 hrs by SYBR Green-1 fluorescence based assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Reinvestigation of structure-activity relationship of methoxylated chalcones as antimalarials: synthesis and evaluation of 2,4,5-trimethoxy substituted patterns as lead candidates derived from abundantly available natural β-asarone. |
| AID540069 | Inhibition of human recombinant NQO2 at 100 uM | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). |
| AID763611 | Tmax in Sprague-Dawley rat at 5 mg/kg, po | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID499272 | Cytotoxicity against human THP1 cells using propidium iodide staining after 72 hrs by flow cytometry | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
| AID449273 | Antimalarial activity against Plasmodium falciparum W2mef trophozoite form by hoechst 33342-thiazole orange stain based flow cytometry assay | 2009 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18 | Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials. |
| AID580680 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID294987 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 by hypoxanthine uptake | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9 | In vitro efficiency of new acridyl derivatives against Plasmodium falciparum. |
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| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
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| AID294068 | Relative activity against Plasmodium falciparum NF54 and K1 as IC50 ratio | 2007 | Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7 | Synthesis and antiplasmodial activity of new N-[3-(4-{3-[(7-chloroquinolin-4-yl)amino]propyl}piperazin-1-yl)propyl]carboxamides. |
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| AID459110 | Therapeutic index, Cytotoxicity against human KB cells to Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo. |
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| AID509184 | Inhibition of TLR7-mediated IFN-gamma production in aldrithiol-2-treated HIV1 MN-stimulated human PBMC at 100 uM after 20 hrs by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
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| AID1808470 | Modulation of full length human Nur77 expressed in SK-N-BE(2) cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
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| AID509180 | Inhibition of TLR7-mediated upregulation of IRAK4 expression in aldrithiol-2-treated HIV1 MN-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
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| AID586924 | Antileishmanial activity against tafenoquine-resistant promastigotes of Leishmania major R4 assessed as inhibition of parasite growth after 72 hrs by MTT assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Increased glycolytic ATP synthesis is associated with tafenoquine resistance in Leishmania major. |
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| AID1894033 | Inhibition of mTOR (unknown origin) activation | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. |
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| AID768485 | Dissociation constant, pKa of the compound | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
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| AID268254 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2006 | Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15 | Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model. |
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| AID263793 | Growth inhibition against Plasmodium falciparum K1 | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents. |
| AID678316 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 after 72 hrs by parasite lactate dehydrogenase assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 22, Issue:18 | Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
| AID1188453 | Antimalarial activity against tightly synchronized Plasmodium falciparum K1 assessed as parasite stage accumulation index at early ring stages at 10 uM treated at 6 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytolo | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
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| AID511100 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 30 mg/kg, perorally administered through 7% Tween80/3% Ethanol formulation 24 hrs post infection for 3 days measured 96 hrs post infecti | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
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| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1732471 | Antimalarial activity against asexual blood stage of artemisinin-resistant Plasmodium falciparum Cam3.12539T cambodian isolate assessed as reduction in cell viability after 72 hrs by EtBr staining based flow cytometric analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
| AID1230199 | Inhibition of hemin crystallization at 0.25 to 10 mol equiv after 18 hrs by spectrophotometric analysis | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Glycosyl hydroperoxides: a new class of potential antimalarial agents. |
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| AID454076 | Cytotoxicity against human 184B5 cells after 48 hrs by SRB assay | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | Hybrid pharmacophore design and synthesis of isatin-benzothiazole analogs for their anti-breast cancer activity. |
| AID1541970 | Antiplasmodial activity against D-sorbitol synchronized ring stage of chloroquine-resistant Plasmodium falciparum W2 assessed as parasite growth inhibition measured after 48 hrs by YOYO-1 dye based FACSort flow cytometry analysis | 2020 | ACS medicinal chemistry letters, Feb-13, Volume: 11, Issue:2 | Functionalized Naphthalimide-4-aminoquinoline Conjugates as Promising Antiplasmodials, with Mechanistic Insights. |
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| AID1182777 | AUClast in Plasmodium berghei infected mouse at 30 mg/kg treated with four once daily doses | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
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| AID1234219 | Cytotoxicity against human SKBR3 cells assessed as reduction in cell number incubated for 72 hrs | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. |
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| AID1628559 | Antimalarial activity against CQ-resistant Plasmodium falciparum K1 infected in human type O+ erythrocytes assessed as growth inhibition incubated for 48 hrs by LDH assay | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
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| AID1437502 | Growth inhibition of HEK293 cells at 40 uM after 72 hrs by PrestoBlue staining based fluorescence assay relative to control | |||
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| AID1057132 | Apparent permeability from basolateral to apical side in MDCK cells at 10 uM after 1 hr by LC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum. |
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| AID1254216 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in po dosed non-myelodepleted NOD-SCID IL2Rgammanull mouse engrafted with human erythrocytes assessed as reduction of parasitemia level administered qd for 4 days | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines. |
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| AID1275777 | Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 by spectroscopic method | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Polycyclic amines as chloroquine resistance modulating agents in Plasmodium falciparum. |
| AID1647634 | Cytotoxicity against HEK293 cells at 40 uM incubated for 72 hrs by resazurin dye based assay relative to control | 2020 | Journal of natural products, 02-28, Volume: 83, Issue:2 | Orthoscuticellines A-E, β-Carboline Alkaloids from the Bryozoan |
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| AID1433554 | Induction of autophagy in human HeLa cells assessed as effect on ratio of LC3-2 to actin at 15 uM after 2 hrs by immunoblot method relative to control | 2016 | Journal of natural products, 10-28, Volume: 79, Issue:10 | Chlorotheolides A and B, Spiroketals Generated via Diels-Alder Reactions in the Endophytic Fungus Pestalotiopsis theae. |
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| AID480230 | Inhibition of CYP3A4 in human liver microsomes assessed as metabolite produced at 1 uM using testosterone as substrate by LC-MS/MS analysis relative to control | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Development of a new generation of 4-aminoquinoline antimalarial compounds using predictive pharmacokinetic and toxicology models. |
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| AID1168873 | Selectivity index, ratio of CC50 for HMEC1 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID1533505 | Hepatotoxicity in 6 hrs post fertilized transgenic l-fabp:EGFP zebrafish embryo assessed as change in liver area index up to 30 uM up to 120 hrs post fertilization by fluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID510925 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as cure rate at 50 mg/kg, perorally administered through 0.5% MCM/0.1%solutol HS15 formulation 24 hrs post infection for 3 days measured on day 30 post | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
| AID1560631 | Antiplasmodial activity against chloroquine-sensitive ring-stage synchronized cultures of Plasmodium falciparum NF54 incubated for 48 hrs by SYBR green I dye based flow cytometry | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Molecular Design and Synthesis of Ivermectin Hybrids Targeting Hepatic and Erythrocytic Stages of |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
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| AID337517 | Antimalarial activity after 24 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected type A+ human erythrocytes by [3H]hypoxanthine uptake | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1524683 | Antiparasitic activity against Plasmodium berghei ANKA infected in Laca mouse assessed as parasitemia at 10 mg/kg, po administered for 4 days measured on day 21 by Giemsa-staining based assay | 2019 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9 | Efficacy of TLR7 agonistic imidazoquinoline as immunochemotherapeutic agent against P. Berghei ANKA infected rodent host. |
| AID768178 | Binding affinity to calf thymus DNA assessed as change in melting temperature at 30 uM by UV-visible spectrophotometry | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID1764404 | Agonist activity at Gal4-fused human Nurr1 LBD expressed in HEK293T cells co-expressing firefly luciferase assessed as fold increase luciferase activity incubated for 12 to 14 hrs by hybrid reporter gene assay relative to control | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Fragment-like Chloroquinolineamines Activate the Orphan Nuclear Receptor Nurr1 and Elucidate Activation Mechanisms. |
| AID626319 | Antiparasitic activity against Plasmodium falciparum K1 infected in rat L6 cells assessed as inhibition of parasite growth preincubated for 48 hrs before [3H]hypoxanthine addition measured after 24 hrs by [3H]hypoxanthine incorporation assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Biological evaluation of glycosyl-isoindigo derivatives against the pathogenic agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis). |
| AID393167 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected human erythrocytes after 72 hrs by [3H]hypoxanthine uptake | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Select pyrimidinones inhibit the propagation of the malarial parasite, Plasmodium falciparum. |
| AID1204844 | Cytotoxicity against human SKOV3 cells assessed as cell growth inhibition after 48 hrs by neutral red assay | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID522090 | AUC (0 to infinity) in Papua new Guinean pregnant women at 750 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID635274 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in erythrocytes after 48 hrs by SYBR green 1-based fluorescence assay | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Triterpenoids as inhibitors of erythrocytic and liver stages of Plasmodium infections. |
| AID673149 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase of mouse survival at 30 mg/kg, po administered 24 hrs post infection qd for 3 days (Rvb = 6 to 7 days) | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
| AID418855 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM6 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID343755 | Cytotoxicity against mouse WEHI13 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Novel amodiaquine congeners as potent antimalarial agents. |
| AID1651546 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1/Columbia infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Molecular Networking Reveals Serpentinine-Related Bisindole Alkaloids from |
| AID419752 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
| AID597076 | Antiplasmodial activity against chloroquine- and pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells assessed as [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Antiparasitic compounds from Cupania cinerea with activities against Plasmodium falciparum and Trypanosoma brucei rhodesiense. |
| AID1359640 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 late forms infected in human RBC using compound encapsulated in to immunoliposome targeted to GPA incubated for 15 mins followed by compound removal and further incubation for | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID504264 | Ratio of IC50 for chloroquine-sensitive Plasmodium falciparum D10 to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID1272452 | Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum Dd2 | 2016 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3 | Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes. |
| AID611731 | Antimalarial activity against erythrocytic stage multidrug-resistant Plasmodium falciparum Dd2 after 48 hrs by fluorescence spectrophotometer | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Synthesis and antimalarial activity of new heterocyclic hybrids based on chloroquine and thiazolidinone scaffolds. |
| AID1594576 | Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 erythrocytic stages incubated for 48 hrs by [3H]-hypoxanthine incorporation assay | 2019 | Bioorganic & medicinal chemistry, 05-15, Volume: 27, Issue:10 | Synthesis and structure-activity relationships for new 6-fluoroquinoline derivatives with antiplasmodial activity. |
| AID1415896 | Cytotoxicity against CHO cells by MTT assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening. |
| AID1421904 | Resistance index, ratio of IC50 for multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes to IC50 for drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID515051 | Drug level in chloroquine-sensitive Plasmodium falciparum D6 digestive vacuole after 1 hr | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID274220 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains. |
| AID351902 | Antimalarial activity after 72 hrs against chloroquine-resistant transporter 106/1'76I mutant Plasmodium falciparum infected in human erythrocytes by SYBR green assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. |
| AID1067233 | Inhibition of ferriprotoporphyrin-9 biocrystallization by micro-ELISA | 2014 | Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5 | Antiprotozoan lead discovery by aligning dry and wet screening: prediction, synthesis, and biological assay of novel quinoxalinones. |
| AID765723 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
| AID412367 | Cytotoxicity against mouse NSO cells by MTT assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID406525 | Toxicity in Plasmodium vinckei petteri infected CD mice (Mus musculus) assessed as mortality at 10 mg/kg/day, intraperitoneally measured on day 1 | 2008 | Journal of natural products, Jul, Volume: 71, Issue:7 | Alisiaquinones and alisiaquinol, dual inhibitors of Plasmodium falciparum enzyme targets from a New Caledonian deep water sponge. |
| AID432027 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2. |
| AID732338 | Antimalarial activity against atovaquone-resistant Plasmodium falciparum TM90C2B | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Discovery and structure-activity relationships of pyrrolone antimalarials. |
| AID359996 | Antimalarial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum W2 as LDH activity by Makler method | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha. |
| AID358505 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 Indochina by [3H]hypoxanthine uptake | 2001 | Journal of natural products, Jan, Volume: 64, Issue:1 | Strychnogucines A and B, two new antiplasmodial bisindole alkaloids from Strychnos icaja. |
| AID593184 | Antimalarial activity against chloroquine-resistant erythrocytic stage of Plasmodium falciparum K1 assessed as inhibition of [3H}hypoxanthine incorporation after 24 hrs by liquid scintillation counter | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7 | β-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase. |
| AID754526 | Inhibition of hemozoin formation in 0.5 M acetate buffer at pH 4.8 after 16 hrs by tube-based high-throughput assay in presence of 0.002 mg/mL phosphatidylcholine | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities. |
| AID1633713 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as mean survival time at 11.1 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 28 post infection (Rvb = 13.2 days) | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
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| AID1383231 | Binding affinity to mu-oxodimeric heme in 0.1M NaOH solution at pH 5.8 by titration analysis | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study. |
| AID337521 | Cytotoxicity against human LUC1 cells after 3 days by sulforhodamine B assay | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID558840 | Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID1335182 | Resistance index, ratio of IC50 for chloroquine-resistant asexual erythrocyte stage of Plasmodium falciparum K1 infected in human type O+ erythrocytes to IC50 for chloroquine-sensitive asexual erythrocyte stage of Plasmodium falciparum NF54 infected in hu | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active against |
| AID1732409 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition | 2021 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 38 | Design, synthesis and biological evaluation of mono- and bisquinoline methanamine derivatives as potential antiplasmodial agents. |
| AID1443731 | Antimalarial activity against chloroquine-sensitive Plasmodium berghei infected in Swiss albino mouse assessed as chemosuppression at 200 mg/kg, po qd administered for 4 days by peter's test relative to control | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Docking, synthesis and antimalarial activity of novel 4-anilinoquinoline derivatives. |
| AID522087 | AUC (0 to infinity) in women at 450 mg/day, po administered as three divided doses by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
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| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID1383237 | Cytotoxicity against African green monkey Vero cells by MTS/PMS assay | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus. |
| AID1810292 | Antimalarial activity against chloroquine, pyrimethamine, mefloquine and atovaquone- resistant Plasmodium falciparum TM90-C2B infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxan | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1 |
| AID294654 | Inhibition of hemozoin formation in presence of hemin chloride and acetate buffer at 1.25 uM to 25 mM after 48 hrs relative to control | 2007 | European journal of medicinal chemistry, Jun, Volume: 42, Issue:6 | Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials. |
| AID1505094 | Antiplasmodial activity against drug-sensitive blood stage Plasmodium falciparum 3D7 by SYBR green 1 staining based fluorescence assay | 2018 | Journal of natural products, 01-26, Volume: 81, Issue:1 | Isolation, Derivative Synthesis, and Structure-Activity Relationships of Antiparasitic Bromopyrrole Alkaloids from the Marine Sponge Tedania brasiliensis. |
| AID524780 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by 96-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
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| AID515064 | Antiplasmodial activity against synchronized chloroquine-sensitive Plasmodium falciparum D6 infected in NMRI mice (Mus musculus) RBC assessed as inhibition of hemozoin formation at 1000 nM after 24 hrs by colorimetric analysis | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID93352 | The compound was tested for survival of the ICR mice (infected with Plasmodium berghei) as a symptom indicative of toxicity on day 4, at a dose of 5 mg/kg/day | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID519273 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum K1Hf pretreated with 0.1 uM phenobarbitone for 48 hrs by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
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| AID710074 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBCs after 72 hrs by parasite lactate dehydrogenase assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents. |
| AID446166 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum FcB1 to IC50 for drug-sensitive Plasmodium falciparum 3D7 | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and antiplasmodial activity of new indolone N-oxide derivatives. |
| AID766750 | Antiparasitic activity against chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as parasite growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18 | Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the Plasmodium falciparum dUTPase. |
| AID1699649 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring stage incubated for 72 hrs by DAPI-staining based imaging analysis | 2020 | Journal of natural products, 11-25, Volume: 83, Issue:11 | Antiplasmodial Alkaloids from the Australian Bryozoan |
| AID564301 | Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID246938 | Effective dose required to reduce the parasitemia in mice by suppressive test after 4 day postinfection | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes. |
| AID392462 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2 | Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity. |
| AID318211 | Cytotoxicity against human lymphocytes after 48 hrs by MTT assay | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
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| AID436173 | Antimalarial activity against Plasmodium berghei infected in mice (Mus musculus) at 100 mg/kg | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Semisynthesis and antiplasmodial activity of the quinoline alkaloid aurachin E. |
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| AID1444623 | Cytotoxicity against African green monkey Vero cells up to 9 uM | 2017 | European journal of medicinal chemistry, May-05, Volume: 131 | N-Piperonyl substitution on aminoquinoline-pyrimidine hybrids: Effect on the antiplasmodial potency. |
| AID504258 | Vacuolar accumulation ratio of the compound at pH 5.2 | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID522077 | Central compartment volume of distribution in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic base model assessed as monodesethychloroquine at 450 mg/day, po administered as three divided doses in presence of sulfad | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1462702 | Antiparasitic activity against intraerythrocytic form of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human RBC preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counti | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | Lead selection of antiparasitic compounds from a focused library of benzenesulfonyl derivatives of heterocycles. |
| AID332192 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum T9-96 | 2002 | Journal of natural products, Jan, Volume: 65, Issue:1 | Indole and beta-carboline alkaloids from Geissospermum sericeum. |
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| AID322133 | In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. |
| AID157704 | Antimalarial activity against Plasmodium falciparum K1 | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of benzylamino and alkylamino ether analogues of artemisinin. |
| AID1664910 | Antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by SYBR Green1 dye based fluorescence assay | 2020 | ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7 | Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity. |
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| AID1162950 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum 3D7 asexual blood stages | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides: a new class of antiplasmodial compounds. |
| AID316603 | Antiplasmodial activity as survival against Plasmodium berghei ANKA infection in NMRI mice (Mus musculus) assessed at 5 mg/kg intraperitoneal dose for 4 days | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity. |
| AID452328 | Growth inhibition of human HeLa cells after 48 hrs by MTT assay in presence of 50 uM ZnCl2 | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | Synthesis and pharmacological exploitation of clioquinol-derived copper-binding apoptosis inducers triggering reactive oxygen species generation and MAPK pathway activation. |
| AID85548 | In vitro cytotoxicity against herpes simplex virus type-1 (HSV-1) HF strain in infected KB cells | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | 7-Aminoquinolines. A novel class of agents active against herpesviruses. |
| AID1274389 | Antimalarial activity against sporozoite stage of Plasmodium berghei yoelii infected in human HepG2 cells | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? |
| AID453373 | Selectivity index, ratio of IC50 for human KB cells to IC50 for chloroquine-resistant Plasmodium falciparum Bre1 | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID256110 | Antileishmanial activity against leishmania amazonensis axenic amastigotes stage; ND = Not determined | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities. |
| AID272298 | Displacement of plasmid pGL3-CV from CDP/plasmid pGL3-CV polyplexes at 20 mM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID1327395 | Selectivity index, ratio of IC50 for CHO cells to IC50 for chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin. |
| AID666879 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as reduction in parasitemia at 3 mg/kg, po administered as single dose measured on day 3 post-infection by flow cytometry | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID1391099 | Cytotoxicity against CHO cells by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | Adamantane amine-linked chloroquinoline derivatives as chloroquine resistance modulating agents in Plasmodium falciparum. |
| AID402126 | Antiplasmodial activity against Plasmodium falciparum K1 infected human erythrocytes by [3H]hypoxanthine uptake | 1997 | Journal of natural products, Jul, Volume: 60, Issue:7 | In vitro and in vivo antiplasmodial activity of cryptolepine and related alkaloids from Cryptolepis sanguinolenta. |
| AID667438 | Antiplasmodial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as decrease in parasitemia measured on day 2 post-treatment by geimsa staining (Rvb = 1.1 +/- 0.09%) | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain. |
| AID303265 | Antiparasitic activity against chloroquine, pyrimethamine-resistant Plasmodium falciparum K1 erythrocyte stage infected rat L6 cells | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and evaluation of antiparasitic activities of new 4-[5-(4-phenoxyphenyl)-2H-pyrazol-3-yl]morpholine derivatives. |
| AID482592 | Antimalarial activity against Plasmodium berghei ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 100 mg/kg, perorally administered as single dose | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria. |
| AID499798 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hrs by LDH assay | 2010 | Journal of natural products, Aug-27, Volume: 73, Issue:8 | Antiplasmodial triterpenoids from the fruits of neem, Azadirachta indica. |
| AID1373374 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Chikungunya virus Indian Ocean 889 infected in African green monkey Vero cells | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents. |
| AID1247271 | Antimalarial activity against Plasmodium berghei NK65 infected in BALB/c mouse assessed as inhibition of parasitemia at 5 mg/kg, po qd for 4 days measured on 7th day after parasite inoculation by Giemsa staining based microscopy relative to control | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents. |
| AID1355869 | Antiplasmodial activity against 4-aminoquinoline/antifolates-resistant Plasmodium falciparum Dd2 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method | 2018 | Journal of natural products, 07-27, Volume: 81, Issue:7 | Antiplasmodial β-Triketone-Flavanone Hybrids from the Flowers of the Australian Tree Corymbia torelliana. |
| AID256063 | Ratio of cytotoxic activity against human MCF-7 cells to that of antiplasmodial activity against Plasmodium falciparum FcB1; ND = Not determined | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities. |
| AID1494331 | Induction of cell proliferation in C57BL/6 mouse hippocampal neurons in CA3 region assessed as BrdU-incorporation at 30 mg/kg, po administered via gavage for 7 days by immunohistochemical analysis (Rvb = 1.5%) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1498894 | Antiplasmodial activity against chloroquine-susceptible blood forms of Plasmodium falciparum 3D7 infected in human erythrocytes measured after 48 hrs by SYBR green1 staining based fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Antiplasmodial activity of hydroxyethylamine analogs: Synthesis, biological activity and structure activity relationship of plasmepsin inhibitors. |
| AID1065144 | Antimalarial activity against Plasmodium chabaudi ASS infected in NIH mouse assessed as inhibition of parasitemia at 4.5 mg/kg, po qd for 4 days | 2014 | ACS medicinal chemistry letters, Jan-09, Volume: 5, Issue:1 | Evaluation of aminohydantoins as a novel class of antimalarial agents. |
| AID1594582 | Antiplasmodial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse assessed as reduction in parasitaemia at 50 mg/kg/day, ip for consecutive 4 days (4, 24, 48 and 72 hrs post infection) and measured up to 20 days after infectio | 2019 | Bioorganic & medicinal chemistry, 05-15, Volume: 27, Issue:10 | Synthesis and structure-activity relationships for new 6-fluoroquinoline derivatives with antiplasmodial activity. |
| AID249022 | In vitro antimalarial activity as schizont maturation against drug-sensitive Plasmodium falciparum | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Design, synthesis and biological evaluation of novel bicyclic beta-lactams as potential antimalarials. |
| AID1188447 | Antimalarial activity against tightly synchronized Plasmodium falciparum W2 assessed as parasite stage accumulation index at schizonts stages at 10 uM treated at 6 hrs post-invasion for continuous duration of 36 hrs by automated image mining based cytolog | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17 | Discovery of carbohybrid-based 2-aminopyrimidine analogues as a new class of rapid-acting antimalarial agents using image-based cytological profiling assay. |
| AID232763 | Relative inhibitory activity to cytotoxicity as selectivity index (CC50/IC50) | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21 | Synthesis and antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives. |
| AID382112 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by LDH reporter assay | 2008 | Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9 | Structural insights into the Plasmodium falciparum histone deacetylase 1 (PfHDAC-1): A novel target for the development of antimalarial therapy. |
| AID576576 | Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax. |
| AID1533487 | Toxicity in 6 hrs post fertilized zebrafish embryo assessed as lethal effect on egg coagulation up to 50 uM up to 120 hrs post fertilization by inverted microscopic method | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID1433155 | Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID728700 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as reduction in parasitemia at 30 mg/kg, po measured on day 3 postinfection relative to control | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. |
| AID688336 | Lipophilicity, log P of the compound at pH 7.4 | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and antiplasmodial activity of new heteroaryl derivatives of 7-chloro-4-aminoquinoline. |
| AID558832 | Antimalarial activity against Plasmodium falciparum HB3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID666878 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as mean survival days of host at 10 mg/kg, po administered as single dose | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID564239 | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 and mutant pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID703902 | Mutagenicity against Salmonella typhimurium TA98 assessed as revertants at 5 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1194357 | Antimalarial activity against multidrug-resistant Plasmodium falciparum thailand TM91C235 assessed as [3H]-hypoxanthine incorporation by liquid scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice. |
| AID340541 | Cytotoxicity against african green monkey Vero cells at 17 uM after 48 hrs by neutral red assay | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 2-N-Methyl modifications and SAR studies of manzamine A. |
| AID158842 | Inhibitory activity against chloroquine-sensitive Plasmodium falciparum D6 (CDC/Sierra Leone I) | 2002 | Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16 | Synthesis and in vitro studies of novel pyrimidinyl peptidomimetics as potential antimalarial therapeutic agents. |
| AID1777162 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 incubated for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay | 2021 | ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7 | Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205. |
| AID1717817 | Cytotoxicity against African green monkey Vero E6 cells by the MTS assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID681132 | TP_TRANSPORTER: ATP hydrolysis in MDR1-expressing Sf9 cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID603025 | Antimalarial activity against Plasmodium falciparum W2 assessed as plasmodial LDH activity after 72 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates. |
| AID1628544 | Binding affinity to Fe(3)PP9 in hematin solution at pH 7.5 by titration-based UV-vis spectrophotometrical analysis | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
| AID688317 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBC assessed as inhibition of parasite growth after 72 hrs by lactate dehydrogenase assay | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | Synthesis and comparison of antiplasmodial activity of (+), (-) and racemic 7-chloro-4-(N-lupinyl)aminoquinoline. |
| AID1810603 | Antimalarial activity against blood stage Plasmodium yoelii infected in CF1 mouse assessed as reduction in parasitemia at 25 mg/kg, po administered once daily for 4 days and measured on day 5 by Giemsa staining based microscopic analysis relative to contr | |||
| AID479488 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by flow-cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90. |
| AID1883293 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as parasite growth inhibition and measured after 72 hrs by ELISA | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Sattahipmycin, a Hexacyclic Xanthone Produced by a Marine-Derived |
| AID569315 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 by parasite LDH assay | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores. |
| AID300113 | Antiparasitemia activity against Plasmodium berghei infected mice (Mus musculus) at 10 mg/kg intravenous dose for 4 days | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Anti-malarial activity of N6-modified purine analogues. |
| AID1808474 | Modulation of full length human Nur77 expressed in PC12 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID1201065 | Antiplasmodial activity against chloroquine/mefloquine-resistant Plasmodium falciparum SRIV35 | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Synthesis of isocryptolepine analogues and their structure-activity relationship studies as antiplasmodial and antiproliferative agents. |
| AID555962 | Antimalarial activity against chloroquine-resistant Plasmodium vivax by Giemsa staining | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax. |
| AID359997 | Selectivity index, ratio of IC50 of african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-resistant Plasmodium falciparum W2 | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha. |
| AID662820 | Antiplasmodial activity against Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation after 18 hrs by liquid scintillation counting | 2011 | ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12 | Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity. |
| AID1204838 | Antiplasmodial activity against Plasmodium falciparum W2 infected in human RBC assessed as parasite growth inhibition measured as LDH activity after 72 hrs by plate reader analysis | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, antimalarial and antitubercular activities of meridianin derivatives. |
| AID423029 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1 | Antimalarial peptides from marine cyanobacteria: isolation and structural elucidation of gallinamide A. |
| AID549522 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human A-positive red blood cells after 72 hrs by lactate dehydrogenase assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Antimalarials based on the dioxane scaffold of plakortin. A concise synthesis and SAR studies. |
| AID524777 | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by 1536-well format based SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID768490 | Antimalarial activity against Plasmodium falciparum K1 infected in RBC assessed as growth inhibition after 48 hrs by SYBR Green-I fluorescence assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID1378987 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by [G-3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID1555143 | Antimalarial activity against synchronized ring stage CQ-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes incubated for 24 hrs followed by compound washout and subsequent compound addition and measured after 48 hrs by YOYO-1 probe-based | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials. |
| AID119885 | In vivo antimalarial activity against Plasmodium yoelii in Swiss mice (Mus musculus) on day 4 at the dose of 96 mg/kg/day orally | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Geraniol-derived 1,2,4-trioxanes with potent in-vivo antimalarial activity. |
| AID510911 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as reduction in parasitaemia at 100 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
| AID112556 | In Vivo antimalarial activity of compound was tested in Plasmodium berghei infected mice (Mus musculus) | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | New semisynthetic quassinoids with in vivo antimalarial activity. |
| AID1830499 | Cytotoxicity against human Hep3B cells assessed as cell viability by MTT assay | |||
| AID562540 | Cytotoxicity against african green monkey Vero cells assessed as incorporation of [3H]hypoxanthine after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID1638536 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC27 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | 3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity. |
| AID263794 | Inhibition of Plasmodium falciparum K1 as [3H]hypoxanthine uptake | 2006 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8 | Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents. |
| AID773692 | Antiplasmodial activity against blood stage of chloroquine-resistant Plasmodium falciparum W2 infected in human RBC assessed as parasite growth inhibition after 48 hrs by flow cytometric analysis | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Structural optimization of quinolon-4(1H)-imines as dual-stage antimalarials: toward increased potency and metabolic stability. |
| AID1752933 | Antimalarial activity against Plasmodium berghei QIMR infected in BALB/c mouse assessed as reduction in peripheral blood parasitemia at 10 mg/kg, po qd for 4 days starting from 2 hrs post-infection and measured on 4 to 6 days post-infection by Giemsa stai | |||
| AID213659 | In vitro anti protozoal activity against Trypanosoma cruzi strain Tulahuen CL2 was determined; ND = Not determined | 2004 | Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14 | Biological evaluation of substituted quinolines. |
| AID343748 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 as LDH reporter activity | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Novel amodiaquine congeners as potent antimalarial agents. |
| AID1673518 | Plasma concentration in NIH mouse infected with Plasmodium chabaudi ASS at 10 mg/kg, po qd for 4 days starting from 4 hrs post-parasite inoculation and measured at 24 hrs post-dosing on day 4 by LC/MS analysis | |||
| AID659137 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67 infected Swiss mouse assessed as mean survival time at 10 mg/kg/day, po qd for 4 days | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Antiplasmodial activity of novel keto-enamine chalcone-chloroquine based hybrid pharmacophores. |
| AID1466468 | Anti-plasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 50 hrs by SYBR green dye based fluorescence assay | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Synthesis and evaluation of anti-plasmodial and cytotoxic activities of epoxyazadiradione derivatives. |
| AID1661404 | Selectivity index, ratio of IC50 for human K562 cells to IC50 for antiplasmodial activity against Plasmodium falciparum 3D7 infected in erythrocytes | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | β-Hydroxy- and β-Aminophosphonate Acyclonucleosides as Potent Inhibitors of |
| AID1779232 | Antimalarial activity against Plasmodium falciparum 3D7 assessed as reduction in parasite growth measured after 72 hrs by Monash assay based fluorescence analysis | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Discovery and development of 2-aminobenzimidazoles as potent antimalarials. |
| AID1408801 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for multidrug-resistant Plasmodium falciparum FRC-3 | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Novel antimalarial chloroquine- and primaquine-quinoxaline 1,4-di-N-oxide hybrids: Design, synthesis, Plasmodium life cycle stage profile, and preliminary toxicity studies. |
| AID1305448 | Antimalarial activity against Plasmodium falciparum 3D7 incubated for 72 hours by DAPI-staining based confocal imaging analysis | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Selective anti-malarial minor groove binders. |
| AID1337668 | Selectivity index, ratio of CC50 for human HepG2 cells to IC50 for chloroquine/pyrimethamine/proguanil-resistant Plasmodium falciparum K1 infected in human erythrocytes | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Discovery of new hit-molecules targeting Plasmodium falciparum through a global SAR study of the 4-substituted-2-trichloromethylquinazoline antiplasmodial scaffold. |
| AID1808276 | Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID285471 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1 | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes. |
| AID499812 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum D6 | 2010 | Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16 | Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton. |
| AID453370 | Selectivity index, ratio of IC50 for human KB cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23 | Antimalarial acridines: synthesis, in vitro activity against P. falciparum and interaction with hematin. |
| AID1359632 | Ratio of IC50 for antiplasmodial activity against Plasmodium falciparum 3D7 ring stage forms infected in immunoliposome encapsulated compound pre-loaded human RBC by [3H]-hypoxanthine incorporation assay to IC50 for antiplasmodial activity against Plasmod | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID683349 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as suppression in parasitemia at 100 mg/kg, po administered QD for 3 days measured on day 5 relative to control | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity. |
| AID1633692 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 incubated for 48 hrs by parasite lactate dehydrogenase assay | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID225006 | In vivo antimalarial activity against Plasmodium chabaudi in mice (Mus musculus) and its survival rate reported | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22 | Synthesis, stability, and antimalarial activity of new hydrolytically stable and water-soluble (+)-deoxoartelinic acid. |
| AID426726 | Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum W2 by Malstat LDH activity | 2009 | Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15 | Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes. |
| AID519198 | Antimicrobial activity against Plasmodium vivax at the ring stage measured within 30 hrs by microscopy | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Determinants of in vitro drug susceptibility testing of Plasmodium vivax. |
| AID1395367 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by Malstat reagent-based spectrophotometric analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives. |
| AID605729 | Antimalarial activity against GFP-transfected Plasmodium berghei strain ANKA infected in NMRI mouse assessed as increase in median survival time at 10 mg/kg/day, ip administered for 4 days measured up to 30 days (Rvb = 5 to 7 days) | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Antimalarial pyrido[1,2-a]benzimidazoles. |
| AID1593254 | Antimalarial activity against multidrug-resistant Plasmodium falciparum 7G8 infected in human erythrocytes by SYBR green 1-based fluorescence assay | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials. |
| AID585010 | Antimalarial activity against Plasmodium malariae ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia. |
| AID562565 | Antiplasmodial activity against Plasmodium vinckei petteri infected in po dosed CD mouse assessed as extended mean survival time at 10 mg/kg/day, ip for 4 days | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Antimalarial activity of simalikalactone E, a new quassinoid from Quassia amara L. (Simaroubaceae). |
| AID411375 | Antimalarial activity as reduced parasitaemia after 72 hrs against chloroquine-resistant Plasmodium falciparum Dd2 in human erythrocytes by DAPI stain | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Synthesis of spiro-1,2-dioxolanes and their activity against Plasmodium falciparum. |
| AID1339559 | Reduction in lysosomal acidification in human HepG2 cells at 50 uM after 6 hrs by DAPI/lyso tracker red-double staining based confocal microscopic analysis relative to control | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | Synthesis, Biological Evaluation, and Autophagy Mechanism of 12 |
| AID580717 | Cytotoxicity against rat L6 cells | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID1431582 | Antimalarial activity against chloroquine and mefloquine resistant Plasmodium falciparum W2mef infected in human erythrocytes incubated for 72 hrs by LDH assay | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity. |
| AID377794 | Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum FCR3 in human erythrocytes after 24 hrs | 2005 | Journal of natural products, Apr, Volume: 68, Issue:4 | Anti-babesial and anti-plasmodial compounds from Phyllanthus niruri. |
| AID272308 | Transfection of CDP/plasmid pGL3-CV in HeLa cells at 200 uM after 48 hrs by luciferase assay | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID322127 | In vitro antimalarial activity against Plasmodium falciparum W2 after 72 hrs in SYBR green fluorescence assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. |
| AID1125282 | Antimicrobial activity against blood-stage Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent lipophilicity (LELP). |
| AID1163255 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
| AID1332934 | Binding affinity to monomeric heme (unknown origin) assessed as association constant at pH 7.4 by UV-titration method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 4, 5-Dihydrooxazole-pyrazoline hybrids: Synthesis and their evaluation as potential antimalarial agents. |
| AID1633698 | Selectivity index, ratio of IC50 for CHO cells to IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID322125 | In vitro antimalarial activity against Plasmodium falciparum D6 after 72 hrs in SYBR green fluorescence assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening. |
| AID419120 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 equivalent of drug to 1 molecule of heme in presence of 20 mM SDS by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID1779234 | Antimalarial activity against synchronous ring stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Discovery and development of 2-aminobenzimidazoles as potent antimalarials. |
| AID545360 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 infected in erythrocytes assessed as [3H]hypoxanthine incorporation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Role of known molecular markers of resistance in the antimalarial potency of piperaquine and dihydroartemisinin in vitro. |
| AID608684 | Cytotoxicity against human KB cells assessed as growth inhibition at 100 uM | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Antiplasmodial and cytotoxicity evaluation of 3-functionalized 2-azetidinone derivatives. |
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| AID472380 | Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Plasmodium falciparum | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Synthesis and biological evaluation of new heterocyclic quinolinones as anti-parasite and anti-HIV drug candidates. |
| AID1421907 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID117997 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium berghei N. activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4-day test at a concentration of 1 mg/kg in experiment 2 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
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| AID1234236 | Inhibition of cell proliferation of lung cancer cells (unknown origin) | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. |
| AID132765 | In vivo antimalarial activity against Plasmodium berghei N on subcutaneous administration. | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2 | Orally active, hydrolytically stable, semisynthetic, antimalarial trioxanes in the artemisinin family. |
| AID401650 | Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 in erythrocytes by [3H]hypoxanthine uptake | 2005 | Journal of natural products, May, Volume: 68, Issue:5 | ent-Dioncophylleine A and related dehydrogenated naphthylisoquinoline alkaloids, the first Asian dioncophyllaceae-type alkaloids, from the "new"plant species Ancistrocladus benomensis. |
| AID700787 | Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5 | A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold. |
| AID1849760 | Antimalarial activity against multidrug resistant Plasmodium falciparum K1 incubated for 72 hrs by malaria SYBR green I nucleic acid staining dye based fluorescence assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins. |
| AID668286 | Antiplasmodial activity against chloroquine-, pyrimethamine-, proguanil-resistant Plasmodium falciparum K1 infected in A-positive human erythrocytes after 72 hrs by SYBR green 1 fluorescence-based method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Discovery of a new antileishmanial hit in 8-nitroquinoline series. |
| AID1072853 | Antiplasmodial activity against Plasmodium berghei ANKA infected in mouse assessed as mean survival time at 10 mg/kg, po administered 4 times per day | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity. |
| AID454073 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by SRB assay | 2009 | Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21 | Hybrid pharmacophore design and synthesis of isatin-benzothiazole analogs for their anti-breast cancer activity. |
| AID1730953 | Antimalarial activity against Plasmodium falciparum assessed as parasite growth inhibition | 2021 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 36 | Structure based design, synthesis, and biological evaluation of imidazole derivatives targeting dihydropteroate synthase enzyme. |
| AID157864 | In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum K1 | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain. |
| AID1274371 | Antimalarial activity against chloroquine-susceptible Plasmodium falciparum D6 after 48 hrs by [3H]hypoxanthine incorporation assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? |
| AID1355304 | Plasmodicidal activity against Plasmodium falciparum 3D7A infected in erythrocytes assessed as parasite survival at 10 times IC50 pre-incubated for 48 hrs followed by compound washout and measured after 24 hrs by 1H-hypoxanthine incorporation assay (Rvb = | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
| AID1241103 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 infected in human erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies. |
| AID1445954 | Antiplasmodial activity against Plasmodium berghei infected in NMRI mouse assessed as parasite-free mouse at 30 mg/kg, po administered at 4, 24, 48, 72 hrs post infection measured on day 30 by Peter's test | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally. |
| AID509196 | Inhibition of TLR9-mediated indoleamine 2,3-dioxygenase activation in CpGA-stimulated human PBMC assessed as decrease in kynurenine to tryptophan level at 100 uM after 20 hrs by ELISA | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID159868 | In vitro antimalarial activity against Plasmodium falciparum | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | New semisynthetic quassinoids with in vivo antimalarial activity. |
| AID564230 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
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| AID1191209 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Reemergence of chloroquine (CQ) analogs as multi-targeting antimalarial agents: a review. |
| AID1780628 | Antimalarial activity against chloroquine sensitive Plasmodium falciparum D10 infected in human red blood cells assessed as reduction in parasite growth measured after 72 hrs by parasite lactate dehydrogenase assay | 2021 | ACS medicinal chemistry letters, Nov-11, Volume: 12, Issue:11 | Development of Potent 3-Br-isoxazoline-Based Antimalarial and Antileishmanial Compounds. |
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| AID703904 | Mutagenicity against Salmonella typhimurium TA98 assessed as revertants at 20 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID378861 | Antimalarial activity as reduced schizont maturation in Plasmodium berghei ANKA infected mice (Mus musculus) at 5 mg/kg/day peroral dose over 4 days | 2006 | Journal of natural products, Oct, Volume: 69, Issue:10 | Antimalarial 4-phenylcoumarins from the stem bark of Hintonia latiflora. |
| AID418052 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected type A+ human erythrocytes after 24 hrs by [G-3H]hypoxanthine uptake | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7 | Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates. |
| AID334267 | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 after 24 hrs by [3H]hypoxanthine uptake | 2002 | Journal of natural products, Apr, Volume: 65, Issue:4 | Efficacy of scopadulcic acid A against Plasmodium falciparum in vitro. |
| AID564232 | Antiplasmodial activity against Plasmodium falciparum clinical isolate after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID1717816 | Antiviral activity against SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells incubated for 3 days by MTS assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID382478 | Cytotoxicity against human MCR5 cells after 7 days by MTT assay | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2 | Synthesis and antimalarial activity of new analogues of amodiaquine. |
| AID522069 | Central compartment volume of distribution in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic base model at 450 mg/day, po administered as three divided doses in presence of sulfadoxine-pyrimethamine by HPLC method | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID597180 | Half life in mouse liver microsomes assessed as compound degradation at 1 uM by LC-MS analysis in presence of NADPH and UDPGA | 2011 | Journal of medicinal chemistry, May-26, Volume: 54, Issue:10 | Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies. |
| AID1351067 | Antimalarial activity against Plasmodium berghei ANKA infected in Balb/c mouse assessed as parasitemia at 25 mg/kg, ip qd administered for 4 days starting from 2 hrs post infection by Giemsa staining based microscopic method (Rvb = 65.2 +/- 2.58%) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis, β-hematin inhibition studies and antimalarial evaluation of new dehydroxy isoquine derivatives against Plasmodium berghei: A promising antimalarial agent. |
| AID1513846 | Antiplasmodial activity against Plasmodium falciparum K1 after 48 hrs by lactate dehydrogenase assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains. |
| AID1361084 | Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Synthesis and antiplasmodial activity of glyco-conjugate hybrids of phenylhydrazono-indolinones and glycosylated 1,2,3-triazolyl-methyl-indoline-2,3-diones. |
| AID600092 | Antiplasmodial activity against chloroquine-sensitive and mefloquine-resistant Plasmodium falciparum D6 | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12 | Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition. |
| AID1187056 | Antimalarial activity against blood stage of multidrug-resistant Plasmodium falciparum K1 after 72 hrs by [3H]hypoxanthine incorporation assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | 2-Octadecynoic acid as a dual life stage inhibitor of Plasmodium infections and plasmodial FAS-II enzymes. |
| AID384322 | Cytotoxicity against rat L6 cells | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity. |
| AID1167713 | Antimalarial activity against chloroquine-resistant Plasmodium yoelii N-67infected in Swiss Albino mouse assessed as suppression of parasitemia at 20 mg/kg, po once daily for 4 days measured on day 4 post infection | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis of chiral chloroquine and its analogues as antimalarial agents. |
| AID658762 | Binding affinity to monomeric heme in HEPES buffer at pH 5.6 by spectrophotometric analysis | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies. |
| AID1176085 | Antileishmanial activity against Leishmania infantum MHOM/TN/80/IPT1 promastigotes assessed as inhibition of parasite growth after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Clofazimine analogs with antileishmanial and antiplasmodial activity. |
| AID509455 | Antiproliferative activity against human MCF10A cells after 48 hrs by SRB assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design and synthesis of chloroquine analogs with anti-breast cancer property. |
| AID509175 | Inhibition of TLR7/TLR9-mediated activation of aldrithiol-2-treated HIV1 Ada-stimulated human PBMC assessed as CD86 expressing cells at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID730536 | Resistance ratio of IC5O for Plasmodium falciparum K1 to IC50 for Plasmodium falciparum 3D7 | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Synthesis and insight into the structure-activity relationships of chalcones as antimalarial agents. |
| AID158386 | In vitro antimalarial activity against Thai strain of Plasmodium falciparum | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines. |
| AID1229877 | Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as mouse survival at 30 mg/kg, po dosed once daily for 4 consecutive days beginning 1 hr after initial infection and measured on day 8 post infection by Giemsa sta | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles. |
| AID401572 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | A new antimalarial quassinoid from Simaba orinocensis. |
| AID1772149 | Antimalarial activity against Plasmodium falciparum K1 assessed as inhibition of parasite growth by microculture radioisotope technique | 2021 | Journal of natural products, 11-26, Volume: 84, Issue:11 | Antimicrobial and Cytotoxic Angucyclic Quinones from |
| AID159717 | Parasitaemia (%) in tail blood smears from Plasmodium berghei infected ICR mice (Mus musculus) after 4 days | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID161627 | Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. |
| AID1201526 | Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium. |
| AID377197 | Antiplasmodial activity against Plasmodium falciparum K1 | 2000 | Journal of natural products, Aug, Volume: 63, Issue:8 | Pelorol from the tropical marine sponge Dactylospongia elegans. |
| AID1225324 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 in human erythrocyte after 72 hrs by SYBR Green I assay | 2015 | Journal of natural products, Mar-27, Volume: 78, Issue:3 | Depsipeptide companeramides from a Panamanian marine cyanobacterium associated with the coibamide producer. |
| AID551214 | Cytotoxicity against HEK293 cells after 72 hrs by Alamar Blue assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | Psammaplysin H, a new antimalarial bromotyrosine alkaloid from a marine sponge of the genus Pseudoceratina. |
| AID477965 | Binding affinity to polydAdT DNA containing 100% AT assessed as maximum melting temperature at 1 uM by spectrophotometry analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA. |
| AID1612296 | Antiplasmodial activity against Plasmodium falciparum NF54 erythrocytic stage assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by liquid scintillation counting | 2018 | Journal of natural products, 10-26, Volume: 81, Issue:10 | Methionine-Containing Rhabdopeptide/Xenortide-like Peptides from Heterologous Expression of the Biosynthetic Gene Cluster kj12ABC in Escherichia coli. |
| AID337542 | Selectivity index, ratio of ED50 for human KB-V1 cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID1574645 | Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based confocal imaging analysis | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases. |
| AID1383238 | Selectivity index, ratio of CC50 for African green monkey Vero cells to EC50 for Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus. |
| AID1664930 | Antiplasmodial activity against Plasmodium falciparum infected in human erythrocytes assessed as reduction in hemozoin size at 30 nM after 48 hrs by giemsa staining based light microscopic analysis | 2020 | ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7 | Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity. |
| AID349010 | Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. |
| AID568764 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen". |
| AID522080 | Intercompartment clearance in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic final covariate model assessed as monodesethychloroquine at 450 mg/day, po administered as three divided doses in presence of sulfadoxine | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1176977 | Antiplasmodial activity against Plasmodium falciparum assessed as growth inhibition | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites. |
| AID347271 | Toxicity in monkey assessed as increase in QTc interval | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID606985 | Antimalarial activity against GFP-transfected Plasmodium berghei strain ANKA infected in NMRI mouse assessed as increase in median survival time at 10 mg/kg/day, po administered as single dose measured up to 30 days (Rvb = 5 days) | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Antimalarial pyrido[1,2-a]benzimidazoles. |
| AID1057135 | Half life in human plasma at 1 mM by LC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum. |
| AID158820 | Inhibition of Plasmodium berghei infection in mice (Mus musculus) at 25 mg/kg peroral dose (expt 2) | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID509199 | Inhibition of TLR7/TLR8-mediated upregulation of PDL1 expression in 3M-011-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID573272 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-susceptible Plasmodium falciparum D10 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Novel antimalarial aminoquinolines: heme binding and effects on normal or Plasmodium falciparum-parasitized human erythrocytes. |
| AID105837 | Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 3.1 uM concentration | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines. |
| AID1626152 | Cytotoxicity against mouse J774 cells | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | ICI 56,780 Optimization: Structure-Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity. |
| AID1355303 | Plasmodicidal activity against Plasmodium falciparum 3D7A infected in erythrocytes assessed as parasite survival at 10 times IC50 pre-incubated for 24 hrs followed by compound washout and measured after 24 hrs by 1H-hypoxanthine incorporation assay (Rvb = | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Discovery of Marinoquinolines as Potent and Fast-Acting Plasmodium falciparum Inhibitors with in Vivo Activity. |
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| AID374064 | Antimalarial activity as MST against chloroquine-sensitive Plasmodium berghei ANKA infected BALB/c mice (Mus musculus) erythrocytes at 25 mg/kg intraperitoneal dose for 4 days (RVb=11.66+/-1.66 days) | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and antimalarial activity of pyrazolo and pyrimido benzothiazine dioxide derivatives. |
| AID359998 | Antimalarial activity after 48 hrs against chloroquine-sensitive Plasmodium falciparum D6 as LDH activity by Makler method | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha. |
| AID497177 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1 after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia. |
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| AID158381 | In vitro antimalarial activity for Plasmodium falciparum BHz26/86 | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID515030 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum 7G8 after 72 hrs by SYBR green 1 fluorescence-based method | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds. |
| AID1688335 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6(CQS)Sierra Leone incubated for 48 hrs by classical radioactive microdilution method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Current progress in antimalarial pharmacotherapy and multi-target drug discovery. |
| AID675270 | Antimalarial activity against chloroquine resistant Plasmodium falciparum K1 infected in RBCs incubated for 72 hrs by SYBRgreen dye based fluorometric assay | 2012 | European journal of medicinal chemistry, Sep, Volume: 55 | One pot efficient diversity oriented synthesis of polyfunctional styryl thiazolopyrimidines and their bio-evaluation as antimalarial and anti-HIV agents. |
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| AID158394 | In vitro antimalarial activity against Plasmodium falciparum Dd2 | 2004 | Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8 | Sulfonyl-phenyl-ureido benzamidines; a novel structural class of potent antimalarial agents. |
| AID544215 | Antiplasmodial activity against Plasmodium falciparum FcB1 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | In vitro and in vivo properties of ellagic acid in malaria treatment. |
| AID1145672 | Antibacterial activity against chlorguanide triazine-resistant Streptococcus faecium ATCC 8043 assessed as reduction in growth | 1977 | Journal of medicinal chemistry, Feb, Volume: 20, Issue:2 | Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli. |
| AID1435974 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O+erythrocytes after 72 hrs by lactate dehydrogenase assay | 2016 | Journal of natural products, 11-23, Volume: 79, Issue:11 | Isolation and Structure Elucidation by LC-DAD-MS and LC-DAD-SPE-NMR of Cyclopeptide Alkaloids from the Roots of Ziziphus oxyphylla and Evaluation of Their Antiplasmodial Activity. |
| AID404598 | Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense. |
| AID347216 | Antimalarial schizonticidal activity against Plasmodium falciparum 3D7 infected erythrocytes at 0.09 ug/ml after 30-39 hrs | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials. |
| AID1433145 | Antiviral activity against Sindbis virus infected in African green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID318217 | Reduced parasitemia in Plasmodium berghei ANKA infected CD1 mice (Mus musculus) at 10 mg/kg peroral dose after 4 days | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1204129 | Antimalarial activity against Plasmodium berghei NK65 infected in Swiss albino mouse assessed as inhibition of parasitemia at 10 mg/kg, po dosed for four consecutive days beginning on first day of infection and measured on day 12 post infection relative t | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1391506 | Antimalarial activity against Plasmodium berghei infected in Swiss albino mouse assessed as suppression of parasitaemia at 20 mg/kg/day, po for 4 consecutive days starting from 4 hrs post infection measured on day 4 post last dose by Giemsa staining based | 2018 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9 | Designing novel inhibitors against falcipain-2 of Plasmodium falciparum. |
| AID1194372 | Binding affinity to heme assessed as inhibition of beta-hematin formation by BHIA assay relative to hemin | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice. |
| AID158878 | In vivo antimalarial activity against Plasmodium falciparum | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID522075 | Clearance in Papua new Guinean women in second or third trimester of pregnancy using pharmacokinetic base model assessed as monodesethychloroquine at 450 mg/day, po administered as three divided doses in presence of sulfadoxine-pyrimethamine by HPLC metho | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy. |
| AID1323834 | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. |
| AID1808468 | Modulation of full length human Nur77 expressed in SK-N-BE(2) cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assa | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID284377 | Selectivity index, Ratio of IC50 in Vero cells to IC50 in chloroquine-resistant Plasmodium falciparum W2 | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis, antimalarial, antileishmanial, antimicrobial, cytotoxicity, and methemoglobin (MetHB) formation activities of new 8-quinolinamines. |
| AID302172 | Antifungal activity against Candida albicans ATCC 90028 after 48 hrs | 2007 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22 | Modifications of the chemical structure of terpenes in antiplasmodial and antifungal drug research. |
| AID1915892 | Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 24 hrs by neutral red dye based analysis | |||
| AID417170 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FCM29 by SYBR green assay | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Antiproliferative and antimalarial anthraquinones of Scutia myrtina from the Madagascar forest. |
| AID568777 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as reduction of parasite infection at 1 mg/kg, sc qd for 4 days relative to control | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1 | Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen". |
| AID152007 | Inhibition of beta-hematin formation | 2002 | Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23 | Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum. |
| AID1176090 | Selectivity index, ratio of IC50 for HMEC1 to IC50 for Leishmania braziliensis MHOM/IT/2006/ISS2848 | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Clofazimine analogs with antileishmanial and antiplasmodial activity. |
| AID1359550 | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum FCR-3 by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID118881 | Total number of mice protected out of the 5 tested at a dose of 48 mg/kg/day (Observation till day 10 post-infection) | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Photo-oxygenation of geraniol: synthesis of a novel series of hydroxy-functionalized anti-malarial 1,2,4-trioxanes. |
| AID436311 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation assay | 2008 | Journal of natural products, Nov, Volume: 71, Issue:11 | Antioxidant C-glucosylxanthones from the leaves of Arrabidaea patellifera. |
| AID1203065 | Ratio of hydroxychloroquine IC50 to compound IC50 for human BxPC3 cells | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID319198 | Antimalarial activity against Plasmodium falciparum HB3 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles. |
| AID1808450 | Modulation of full length human Nur77 expressed in SK-N-BE(2) cells co-transfected with luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 by luciferase reporter gene assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID774663 | Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Approaches to protozoan drug discovery: phenotypic screening. |
| AID1436319 | Antimalarial activity against intraerythrocytic stage of Plasmodium falciparum 3D7A assessed as log (viable parasites +1) at 10 times IC50 after 48 hrs by [3H]-hypoxanthine incorporation assay (Rvb = 5 No_unit) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans. |
| AID401646 | Displacement of methyl green dye from DNA | 2005 | Journal of natural products, May, Volume: 68, Issue:5 | Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound. |
| AID1349490 | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes engrafted in NOD-SCID IL-2Rgamma null mouse assessed as reduction in blood parasitemia administered as single dose via oral gavage measured on day 7 post treatment by | 2017 | ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12 | Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol. |
| AID704125 | Mutagenicity against Salmonella typhimurium TA100 assessed as revertants at 80 uM incubated for 90 mins followed by drug washout measured after 2 days relative to positive control | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID510914 | Antimalarial activity against Plasmodium berghei GFP ANKA infected in NMRI mice (Mus musculus) assessed as survival at 100 mg/kg, perorally administered as single dose 24 hrs post infection for 1 day measured 72 hrs post infection | 2010 | Science (New York, N.Y.), Sep-03, Volume: 329, Issue:5996 | Spiroindolones, a potent compound class for the treatment of malaria. |
| AID1348371 | Cytotoxicity against human MRC5 SV2 cells assessed as decrease in cell viability after 72 hrs by resazurin dye-based fluorometric method | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Novel triazine dimers with potent antitrypanosomal activity. |
| AID1405075 | Antiplasmodial activity against synchronized ring stage of chloroquine-resistant Plasmodium falciparum INDO infected in human erythrocytes after 48 hrs by SYBR Green 1 dye based fluorescence assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Facile synthesis of vanillin-based novel bischalcones identifies one that induces apoptosis and displays synergy with Artemisinin in killing chloroquine resistant Plasmodium falciparum. |
| AID580695 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of ring stage parasite growth at 100 times IC50 after 1 hr by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2 | Compounds structurally related to ellagic acid show improved antiplasmodial activity. |
| AID590136 | Antiplasmodial activity against Plasmodium falciparum W2 | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. |
| AID763605 | Volume of distribution in Sprague-Dawley rat at 5 mg/kg, po | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID1409622 | Activity of compound against Muscarinic acetylcholine receptor M5 (CHRM5) by displacement of 3H-QNB | 2020 | Nature, 07, Volume: 583, Issue:7816 | A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
| AID113168 | In vivo antimalarial activity in mice (Mus musculus) against chloroquine-resistant Plasmodium yoelii species. NS after subcutaneous administration | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides. |
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| AID1378982 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human type A+ erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
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| AID118002 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS., activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4-day test at a concentration of 10 mg/kg in experiment 1 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
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| AID449705 | NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7) | 2008 | Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26 | In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. |
| AID1383236 | Antiviral activity against Chikungunya virus Indian Ocean strain 899 infected in African green monkey Vero cells assessed as inhibition of viral-induced cytopathic effect measured on day 5 post infection by MTS/PMS assay | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus. |
| AID272296 | Binding affinity to plasmid pGL3-CV assessed as retardation of movement in gel at 100 uM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID418859 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM4 | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID1633708 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as host survival at 33.3 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 28 post infection relative to untreated control | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID346849 | Inhibition of human cloned ERG | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID417933 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 in erythrocytes after 72 hrs by LDH activity | 2009 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 19, Issue:6 | Iodine-catalyzed one-pot synthesis and antimalarial activity evaluation of symmetrically and asymmetrically substituted 3,6-diphenyl[1,2,4,5]tetraoxanes. |
| AID564303 | Antimalarial activity against Plasmodium falciparum IMT K2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter | 2010 | Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9 | Absence of association between piperaquine in vitro responses and polymorphisms in the pfcrt, pfmdr1, pfmrp, and pfnhe genes in Plasmodium falciparum. |
| AID336443 | Antiprotozoal activity against Plasmodium falciparum K1 | 2002 | Journal of natural products, Oct, Volume: 65, Issue:10 | Assessment of the antiprotozoal activity of Galphimia glauca and the isolation of new nor-secofriedelanes and nor-friedelanes. |
| AID72016 | In vitro cytotoxicity against mouse mammary FM3A cells | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12 | Potent antimalarial febrifugine analogues against the plasmodium malaria parasite. |
| AID1414154 | Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 40) level after 24 hrs by ELISA method | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | A phenotypic approach to the discovery of compounds that promote non-amyloidogenic processing of the amyloid precursor protein: Toward a new profile of indirect β-secretase inhibitors. |
| AID1182775 | Half life in Plasmodium berghei infected mouse at 30 mg/kg treated with four once daily doses | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
| AID1728292 | Antiplasmodial activity against Plasmodium falciparum NF54 erythrocytic stages assessed as reduction in [3H]hypoxanthine incorporation measured after 48 hrs by liquid scintillation counting method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities. |
| AID1633716 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as parasitemia cure at 11.1 mg/kg, po dosed once daily on days 0, 1, and 2 days post infection measured on day 28 post infection | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Hybridization of Fluoro-amodiaquine (FAQ) with Pyrimidines: Synthesis and Antimalarial Efficacy of FAQ-Pyrimidines. |
| AID1829855 | Resistance index, ratio of IC50 for antiplasmodial activity against artemisinin-resistant Plasmodium falciparum Cam 3.1 R539 to IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum INDO | |||
| AID1202792 | Half life in human liver microsomes at 1 uM by LC/MS analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives. |
| AID1636356 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID658767 | Inhibition of beta-hematin formation assessed as Ferriprotoporphyrin IX biomineralisation after 24 hrs | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | 2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies. |
| AID1202793 | Half life in mouse liver microsomes at 1 uM by LC/MS analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8 | Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives. |
| AID1494326 | Induction of cell proliferation in C57BL/6 mouse hippocampal neurons in CA2 region assessed as BrdU-incorporation at 0.5 uL/hr, icv for 7 days by immunohistochemical analysis (Rvb = 2.4%) | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID151354 | In vitro efficacy for chloroquine-resistant Plasmodium falciparum D6 | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24 | A prodrug form of a Plasmodium falciparum glutathione reductase inhibitor conjugated with a 4-anilinoquinoline. |
| AID1719380 | Antimalarial activity against Plasmodium falciparum NF54 assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method | 2021 | Bioorganic & medicinal chemistry, 03-01, Volume: 33 | Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines. |
| AID401525 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | Ancistrotanzanine C and related 5,1'- and 7,3'-coupled naphthylisoquinoline alkaloids from Ancistrocladus tanzaniensis. |
| AID158642 | Effective dose ED50 against Plasmodium berghei N in mice (Mus musculus) malaria model after subcutaneous administration | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID1457213 | Antimalarial activity against Plasmodium falciparum 7G8 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID673148 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as increase of mouse survival at 100 mg/kg, po administered 24 hrs post infection (Rvb = 6 to 7 days) | 2012 | Journal of medicinal chemistry, May-10, Volume: 55, Issue:9 | Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. |
| AID1915914 | Antimalarial activity against Plasmodium berghei infected in mouse assessed as reduction in parasitemia in blood at 30 mg/kg, po administered for 4 times starting from 4 to 72 hrs and measured after 96 hrs post infection (Rvb = 0%) | |||
| AID1653749 | Selectivity index, ratio of IC50 for rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis to IC50 for Plasmodium falciparum NF54 measured after 24 hrs in presence of [3H] hypoxanthine | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives. |
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| AID1379021 | Inhibition of Cu2+-mediated aggregation of amyloid beta (1 to 42) (unknown origin) at 50 uM after 24 hrs by thioflavin T fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel cinnamamide-dibenzylamine hybrids: Potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
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| AID1699574 | Inhibition of beta-hematin formation assessed as reduction in hemozoin formation incubated for 5 hrs by NP40 detergent-mediated assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21 | Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and |
| AID1808282 | Modulation of full length human Nurr1 expressed in HEK293T cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NBRE response element assessed as increase in luciferase activity incubated for 18 hrs by luciferase reporter-gene assa | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
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| AID116780 | Mean survival time calculated for the mice which died during 28 day observation period at the dose of 96 mg/kg/day orally | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Geraniol-derived 1,2,4-trioxanes with potent in-vivo antimalarial activity. |
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| AID1558335 | Antiviral activity against Zika virus MR 766 infected in human NSC measured 5 days post infection by CellTiter Blue assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Drugs for the Treatment of Zika Virus Infection. |
| AID607824 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7A assessed as death of all detectable parasites at 4 days dosage of 0.5 to 500 uM using Hema 3 staining by microscopic analysis | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis and biological activities of 4-N-(anilinyl-n-[oxazolyl])-7-chloroquinolines (n=3' or 4') against Plasmodium falciparum in in vitro models. |
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| AID1808438 | Modulation of full length human Nurr1 expressed in SK-N-BE(2) cells co-transfected with luciferase reporter plasmid harboring NurRE response element assessed as increase in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by luciferase reporter | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
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| AID705465 | Antiapicomplexan activity against chloroquine-resistant Plasmodium falciparum TM91-C235 assessed as growth inhibition after 72 hrs by MSF assay | 2012 | Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19 | Salicylanilide inhibitors of Toxoplasma gondii. |
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| AID1677768 | Induction of cytological phenotypic changes in cellular organelles in Parkinson's disease patient human ONS derived C1200080013 cells assessed as changes in features associated with early endosome antigen1 by measuring alteration in EEA1 staining intensit | 2020 | Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21 | Chemical constituents from Macleaya cordata (Willd) R. Br. and their phenotypic functions against a Parkinson's disease patient-derived cell line. |
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| AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
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| AID509178 | Inhibition of TLR7/TLR9-mediated maturation of aldrithiol-2-treated HIV1 MN-stimulated human PBMC assessed as CD83 expressing cells at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
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| AID1717752 | cytotoxicity against golden hamster BHK-21 cells incubated for 72 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
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| AID726921 | Antimalarial activity against Plasmodium falciparum D6 assessed as growth inhibition after 72 hrs by SYBR Green 1-based fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | From a cytotoxic agent to the discovery of a novel antimalarial agent. |
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| AID1415879 | Inhibition of human G9a using biotinylated peptide H3( 1 to 25 residues) as substrate measured after 15 mins in presence of [3H]-SAM by scintillation proximity assay | 2017 | MedChemComm, May-01, Volume: 8, Issue:5 | Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti- |
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| AID731059 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Synthesis of 2-aminomethyl-4-phenyl-1-azabicyclo[2.2.1]heptanes via LiAlH₄-induced reductive cyclization of 2-(4-chloro-2-cyano-2-phenylbutyl)aziridines and evaluation of their antimalarial activity. |
| AID1156429 | Antiplasmodial activity against chloroquine-, pyrimethamine- and proguanil-resistant Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by SYBR Green I fluorescence-based method | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Synthesis and in vitro evaluation of 4-trichloromethylpyrrolo[1,2-a]quinoxalines as new antiplasmodial agents. |
| AID525276 | Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 trophozoites assessed as inhibition of parasite growth at 50 nM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID1327389 | Antiplasmodial activity against chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 measured after 48 hrs by pLDH assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin. |
| AID587702 | Inhibition of Plasmodium falciparum falcipain 3 incubated with compound for 10 mins before addition of 25 uM Z-Leu-Arg-AMC substrate by fluorescence spectrophotometry | 2011 | European journal of medicinal chemistry, Mar, Volume: 46, Issue:3 | Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials. |
| AID118133 | The compound was tested in vivo antimalarial response against multidrug-resistant Plasmodium yoelii in Swiss mice (Mus musculus) at a dose of 48 (mg/kg/day) after 7 days | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Photo-oxygenation of geraniol: synthesis of a novel series of hydroxy-functionalized anti-malarial 1,2,4-trioxanes. |
| AID159030 | Antimalarial activity against Plasmodium falciparum NF54 | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15 | Photo-oxygenation of geraniol: synthesis of a novel series of hydroxy-functionalized anti-malarial 1,2,4-trioxanes. |
| AID630758 | Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse assessed as mean survival time at 100 mg/kg, po administered as single dose | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21 | Novel orally active antimalarial thiazoles. |
| AID1143191 | Water-lipid distribution coefficient, log D of the compound at pH 7.4 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
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| AID403581 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation assay | 1997 | Journal of natural products, Jul, Volume: 60, Issue:7 | New anti-HIV-1, antimalarial, and antifungal compounds from Terminalia bellerica. |
| AID703711 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBC after 72 hrs by parasite lactate dehydrogenase assay | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID1306904 | Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead. |
| AID1124790 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected after 72 hrs by Malaria SYBR Green I-staining based fluorescence assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7 | Synthesis and evaluation of new diaryl ether and quinoline hybrids as potential antiplasmodial and antimicrobial agents. |
| AID1880208 | Antiviral activity against HCoV-229E infected in HEL 299 cells assessed as reduction in virus-induced cytopathic effect preincubated with compound followed by viral infection and measured after 7 days by MTS cell viability assay | 2022 | ACS medicinal chemistry letters, May-12, Volume: 13, Issue:5 | Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity. |
| AID277603 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore. |
| AID1069372 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by flow cytometry | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | 1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: synthesis and antimalarial evaluation. |
| AID1808449 | Modulation of full length human Nurr1 expressed in PC12 cells co-transfected with RXRalpha and luciferase reporter plasmid harboring NurRE response element assessed as decrease in luciferase activity at 1.95 to 125 uM incubated for 18 hrs by luciferase re | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24 | Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1. |
| AID272295 | Binding affinity to plasmid pGL3-CV assessed as retardation of movement in gel at 1 mM | 2006 | Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22 | Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery. |
| AID360324 | Antiplasmodial activity after 24 hrs against chloroquine-sensitive, mefloquine-resistant Plasmodium falciparum D6 infected human erythrocytes by [G-3H]hypoxanthine uptake | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | In vitro antiplasmodial activity of extracts of Tristaniopsis species and identification of the active constituents: ellagic acid and 3,4,5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside. |
| AID1383218 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum RKL9 infected in red blood cells assessed as reduction in mature schizonts formation after 24 hrs by Giemsa-staining based assay | 2018 | European journal of medicinal chemistry, Apr-10, Volume: 149 | Pyrazole-pyrazoline as promising novel antimalarial agents: A mechanistic study. |
| AID1489613 | Antimalarial activity against mefloquine/chloroquine/atovaquone/pyrimethamine-resistant Plasmodium falciparum TM90-C2B infected in human type A-positive erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies. |
| AID1143196 | Inhibition of hemozoin-like crystal formation after 5 days | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1373907 | Inhibition of beta-hematin formation assessed as reduction in acetate buffer-initiated hemozoin formation measured after 48 hrs | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
| AID1433142 | Antiviral activity against Respiratory syncytial virus infected in human HeLa cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID352676 | Antiplasmodial activity as reduced parasitaemia against chloroquine-resistant Plasmodium yoelii N67 infected Swiss mice (Mus musculus) at 10 mg/kg/day peroral dose after 4 days | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9 | Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials. |
| AID412380 | Inhibition of beta-hematin assessed as molar equivalents at pH 2.7 after 18 hrs by spectrophotometric microassay relative to hemin | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials. |
| AID519265 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum K1Hf in presence of 5 uM verapamil by [3H]hypoxanthine incorporation assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Drug-regulated expression of Plasmodium falciparum P-glycoprotein homologue 1: a putative role for nuclear receptors. |
| AID71879 | Cytotoxicity of compound was tested against mouse mammary tumor FM3A cells | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | New semisynthetic quassinoids with in vivo antimalarial activity. |
| AID333069 | Antitubercular activity against Mycobacterium tuberculosis H37Rv | 2004 | Journal of natural products, Aug, Volume: 67, Issue:8 | Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases. |
| AID343754 | Cytotoxicity against human K562 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | Novel amodiaquine congeners as potent antimalarial agents. |
| AID1558339 | Cytotoxicity against human NSC after 5 days by CellTiter Blue assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Drugs for the Treatment of Zika Virus Infection. |
| AID366979 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum THAI/Thailand as [3H]hypoxanthine uptake after 24 hrs by semi-automated micro dilution | 2008 | European journal of medicinal chemistry, Oct, Volume: 43, Issue:10 | Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline. |
| AID287845 | Antimalarial activity as parasitaemia after 14 days against Plasmodium berghei NK65 infected JCL-ICR mice (Mus musculus) at 50 mg/kg | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Antimalarial activity of 1-aryl-3,3-dialkyltriazenes. |
| AID1228727 | Antiviral activity against Chikungunya virus strain 899 infected in african green monkey Vero cells assessed as inhibition of virus induced cell death measured after 7 days | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID691747 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as growth inhibition after 72 hrs by DAPI staining | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp. |
| AID1594581 | Antiplasmodial activity against GFP-transfected Plasmodium berghei ANKA infected in NMRI mouse assessed as mean survival days at 50 mg/kg/day, ip for consecutive 4 days (4, 24, 48 and 72 hrs post infection) and measured up to 20 days after infection (Rvb | 2019 | Bioorganic & medicinal chemistry, 05-15, Volume: 27, Issue:10 | Synthesis and structure-activity relationships for new 6-fluoroquinoline derivatives with antiplasmodial activity. |
| AID1814063 | Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at 60 mM at pH 6 in presence of glucose measured after 48 hrs by visual analysis | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH. |
| AID1778134 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1/Colombia infected in human red blood cells assessed as reduction in [3H]-hypoxanthine incorporation measured after 24 hrs liquid scintillation counting method | 2021 | Journal of natural products, 04-23, Volume: 84, Issue:4 | Targeted Isolation of Hemitheion from |
| AID1255406 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in NMRI mouse assessed as inhibition of parasitemia at 10 mg/kg, ip qd administered as single dose on day 0 to 4 of exposure measured on day 5 post exposure by FACS method relat | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Discovery and optimisation studies of antimalarial phenotypic hits. |
| AID1225323 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D6 in human erythrocyte after 72 hrs by SYBR Green I assay | 2015 | Journal of natural products, Mar-27, Volume: 78, Issue:3 | Depsipeptide companeramides from a Panamanian marine cyanobacterium associated with the coibamide producer. |
| AID1182795 | Resistance index, ratio of IC50 for Plasmodium falciparum W2 to IC50 for Plasmodium falciparum NF54 | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
| AID666880 | Antimalarial activity against Plasmodium berghei ANKA expressing GFP infected in Sprague-Dawley rat assessed as mean survival days of host at 3 mg/kg, po administered as single dose | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. |
| AID558844 | Antimalarial activity against Plasmodium falciparum IMT K2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID1221964 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID635310 | Selectivity index, ratio of IC50 for mouse 3T3 cells to IC50 for chloroquine-resistant Plasmodium falciparum W2mef | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Synthesis and antimalarial evaluation of novel isocryptolepine derivatives. |
| AID454902 | Selectivity index, IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for chloroquine-sensitive Plasmodium falciparum D6 | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline-triazine conjugates. |
| AID643383 | Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets. |
| AID1168876 | Binding affinity to heme assessed as inhibition of beta-hematin formation measured as compound IC50 to haemin molar ratio by BHIA assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID311097 | Effect on erythrocyte shape in human erythrocytes assessed as echinocytes at 50 ug/mL after 48 hrs | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Transformations of manool. tri- and tetracyclic norditerpenoids with in vitro activity against Plasmodium falciparum. |
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| AID1572686 | Antimalarial activity against Plasmodium berghei NK65 infected in mouse assessed as reduction in parasite growth at 20 mg/kg, po administered daily for 3 consecutive days and measured on day 7 post parasite inoculation relative to control | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | New hybrid trifluoromethylquinolines as antiplasmodium agents. |
| AID159029 | In vitro antimalarial activity for Plasmodium falciparum NF54 | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | In vivo active antimalarial isonitriles. |
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| AID554562 | Cytotoxicity against african green monkey Vero cells upto 10 uM after 72 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID416484 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates. |
| AID1649916 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Triazole derivatives and their antiplasmodial and antimalarial activities. |
| AID1391092 | Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as increase in CTFalpha level at 3 uM measured after 24 hrs by Western blot analysis relative to chloroquine | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | New phenylaniline derivatives as modulators of amyloid protein precursor metabolism. |
| AID1391101 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in normal type A human erythrocytes incubated for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | Adamantane amine-linked chloroquinoline derivatives as chloroquine resistance modulating agents in Plasmodium falciparum. |
| AID27167 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
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| AID360325 | Antiplasmodial activity after 24 hrs against chloroquine-resistant, mefloquine-sensitive Plasmodium falciparum W2 infected human erythrocytes by [G-3H]hypoxanthine uptake | 2001 | Journal of natural products, May, Volume: 64, Issue:5 | In vitro antiplasmodial activity of extracts of Tristaniopsis species and identification of the active constituents: ellagic acid and 3,4,5-trimethoxyphenyl-(6'-O-galloyl)-O-beta-D-glucopyranoside. |
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| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
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| AID1188916 | Cytotoxicity against african green monkey Vero cells after 2 days by resazurin assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents. |
| AID459098 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O+ erythrocytes by parasite LDH assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo. |
| AID1057131 | Efflux ratio of apparent permeability from basolateral to apical side to apical to basolateral side in MDCK cells | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum. |
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| AID644259 | Antiplasmodial activity against chloroquine-sensitive ring-stage Plasmodium falciparum 3D7 assessed as [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counter | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Synthesis and antiplasmodial evaluation of novel chromeno[2,3-b]chromene derivatives. |
| AID1182789 | Antiplasmodial activity against Plasmodium falciparum 7G8 harboring mutations conferring drug-resistance by SYBR-green based assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds. |
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| AID316967 | Antimalarial activity against Plasmodium falciparum W2 in parasite LDH assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Synthesis, thermal stability, antimalarial activity of symmetrically and asymmetrically substituted tetraoxanes. |
| AID320716 | Resistance index, IC50 for chloroquine-resistant Plasmodium falciparum FcB1 to chloroquine-sensitive Plasmodium falciparum Thai | 2008 | Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2 | Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents. |
| AID427683 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13 | Synthesis and in vitro antiplasmodial evaluation of 4-anilino-2-trichloromethylquinazolines. |
| AID334843 | Antimalarial activity after 24 hrs against Plasmodium falciparum W2 infected in type A+ human erythrocytes by [3H]hypoxanthine uptake | 1993 | Journal of natural products, Aug, Volume: 56, Issue:8 | Cytotoxic and antimalarial alkaloids from the bulbs of Crinum amabile. |
| AID1814042 | Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at pH 8 in presence of glucose measured after 48 hrs by visual analysis | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH. |
| AID718287 | Selectivity index, ratio of CC50 for african green monkey Vero cells to EC50 for Chikungunya virus 899 | 2012 | Journal of natural products, Dec-28, Volume: 75, Issue:12 | Prostratin and 12-O-tetradecanoylphorbol 13-acetate are potent and selective inhibitors of Chikungunya virus replication. |
| AID1538874 | Antiplasmodial activity against Plasmodium falciparum infected in human RBC assessed as reduction in parasite LDH activity by spectrophotometric assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway. |
| AID502039 | Antimicrobial activity against Trichomonas vaginalis GT3 after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas. |
| AID1190840 | Antiplasmodial activity against Plasmodium falciparum NF54 by SYBR Green-based method | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Synthesis and biological evaluation of adamantane-based aminophenols as a novel class of antiplasmodial agents. |
| AID352672 | Selectivity index, ratio of IC50 for african green monkey (Cercopithecus aethiops) Vero cells to IC50 for Plasmodium falciparum 3D7 | 2009 | Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9 | Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials. |
| AID554754 | Antimalarial activity against Plasmodium berghei NK-65 infected in Swiss Webster mouse assessed as mean survival time at 30 mg/kg, ip QD for 3 days administered 2 hrs post infection | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Synthesis and antimalarial activities of cyclen 4-aminoquinoline analogs. |
| AID464869 | Antiparasitic activity against Plasmodium falciparum 3D7 at erythrocytic stage | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi. |
| AID1057133 | Half life in mouse plasma at 1 mM by LC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum. |
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| AID1574995 | Antiplasmodial activity against chloroquine-resistant asexual blood stage of Plasmodium falciparum K1 infected in human RBC assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured afte | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria. |
| AID1433154 | Antiviral activity against influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect by visual scoring analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids. |
| AID159724 | Parasitaemia (%) in tail blood smears of Plasmodium berghei infected ICR mice (Mus musculus) at 20 mg/kg/day after 4 days | 2002 | Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3 | New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor. |
| AID598733 | Antiprion activity against Chandler strain of sheep scrapie prion protein infected in mouse SMB cells assessed as clearance of disease-associated scrapie prion protein | 2011 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12 | 2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads. |
| AID1155329 | Antimalarial activity against asexual blood stage of Plasmodium falciparum 3D7 infected in human serum assessed as [3H]hypoxanthine incorporation incubated for 48 hrs prior to 3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages. |
| AID1169349 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 72 hrs by cell based assay | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22 | Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group. |
| AID323675 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum RSA11 | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
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| AID158844 | Inhibitory activity against Plasmodium falciparum D6 | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates. |
| AID323678 | Reduction of [3H]chloroquine uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains. |
| AID504272 | Distribution coefficient, log D of the compound at pH 5.2 | 2010 | Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18 | Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines. |
| AID378803 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 as parasite DNA microfluorimetric assay | 2006 | Journal of natural products, Oct, Volume: 69, Issue:10 | Antiplasmodial metabolites isolated from the marine octocoral Muricea austera. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID157839 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 | 2000 | Journal of medicinal chemistry, Feb-24, Volume: 43, Issue:4 | Phenyl beta-methoxyacrylates: a new antimalarial pharmacophore. |
| AID601644 | Plasma protein binding in human by albumin chromatographic method | 2011 | Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11 | Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1200886 | Antiplasmodial activity against Plasmodium falciparum W2 | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Antiplasmodial activity: the first proof of inhibition of heme crystallization by marine isonitriles. |
| AID773687 | Inhibition of hemozoin-like crystal formation after 5 days | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19 | Structural optimization of quinolon-4(1H)-imines as dual-stage antimalarials: toward increased potency and metabolic stability. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
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| AID1628566 | Inhibition of beta-hematin | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
| AID366960 | Cytotoxicity against human KB cells after 48 hrs by alamar blue assay | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | Synthesis and structure-activity relationship of 3-phenylquinoxaline 1,4-di-N-oxide derivatives as antimalarial agents. |
| AID123179 | Number of Plasmodium berghei infected mice died on day 12 at 40 mg/kg | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Bisquinolines. 2. Antimalarial N,N-bis(7-chloroquinolin-4-yl)heteroalkanediamines. |
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| AID1188915 | Antimalarial activity against Plasmodium falciparum K1 after 72 hrs by SYBR Green fluorescence assay | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8 | Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents. |
| AID444050 | Fraction unbound in human plasma | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID1351060 | Inhibition of acetate buffer-initiated beta-hematin polymerization at 50 uM measured after 48 hrs relative to control | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis, β-hematin inhibition studies and antimalarial evaluation of new dehydroxy isoquine derivatives against Plasmodium berghei: A promising antimalarial agent. |
| AID441598 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as inhibition of schizont maturation at 0.25 ug/ml after 36-40 hrs relative to control | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Synthesis of new chalcone derivatives containing acridinyl moiety with potential antimalarial activity. |
| AID1700305 | Antimalarial activity against Plasmodium berghei NK65 infected in mouse assessed as increase in mouse survival at 20 mg/kg, po administered for 3 days and observed for 7 days | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission. |
| AID441658 | Cytotoxicity against rat L6 cells | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities. |
| AID1815846 | Hemolytic activity against human erythrocytes at <=10 uM incubated for 1 hr by microplate reader assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Indole-Containing Pyrazino[2,1- |
| AID228277 | Cellular accumulation ratio (CAR) for chloroquine sensitive HB3 strain of Plasmodium falciparum | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | Synthesis, antimalarial activity, and molecular modeling of tebuquine analogues. |
| AID338768 | Antimalarial activity against Plasmodium falciparum W2 in human erythrocytes after 24 hrs by [3H]hypoxanthine uptake | |||
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| AID768184 | Binding affinity to monomeric heme (unknown origin) in HEPES buffer at pH 7.4 at 1 to 25 uM by UV-visible spectrophotometry | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies. |
| AID158826 | Inhibition of Plasmodium berghei in mice (Mus musculus) after 15 mg/kg subcutaneous dose (experiment 1) | 2004 | Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5 | Antimalarial activity of phenazines from lapachol, beta-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID734081 | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis, cytotoxicity and antiplasmodial activity of novel ent-kaurane derivatives. |
| AID775958 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | In vitro antimalarial activity, β-haematin inhibition and structure-activity relationships in a series of quinoline triazoles. |
| AID672050 | Inhibition of Plasmodium falciparum phosphoethanolamine methyltransferase using phospethanolamine as substrate by radiochemical assay in presence of S-adenosylmethionine | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15 | Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine. |
| AID1538872 | Inhibition of bovine liver DHFR using FH2 as substrate incubated for 2 mins followed by substrate addition | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway. |
| AID346858 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3 in human erythrocytes after 48 hrs by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. |
| AID547315 | Antimalarial activity against Plasmodium falciparum | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | In vitro activities of quinine and other antimalarials and pfnhe polymorphisms in Plasmodium isolates from Kenya. |
| AID509198 | Inhibition of TLR7/TLR9-mediated upregulation of PDL1 expression in aldrithiol-2-treated HIV1 MN-stimulated human PBMC at 100 uM after 20 hrs by flow cytometry | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Chloroquine modulates HIV-1-induced plasmacytoid dendritic cell alpha interferon: implication for T-cell activation. |
| AID277606 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore. |
| AID402129 | Antimalarial activity as reduced parasitaemia against Plasmodium berghei yoelii infected Swiss albino mice (Mus musculus) at 5 mg/kg/day peroral dose for 4 days | 1997 | Journal of natural products, Jul, Volume: 60, Issue:7 | In vitro and in vivo antiplasmodial activity of cryptolepine and related alkaloids from Cryptolepis sanguinolenta. |
| AID1201059 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Synthesis of isocryptolepine analogues and their structure-activity relationship studies as antiplasmodial and antiproliferative agents. |
| AID647318 | Therapeutic index, ratio of IC50 for human HeLa cells to IC50 for ring stage chloroquine-sensitive Plasmodium falciparum 3D7 | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Stilbene-chalcone hybrids: design, synthesis, and evaluation as a new class of antimalarial scaffolds that trigger cell death through stage specific apoptosis. |
| AID405006 | Selectivity for chloroquine-resistant Plasmodium falciparum K1 over chloroquine-sensitive Plasmodium falciparum NF54 as IC50 ratio by [3H]hypoxanthine uptake | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID284885 | Anti-infective activity against Plasmodium falciparum D6 infected red blood cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2 | Synthesis and evaluation of isosteres of N-methyl indolo[3,2-b]-quinoline (cryptolepine) as new antiinfective agents. |
| AID322591 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 by LDH release assay | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | S-Euglobals: biomimetic synthesis, antileishmanial, antimalarial, and antimicrobial activities. |
| AID404793 | Inhibition of haemozoin formation at pH 5.2 after 18 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | 4-N-, 4-S-, and 4-O-chloroquine analogues: influence of side chain length and quinolyl nitrogen pKa on activity vs chloroquine resistant malaria. |
| AID300104 | Antimalarial activity against chloroquine, pyrimethamine and cycloguanil-resistant Plasmodium falciparum VS1 after 24 hrs | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Anti-malarial activity of N6-modified purine analogues. |
| AID1575014 | Antimalarial activity against GFP-fused Plasmodium berghei ANKA infected in NMRI mouse assessed as host mean survival time at 30 mg/kg, po administered for 4 consecutive days | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria. |
| AID703713 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation incubated for 48 hrs prior to [3H]hypoxanthine addition measured after 48 hrs by liquid | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15 | Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling. |
| AID419131 | Binding affinity to heme assessed as binding constant for stepwise binding of 2 molecules of heme to 1 equivalent of drug in presence of 1.22 mM TX-100 by UV-visible spectroscopy | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID756891 | Antiprotozoal activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
| AID1472106 | Decrease in hemozoine formation in chloroquine-sensitive synchronized ring stage of Plasmodium falciparum NF54 after 32 hrs by flow cytometric analysis | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 | 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. |
| AID256107 | Antileishmanial activity against leishmania amazonensis promastigotes stage; ND = Not determined | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22 | New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities. |
| AID422747 | Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum W2 by pLDH activity | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1 | Indolizidine, antiinfective and antiparasitic compounds from Prosopis glandulosa var. glandulosa. |
| AID441599 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as inhibition of schizont maturation at 0.125 ug/ml after 36-40 hrs relative to control | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Synthesis of new chalcone derivatives containing acridinyl moiety with potential antimalarial activity. |
| AID1391100 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in normal type A human erythrocytes incubated for 72 hrs by spectrophotometry based parasite lactate dehydrogenase assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | Adamantane amine-linked chloroquinoline derivatives as chloroquine resistance modulating agents in Plasmodium falciparum. |
| AID444051 | Total clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
| AID445253 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes after 48 hrs assessed as [3H]hypoxanthine incorporation by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles. |
| AID1846639 | Antiprotozoal activity against erythrocytic stage Plasmodium falciparum NF54 assessed as parasite growth inhibition incubated for 48 hrs by 3H-hypoxanthine incorporation assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9 | Synthesis and Biological Evaluation of Natural-Product-Inspired, Aminoalkyl-Substituted 1-Benzopyrans as Novel Antiplasmodial Agents. |
| AID360364 | Antimalarial activity after 48 hrs against Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake | 2007 | The Journal of biological chemistry, Jan-26, Volume: 282, Issue:4 | In vitro efficacy, resistance selection, and structural modeling studies implicate the malarial parasite apicoplast as the target of azithromycin. |
| AID564242 | Antiplasmodial activity against Plasmodium falciparum harboring wild type pfcrt-76 and wild type pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1. |
| AID473009 | Inhibition of Plasmodium falciparum recombinant falcipain-2 using Cbz-Leu-Arg-AMC as substrate by standard fluorescence assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids. |
| AID567865 | Selectivity index, IC50 for african green monkey Vero cells to IC50 for Trypanosoma cruzi 320I01 amastigotes | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | 4-anilinoquinoline triazines: a novel class of hybrid antimalarial agents. |
| AID1368010 | Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24 | Ionic liquid mediated stereoselective synthesis of alanine linked hybrid quinazoline-4(3H)-one derivatives perturbing the malarial reductase activity in folate pathway. |
| AID1450025 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 measured after 72 hrs by DAPI staining based high throughput screening assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Antiplasmodial β-triketones from the flowers of the Australian tree Angophora woodsiana. |
| AID377918 | Antiplasmodial activity against Plasmodium falciparum NF54 in human erythrocytes by [3H]hypoxanthine uptake | 2000 | Journal of natural products, Nov, Volume: 63, Issue:11 | Ancistroealaines A and B, two new bioactive naphthylisoquinolines, and related naphthoic acids from Ancistrocladus ealaensis. |
| AID1439512 | Antimalarial activity against Plasmodium falciparum infected in RBC after 5 days by MTT assay | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Novel 2,3-disubstituted quinazoline-4(3H)-one molecules derived from amino acid linked sulphonamide as a potent malarial antifolates for DHFR inhibition. |
| AID1359555 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 by [3H]-hypoxanthine incorporation assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery. |
| AID393082 | Antimalarial activity as reduced parasitaemia against Plasmodium berghei NK65 infected ICR mice (Mus musculus) at 30 mg/kg/day peroral dose at day 4 | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4 | Pharmacodynamics and pharmacokinetics studies of phenoxazinium derivatives for antimalarial agent. |
| AID1378962 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Quinoline hybrids and their antiplasmodial and antimalarial activities. |
| AID536137 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 72 hrs by SYBR Green I fluorescence based method | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | 4-Aminoquinoline derived antimalarials: synthesis, antiplasmodial activity and heme polymerization inhibition studies. |
| AID118000 | Antimalarial activity in mice (Mus musculus), infected with Plasmodium yoelii NS. activity is expressed as the percent of parasitaemia observed in mice (Mus musculus) at end of 4-day test at a concentration of 1 mg/kg in experiment 1 | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue. |
| AID1203042 | Antiproliferative activity against human HCC827 cells after 72 hrs by SRB method | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells. |
| AID558835 | Antimalarial activity against Plasmodium falciparum IMT Guy assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Atorvastatin is a promising partner for antimalarial drugs in treatment of Plasmodium falciparum malaria. |
| AID1494296 | Induction of disaggregation of amyloid beta (1 to 42) (unknown origin) fibrils at compound to amyloid beta ratio of 1:1 after 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID442259 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes after 96 hrs by [3H]hypoxanthine incorporation assay | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24 | Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach. |
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| AID347212 | Antimalarial schizonticidal activity against Plasmodium falciparum 3D7 infected erythrocytes at 2.5 ug/ml after 30-39 hrs | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Organocatalyzed highly atom economic one pot synthesis of tetrahydropyridines as antimalarials. |
| AID158366 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 (CDC/Sierra Leone I) | 1995 | Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26 | In vitro antimalarial activity of chalcones and their derivatives. |
| AID760224 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition after 24 hrs by [3H]-hypoxathine incorporation assay | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids. |
| AID1274381 | Antimalarial activity against Plasmodium berghei ANKA infected in C57Bl6 mouse at 160 mg/kg/day, po measured on day 3 to 5 by Thompson test | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? |
| AID482878 | Inhibition of Plasmodium falciparum recombinant falcipain-2 expressed in Escherichia coli after 20 min using Cbz-Phe-Arg-AMC as substrate by spectrofluorometry | 2009 | Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18 | On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences. |
| AID1494309 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as metabolic rate constant at 100 uM up to 180 mins by HPLC-UV analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5 | Design, Synthesis, and Evaluation of Orally Bioavailable Quinoline-Indole Derivatives as Innovative Multitarget-Directed Ligands: Promotion of Cell Proliferation in the Adult Murine Hippocampus for the Treatment of Alzheimer's Disease. |
| AID1373906 | Cytotoxicity against human Jurkat cells after 20 hrs by propidium iodide staining based flow cytometry | 2018 | Bioorganic & medicinal chemistry, 02-15, Volume: 26, Issue:4 | Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate. |
| AID1335177 | Antimalarial activity against chloroquine-sensitive asexual erythrocyte stage of Plasmodium falciparum NF54 infected in human type O+ erythrocytes assessed as growth inhibition incubated for 48 hrs by NBT dye based LDH release assay | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2 | Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active against |
| AID1538876 | Cytotoxicity against human RBC assessed as reduction in cell viability by MTT assay | 2019 | Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16 | Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway. |
| AID1457076 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by YOYO-1 dye based flow cytometric analysis | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. |
| AID1555141 | Inhibition of Plasmodium falciparum N-terminal His6-tagged falcipain-2 (35 residues) expressed in Escherichia coli M15 pREP4 using Z-Lue-Arg-AMC as substrate measured after 30 mins by spectrofluorometric method | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials. |
| AID396978 | Inhibition of acetate buffer-induced hemozoin formation at 1.25 to 25 mM/well after 48 hrs | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities. |
| AID1661405 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcM29 infected in erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition and measured after 18 hrs by t | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | β-Hydroxy- and β-Aminophosphonate Acyclonucleosides as Potent Inhibitors of |
| AID1168871 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum 3D7 | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives. |
| AID1336739 | Resistance index, ratio of IC50 for chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human RBC to IC50 for chloroquine-sensitive Plasmodium falciparum NF54 infected in human RBC | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity. |
| AID243141 | Binding constant dissolved in DMSO against hematin receptor at pH 7.4 (HEPES Buffer) upon incubation at 30 degree C | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: design, construction, characterization, and pharmacology of metaquine. |
| AID1445973 | Gametocytocidal activity against GFP-fused Plasmodium berghei liver stage gametocytes infected in human HepG2-A16-CD81-EGFP cells after 48 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14 | 3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally. |
| AID1204114 | Cytotoxic activity against human HeLa cells assessed as cell viability at 10 ug/ml incubated for 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11 | New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo. |
| AID1771332 | Antimalarial activity against Plasmodium falciparum TM90C2b harbouring Pf-crt, Pf-mdrl,Pfd-hfr, Pf-cytbQ0 mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counti | 2021 | Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17 | Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials. |
| AID525275 | Antigametocyte activity against drug-resistant ring stage Plasmodium falciparum Dd2 schizonts assessed as inhibition of parasite growth at 50 nM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID1624374 | Antimalarial activity against Plasmodium berghei ANKA infected in Swiss mouse assessed as parasitaemia at 10 mg/kg, ip administered once daily for 5 days measured on 11 days post infection by flow cytometry (Rvb = 44%) | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | Amino acid based prodrugs of a fosmidomycin surrogate as antimalarial and antitubercular agents. |
| AID576577 | Antimalarial activity against Plasmodium vivax with >50% parasites at ring stage infected in human erythrocytes assessed as growth inhibition after 30 to 50 hrs by microscopic analysis using giemsa staining | 2010 | Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12 | In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax. |
| AID1228555 | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum V1/S assessed as inhibition of parasite growth | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides. |
| AID539292 | Resistance index, ratio of IC50 for chloroquine-sensitive Plasmodium falciparum D10 to IC50 for chloroquine-resistant Plasmodium falciparum Dd2 | 2010 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 20, Issue:23 | Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity. |
| AID1126849 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1 infected in RBC assessed as inhibition of [3H]-hypoxanthine incorporation after 48 hrs by beta-counting | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | 2-Aryl-3H-indol-3-ones: synthesis, electrochemical behaviour and antiplasmodial activities. |
| AID1915895 | Selectivity index, ratio of IC50 for cytotoxicity against HEK293 cells to IC50 for antiplasmodial activity against chloroquine-sensitive asexual blood stage Plasmodium falciparum 3D7 | |||
| AID492436 | Antimalarial activity against Plasmodium falciparum 3D7 | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9 | Antimalarials from nature. |
| AID1700303 | Antimalarial activity against Plasmodium berghei NK65 infected in mouse assessed as parasite growth at 20 mg/kg, po administered for 3 days and measured on day 7 Giemsa staining based assay relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Antimalarial and anti-inflammatory activities of new chloroquine and primaquine hybrids: Targeting the blockade of malaria parasite transmission. |
| AID389357 | Cytotoxicity against human MRC5 cells after 5 days by MTT assay | 2008 | Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20 | New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: synthesis, and in vitro antimalarial activity. |
| AID258361 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1 | 2006 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1 | Design, synthesis and in vitro antimalarial activity of an acylhydrazone library. |
| AID776774 | Aqueous solubility of the compound | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Flavones as isosteres of 4(1H)-quinolones: discovery of ligand efficient and dual stage antimalarial lead compounds. |
| AID1628545 | Ratio of compound Ka to 3,5-Dinitro-N-(pyridin-4-yl)benzamide Ka for binding affinity to Fe(3)PP9 in hematin solution at pH 7.5 by titration-based UV-vis spectrophotometrical analysis | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13 | Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum. |
| AID1899009 | Selectivity index, ratio of IC50 for antiplasmodial activity against CQ-susceptible Plasmodium falciparum 3D7 to IC50 for antiplasmodial activity against CQ-resistant Plasmodium falciparum W2 by SYBR Green 1 dye based fluorescence assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Design, synthesis, and characterization of novel aminoalcohol quinolines with strong in vitro antimalarial activity. |
| AID768491 | Antimalarial activity against Plasmodium falciparum 3D7 infected in RBC assessed as growth inhibition after 48 hrs by SYBR Green-I fluorescence assay | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15 | Novel conjugated quinoline-indoles compromise Plasmodium falciparum mitochondrial function and show promising antimalarial activity. |
| AID335153 | Selectivity index, ED50 for human KB cells to ED50 for chloroquine-sensitive Plasmodium falciparum D6 | 1993 | Journal of natural products, Sep, Volume: 56, Issue:9 | Cytotoxic and antimalarial alkaloids from the tubers of Stephania pierrei. |
| AID138101 | Dose needed to increase the survival of treated animals(mouse), to twice the number of days | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials. |
| AID763625 | Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Plasmodium falciparum | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents. |
| AID1732464 | Antimalarial activity against Plasmodium falciparum 3D7 incubated for 72 hrs by LDH assay | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion. |
| AID717064 | Antimalarial activity against schizonts of chloroquine-sensitive Plasmodium berghei ANKA 2.34 assessed as chemosuppression of schizont numbers at 200 uM after 16 hrs relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Linear and cyclic dipeptides with antimalarial activity. |
| AID1174521 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of parasite growth after 72 hrs by parasite LDH release assay | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | 4-Aminoquinoline-pyrimidine hybrids: synthesis, antimalarial activity, heme binding and docking studies. |
| AID414512 | Partition coefficient, log P of the compound | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine. |
| AID337518 | Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum W2 infected type A+ human erythrocytes by [3H]hypoxanthine uptake | 1993 | Journal of natural products, Jan, Volume: 56, Issue:1 | Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta. |
| AID160054 | In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR3 | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity. |
| AID496888 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Quinolines and structurally related heterocycles as antimalarials. |
| AID461169 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D10 | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. |
| AID1533533 | Induction of lysosomotropism in human HeLa cells infected with Ebolavirus assessed as increase in fluorescence intensity of acid compartments at 10 uM for 1 hr by Lysosensor DND189 staining based assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
| AID335154 | Selectivity index, ED50 for human KB cells to ED50 for chloroquine-resistant Plasmodium falciparum W2 | 1993 | Journal of natural products, Sep, Volume: 56, Issue:9 | Cytotoxic and antimalarial alkaloids from the tubers of Stephania pierrei. |
| AID609559 | Selectivity index, ratio of CC50 for mouse peritoneal macrophages to IC50 for axenic amastigotes of Leishmania amazonensis | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1804171 | DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\ | 2020 | Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7 | Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs. |
| AID1798279 | In Vitro Ligase Activity Assay from Article 10.1002/prot.21457: \\NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor.\\ | 2007 | Proteins, Oct-01, Volume: 69, Issue:1 | NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor. |
| AID1798278 | In Vitro Ligase Activity Assay from Article 10.1074/jbc.M503780200: \\NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors.\\ | 2005 | The Journal of biological chemistry, Aug-26, Volume: 280, Issue:34 | NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors. |
| AID1799369 | Parasite Proliferation Assay from Article 10.1038/nchembio.87: \\Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility.\\ | 2008 | Nature chemical biology, Jun, Volume: 4, Issue:6 | Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. |
| AID1804127 | No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\ | 2021 | Medicinal research reviews, 01, Volume: 41, Issue:1 | The recent outbreaks of human coronaviruses: A medicinal chemistry perspective. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1345402 | Human MRGPRX1 (Class A Orphans) | 2009 | Cell, Dec-24, Volume: 139, Issue:7 | Sensory neuron-specific GPCR Mrgprs are itch receptors mediating chloroquine-induced pruritus. |
| AID602156 | Novartis GNF Liver Stage Dataset: Malariabox Annotation | 2011 | Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061 | Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 6056 (39.71) | 18.7374 |
| 1990's | 2359 (15.47) | 18.2507 |
| 2000's | 2514 (16.49) | 29.6817 |
| 2010's | 2970 (19.48) | 24.3611 |
| 2020's | 1350 (8.85) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (115.58) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 763 (4.65%) | 5.53% |
| Reviews | 1,006 (6.13%) | 6.00% |
| Case Studies | 1,185 (7.22%) | 4.05% |
| Observational | 22 (0.13%) | 0.25% |
| Other | 13,429 (81.86%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Intermittent Preventive Treatment With Azithromycin-containing Regimens for the Prevention of Malarial Infections and Anaemia and the Control of Sexually Transmitted Infections in Pregnant Women in Papua New Guinea [NCT01136850] | Phase 3 | 2,793 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Experimental Human Malaria Infection After Immunization With Plasmodium Falciparum Sporozoites Under Chloroquine Prophylaxis [NCT01236612] | 25 participants (Actual) | Interventional | 2011-04-30 | Completed | |||
| A Phase I Study to Investigate the Hemolytic Potential of Tafenoquine in Healthy Subjects With Glucose-6-phosphate Dehydrogenase Deficiency and the Safety and Tolerability of Tafenoquine in Acute Plasmodium Vivax Malaria Patients With Glucose-6-phosphate [NCT01205178] | Phase 1 | 192 participants (Actual) | Interventional | 2009-07-02 | Completed | ||
| A Phase III Randomised, Double-blind, Double-dummy, Comparative Study to Assess the Safety and Efficacy of Pyronaridine Artesunate (180:60 mg) Versus Chloroquine (155 mg) in Children and Adult Patients in Korea With Acute P. Vivax Malaria [NCT04368910] | Phase 3 | 30 participants (Actual) | Interventional | 2007-09-06 | Terminated(stopped due to Due to slow recruitment the study was terminated prematurely by the Sponsor after 30 subjects had been included) | ||
| Chloroquine/ Hydroxychloroquine Prevention of Coronavirus Disease (COVID-19) in the Healthcare Setting; a Randomised, Placebo-controlled Prophylaxis Study (COPCOV) [NCT04303507] | 4,652 participants (Actual) | Interventional | 2020-04-29 | Completed | |||
| Open Label, Single Center, Phase 1 Dose Escalation and Extension Trial to Evaluate Safety and Tolerability of Chlorquine as Adjuvant Drug to Standard 4-drug Anti-tuberculosis Therapy in Healthy Volunteers [NCT05443178] | Phase 1 | 16 participants (Anticipated) | Interventional | 2022-01-04 | Recruiting | ||
| Artemether-lumefantrine vs Chloroquine in Patients With Acute Non-severe P. Vivax Malaria in Sabah, Malaysia [NCT02348788] | Phase 3 | 98 participants (Anticipated) | Interventional | 2015-01-31 | Recruiting | ||
| A Phase 2 Randomized, Double-blind, Window of Opportunity Trial Evaluating Clinical and Correlative Effects of Chloroquine as a Novel Therapeutic Strategy in Breast Cancer [NCT02333890] | Phase 2 | 60 participants (Anticipated) | Interventional | 2015-07-31 | Recruiting | ||
| Sanaria PfSPZ Challenge With Pyrimethamine Chemoprophylaxis (PfSPZ-CVac Approach): Phase 1 Dose Escalation Trial to Determine Safety and Development of Protective Efficacy After Exposure to Only Pre-erythrocytic Stages of Plasmodium Falciparum [NCT03083847] | Phase 1 | 55 participants (Actual) | Interventional | 2017-06-05 | Completed | ||
| A Randomised Open Label Study Comparing the Efficacy of Chloroquine/Primaquine, Chloroquine and Artesunate in the Treatment of Vivax Malaria Along the Thai-Burmese Border [NCT01074905] | Phase 3 | 655 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Clinical Trial for Evaluation of Ethnic Differences in Pharmacokinetics of Chloroquine, an Anti-malarial Drug [NCT01366235] | Phase 1 | 10 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| Host and Parasites Factors Contributing to Risk of Plasmodium Re-infection and Morbidity in Elementary School Children in Maprik, East Sepik Province [NCT02143934] | Phase 4 | 524 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Efficacy and Safety of Chloroquine for Plasmodium Vivax in the Philippines in 2016. [NCT05958797] | 74 participants (Actual) | Observational | 2016-01-04 | Completed | |||
| Optimizing the Dose of Tafenoquine for the Radical Cure of Plasmodium Vivax Malaria in Southeast Asia [NCT04704999] | Phase 4 | 700 participants (Anticipated) | Interventional | 2023-09-18 | Not yet recruiting | ||
| A Phase 1, Open-Label, Randomized, Single Dose, Parallel Design Study To Estimate The Relative Bioavailability Of Co Administered Formulations Of Azithromycin Microsphere (AZ) And Chloroquine Test Formulation (CQ) Compared With Co Administered Immediate R [NCT01100060] | Phase 1 | 40 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
| Effect of Sarilumab on Patient-reported Outcomes in Patients With Moderately to Severely Active Rheumatoid Arthritis and With Inadequate Response or Intolerance to Current Conventional Synthetic DMARDs or Tumor Necrosis Factor Inhibitors [NCT03449758] | Phase 4 | 84 participants (Actual) | Interventional | 2018-03-05 | Completed | ||
| Comparative Study Between Chloroquine and Hydroxychloroquine as Therapeutic Modalities for Children and Adolescents With Proliferative Lupus Nephritis [NCT03687905] | 60 participants (Anticipated) | Observational [Patient Registry] | 2018-09-18 | Recruiting | |||
| Genotoxic Stress, Atherosclerosis, and Metabolic Syndrome- Aim 3 [NCT00455403] | 357 participants (Actual) | Interventional | 2006-04-30 | Completed | |||
| Identification of Pre-erythrocytic Target Antigens Induced by Plasmodium Falciparum Sporozoite Immunization Under Chemoprophylaxis [NCT02080026] | 15 participants (Actual) | Interventional | 2014-06-30 | Completed | |||
| Chloroquine (CQ) Prophylaxis for Health Care Workers at Risk for COVID [NCT04349371] | Phase 2 | 8 participants (Actual) | Interventional | 2020-04-21 | Terminated(stopped due to Low enrollment.) | ||
| Chemoprophylaxis and Plasmodium Falciparum NF54 Sporozoite Immunization Challenged by Heterologous Infection [NCT02098590] | 40 participants (Actual) | Interventional | 2014-10-31 | Completed | |||
| Assessing Chloroquine Resistance of Plasmodium Vivax in Malaria Endemic Area [NCT02118090] | Phase 4 | 73 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Efficacy and Safety of Artemether-lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria and Chloroquine for Plasmodium Vivax in the Philippines From 2013-2014 [NCT04222088] | 159 participants (Actual) | Observational | 2013-05-01 | Completed | |||
| Phase II, Randomized, Double-blind, Controlled Clinical Trial Evaluating the Efficacy and Safety of Chloroquine + Low Dose Losartan Compared to Chloroquine Monotherapy in Subjects With SARS-CoV-2 Pneumonia [NCT04428268] | Phase 2 | 0 participants (Actual) | Interventional | 2020-03-10 | Withdrawn(stopped due to evidence showed chloroquine is not effective against COVID-19) | ||
| Radical CUREfor MAlaria Among Highly Mobile and Hard-to-reach Populations in the Guyanese Shield [NCT05540470] | 5,000 participants (Anticipated) | Interventional | 2022-09-12 | Not yet recruiting | |||
| A Randomised, Double-blind, Placebo Controlled Trial of Chloroquine for the Prevention of Influenza [NCT01078779] | Phase 2 | 1,516 participants (Actual) | Interventional | 2009-11-30 | Active, not recruiting | ||
| Comparison of the Electrocardiographic Effects in Relation to Pharmacokinetic Profile of Chloroquine and Piperaquine in Healthy Thai Subjects [NCT02192944] | Phase 4 | 16 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| A Multi-center, Open-label, Randomized Trial of Chloroquine, Artemether-Lumefantrine, and Mefloquine-Artesunate for the Treatment of Uncomplicated P. Vivax Malaria in Pregnant Women in Brazil [NCT01107145] | Phase 4 | 16 participants (Actual) | Interventional | 2011-02-28 | Terminated(stopped due to Extremely slow enrollment) | ||
| Safety and Efficacy of Different Regimens of Primaquine on Vivax Malaria Treatment in Glucose 6-phosphate Dehydrogenase Deficient Patients [NCT03529396] | Phase 2 | 106 participants (Actual) | Interventional | 2018-07-20 | Active, not recruiting | ||
| Immunization With Different Doses of Plasmodium Falciparum Sporozoites Under Chloroquine Prophylaxis [NCT01218893] | 30 participants (Actual) | Interventional | 2011-04-30 | Completed | |||
| Developing a Methodology to Assess 8-aminoquinoline Associated Haemolytic Risk in Females Heterozygous for G6PD in Endemic Populations [NCT03337152] | Phase 4 | 54 participants (Actual) | Interventional | 2018-05-07 | Terminated(stopped due to study met study halting rules) | ||
| A Randomised Comparative Study to Assess the Efficacy and Tolerability of Blood Schizonticidal Treatments With Artesunate Amodiaquine Winthrop® / Coarsucam (ASAQ) Versus Chloroquine (CQ) for Uncomplicated Plasmodium Vivax Monoinfection Malaria [NCT01378286] | Phase 3 | 380 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Estimating the Risk of Plasmodium Vivax Relapses in Afghanistan [NCT01178021] | Phase 4 | 593 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| Phase 2/3, Open-Label, Comparative Trial Of Azithromycin Plus Chloroquine Versus Artemether-Lumefantrine For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria In Children In Africa [NCT00677833] | Phase 2/Phase 3 | 361 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Efficacy and Safety of Prednisolone and Chloroquine Add on Therapy in Osteoarthritis of the Knee Treated With Fixed Dose Combination of Glucosamine and Chondroitin Sulfate. [NCT00805519] | Phase 4 | 230 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Phase 1, Open Label, Randomized, Single Dose, Parallel Group Study To Estimate The Relative Bioavailability Of Fixed Combination Tablets Of Azithromycin And Chloroquine Compared To Co-Administered Individual Tablets Of Azithromycin And Chloroquine In He [NCT00844207] | Phase 1 | 40 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| Clinical Trial to Evaluate Intermittent Screening and Treatment and Intermittent Preventive Treatment of Malaria in Asymptomatic Schoolchildren to Decrease P. Falciparum Infection and Transmission: Phase 2 Comparing Drug Regimens [NCT05980156] | Phase 4 | 646 participants (Actual) | Interventional | 2023-02-13 | Completed | ||
| Phase Ib Study of Metformin and Chloroquine in IDH1/2-mutated Patients With Glioma, Intrahepatic Cholangiocarcinoma or Chondrosarcoma [NCT02496741] | Phase 1/Phase 2 | 15 participants (Actual) | Interventional | 2015-11-30 | Completed | ||
| A Phase 1 Study of Chloroquine in Combination With Carboplatin/Gemcitabine in Advanced Solid Tumors [NCT02071537] | Phase 1 | 24 participants (Actual) | Interventional | 2014-05-13 | Completed | ||
| An Adaptive, Multicenter, Randomized, Open-label, Comparative Clinical Study to Assess Efficacy and Safety of Favipiravir in Hospitalized Patients With COVID-19 [NCT04434248] | Phase 2/Phase 3 | 330 participants (Actual) | Interventional | 2020-04-23 | Active, not recruiting | ||
| [NCT02058173] | Phase 4 | 10 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| A Phase II Randomized Controlled Trial for the Addition of Chloroquine, an Autophagy Inhibitor, to Concurrent Chemoradiation for Newly Diagnosed Glioblastoma [NCT02432417] | Phase 2 | 0 participants (Actual) | Interventional | 2023-11-10 | Withdrawn(stopped due to The study was withdrawn due to a lack of funding. The researchers were unable to secure the necessary financial support to continue and complete the trial.) | ||
| Sanaria PfSPZ Challenge With Pyrimethamine or Chloroquine Chemoprophylaxis Vaccination (PfSPZ-CVac Approach): A Randomized Double Blind Placebo Controlled Phase I/II Trial to Determine Safety and Protective Efficacy Against Natural Plasmodium Falciparum I [NCT03952650] | Phase 1/Phase 2 | 252 participants (Actual) | Interventional | 2019-05-23 | Completed | ||
| Chloroquine as an Anti-autophagy Drug in Stage IV Small Cell Lung Cancer (SCLC) Patients: A Phase 1 Trial [NCT00969306] | Phase 1 | 5 participants (Actual) | Interventional | 2013-09-30 | Terminated(stopped due to Poor accrual) | ||
| Genotoxic Stress, Atherosclerosis, and Metabolic Syndrome-AIM 2 [NCT00455325] | Phase 2 | 35 participants (Actual) | Interventional | 2004-09-30 | Completed | ||
| Ethiopia In-vivo Efficacy Study 2009: Evaluating the Efficacy of Artemether-lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Infection and Either Artemether-lumefantrine or Chloroquine for P. Vivax Infection [NCT01052584] | 354 participants (Actual) | Interventional | 2009-10-31 | Completed | |||
| Efficacy and Safety of Chloroquine Diphosphate for the Treatment of Hospitalized Patients With Severe Acute Respiratory Syndrome Secondary to SARS-CoV2: a Phase IIb, Double-blind, Randomized Adaptive Clinical Trial [NCT04323527] | Phase 2 | 278 participants (Actual) | Interventional | 2020-03-23 | Completed | ||
| A Phase III Comparative (Double-blind, Double-dummy) Randomised Multicentre Study to Assess the Safety & Efficacy of Oral Pyronaridine Artesunate (180:60 mg) Versus Chloroquine (155 mg) in Children & Adult Patients With Acute Vivax Malaria [NCT00440999] | Phase 3 | 456 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
| Evaluating the Potential Role of Chloroquine in Preventing Infections During Elimination Campaigns: A Randomized, Single-blind, Placebo-controlled Trial in Asymptomatic Mozambican Adults [NCT02698748] | Phase 2/Phase 3 | 75 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
| A Phase 1 Dose Escalation Trial to Assess the Safety and Efficacy of Infectious (Replication-intact), Cryopreserved Plasmodium Falciparum Sporozoites (PfSPZ Challenge) Administered by Direct Venous Inoculation Under Chloroquine Cover (PfSPZ-CVac) on Varyi [NCT02773979] | Phase 1 | 28 participants (Actual) | Interventional | 2016-09-12 | Completed | ||
| Randomized Clinical Trial of the Efficacy and Safety of Dihydroartimisinine+Papiraquine (Artekin) Compared With First Line Drugs for Treatment of Vivax and Uncomplicated Falciparum Malaria in Afghanistan [NCT00682578] | Phase 3 | 1,086 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| Monitoring Therapeutic Efficacy of Chloroquine Plus Primaquine in the Treatment of Uncomplicated Plasmodium Vivax Based on Clinical, Parasitologic and Hematologic Parameters in Shecha Health Center: Open Label Clinical Trial [NCT06044805] | Phase 4 | 100 participants (Actual) | Interventional | 2022-12-19 | Completed | ||
| Safety, Tolerability, Immunogenicity and Protective Efficacy Against Naturally-Transmitted Malaria in Eastern Indonesia of Two Plasmodium Falciparum Sporozoite Vaccines, Sanaria® PfSPZ Vaccine and Sanaria® PfSPZ-CVac: A Randomized, Double-Blind, Placebo-C [NCT03503058] | Phase 2 | 372 participants (Anticipated) | Interventional | 2022-05-07 | Recruiting | ||
| A Randomized, Pilot Study of the Anti-Viral and Anti-Inflammatory Effects of Chloroquine in Early HIV Infection [NCT00308620] | Phase 2/Phase 3 | 13 participants (Actual) | Interventional | 2006-03-31 | Terminated(stopped due to Insufficient financial support; lack of efficacy for primary endpoint) | ||
| Intermittent Preventive Treatment With Sulfadoxine-Pyrimethamine Versus Weekly Chloroquine Prophylaxis During Pregnancy in Solomon Islands: a Randomized Controlled Trial [NCT00964691] | Phase 4 | 2,504 participants (Anticipated) | Interventional | 2009-08-31 | Terminated(stopped due to Low prevalence of malaria, high prevalence of reported allergy to sulphur drugs, high proportion of women not meeting the inclusion criterea.) | ||
| Clinical Trial of Extended-dose Chloroquine Versus Standard Chloroquine Treatment for Resistant Falciparum Malaria Among Afghan Refugees in NWFP Pakistan [NCT01019408] | Phase 4 | 163 participants (Actual) | Interventional | 1993-11-30 | Completed | ||
| Prevention of Intrauterine Growth Retardation in Hounde District, Burkina Faso: the Malaria Component [NCT00680732] | Phase 4 | 1,370 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
| A Phase II, Double Blind, Randomized, Exploratory Study of Chloroquine for Reducing HIV-Associated Immune Activation [NCT00819390] | Phase 2 | 70 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Pilot Human Study of Tinidazole Efficacy For Radical Cure Of Plasmodium Vivax [NCT00811096] | Phase 2 | 20 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
| Evaluating the Efficacy of Chloroquine for the Treatment of Plasmodium Vivax Infections in Central Vietnam [NCT02610686] | Phase 4 | 100 participants (Anticipated) | Interventional | 2015-03-31 | Recruiting | ||
| Efficacy of Chloroquine (CQ) Alone Compared to Concomitant CQ and Primaquine (PQ) for the Treatment of Uncomplicated Plasmodium Vivax Infection [NCT02691910] | Phase 2/Phase 3 | 204 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| A Phase 3, Open Label, Randomized, Comparative Study To Evaluate Azithromycin Plus Chloroquine And Sulfadoxine Plus Pyrimethamine Combinations For Intermittent Preventive Treatment Of Falciparum Malaria Infection In Pregnant Women In Africa [NCT01103063] | Phase 3 | 2,891 participants (Actual) | Interventional | 2010-10-31 | Terminated(stopped due to See termination reason in detailed description.) | ||
| Prophylaxis With Chloroquine in Health Personnel Exposed to Infection With Coronavirus Disease 2019 (COVID-19) [NCT04627467] | Phase 2 | 3,217 participants (Actual) | Interventional | 2020-03-28 | Completed | ||
| The Effect of Chloroquine in the Treatment of Patients With Dengue [NCT00849602] | Phase 1/Phase 2 | 132 participants (Anticipated) | Interventional | 2008-02-29 | Active, not recruiting | ||
| A Study to Assess Safety of Current Standard Malaria Treatment and an Assessment of Glucose-6-dehydrogenase Status in South-east Bangladesh [NCT02389374] | Phase 4 | 181 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| Pseudo-randomised, Double-blinded Placebo-controlled Trial of Chloroquine or Sulphadoxine-pyrimethamine Alone or in Combination With Primaquine or Artesunate for the Treatment of Uncomplicated Falciparum Malaria in Pakistan [NCT00959517] | Phase 2 | 588 participants (Actual) | Interventional | 2001-07-31 | Completed | ||
| A Phase 2, Open Label, Non-Comparative Trial Of Azithromycin 2000 mg Plus Chloroquine 600 Mg Base Daily For Three Days For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria [NCT00282919] | Phase 2 | 110 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| IMPact of Inflammatory Arthritis on COVID-19 sTudy of the RAPPORT-ONTRAAC and FORCAST Rheumatic Disease Registries [NCT04347798] | 773 participants (Actual) | Observational [Patient Registry] | 2020-11-01 | Completed | |||
| To Evaluate the Efficacy of Chloroquine and SP for Acute Uncomplicated P. Falciparum and the Efficacy of Chloroquine for Acute Uncomplicated P. Vivax in the Timika Region of Papua, Indonesia. [NCT00157859] | 150 participants | Interventional | 2004-04-30 | Completed | |||
| A Randomised Controlled Trial to Assess the Antimalarial Drug Susceptibility and Molecular Characterization of Plasmodium Vivax Isolates in Vietnam [NCT01887821] | Phase 4 | 330 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
| Chloroquine and Sulfadoxine-Pyrimethamine Efficacy for the Treatment of Uncomplicated Falciparum Malaria in Blantyre, Malawi [NCT00125489] | Phase 4 | 210 participants | Interventional | 2005-05-31 | Completed | ||
| DOUBLE-BLIND RANDOMIZED CLINICAL TRIAL WITH CHLOROQUINE VERSUS PLACEBO FOR MAINTENANCE OF REMISSION OF AUTOIMMUNE HEPATITIS [NCT01980745] | Phase 4 | 61 participants (Actual) | Interventional | 2002-02-28 | Completed | ||
| Artemether-lumefantrine vs Chloroquine in Patients With Acute Uncomplicated P. Knowlesi Malaria: a Randomized Open Label Trial in Sabah, Malaysia (CAN KNOW Trial) [NCT02001012] | Phase 3 | 123 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Chloroquine as a Modulator of T Cell Immune Activation to Improve CD4 Recovery in HIV-infected Participants Receiving Antiretroviral Therapy: A Proof-of-concept Study [NCT02004314] | 19 participants (Actual) | Interventional | 2009-10-31 | Completed | |||
| Chloroquine as Adjuvant to the Treatment of Glioblastoma Multiforme, A Randomized Trial [NCT00224978] | Phase 3 | 0 participants | Interventional | 2005-01-31 | Completed | ||
| Randomised Parallel Open Label Comparison Between 7 and 14 Day Primaquine Combined With 3-day Dihydroartemisinin-piperaquine or 3-day Chloroquine Regimens for Radical Cure of Plasmodium Vivax [NCT01640574] | Phase 3 | 680 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| A Multi Center Randomized Open Label Trial on the Safety and Efficacy of Chloroquine for the Treatment of Hospitalized Adults With Laboratory Confirmed SARS-CoV-2 Infection in Vietnam [NCT04328493] | Phase 2 | 10 participants (Actual) | Interventional | 2020-04-07 | Completed | ||
| An Open Label, Non-comparative Study To Evaluate Parasitological Clearance Rates And Pharmacokinetics Of Azithromycin And Chloroquine Following Administration Of A Fixed Dose Combination Of Azithromycin And Chloroquine (Azcq) In Asymptomatic Pregnant Wome [NCT01103713] | Phase 3 | 168 participants (Actual) | Interventional | 2011-03-31 | Terminated(stopped due to See termination reason in detailed description.) | ||
| Safety, Tolerability, and Pharmacokinetic Study of Concomitant Chloroquine and Tafenoquine in Healthy Volunteers [NCT00871156] | Phase 1 | 68 participants (Actual) | Interventional | 2009-03-24 | Completed | ||
| New Approaches to Improve Coverage and Compliance of Antimalarial Treatment for Pregnant Women in Rural Africa. [NCT00730366] | Phase 3 | 2,766 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
| Clinical Trial of Favipiravir Tablets Combine With Chloroquine Phosphate in the Treatment of Novel Coronavirus Pneumonia [NCT04319900] | Phase 2/Phase 3 | 150 participants (Anticipated) | Interventional | 2020-03-05 | Recruiting | ||
| G6PD Assessment Before Primaquine for Radical Treatment of Vivax Malaria [NCT02876549] | Phase 4 | 1,000 participants (Actual) | Interventional | 2016-09-01 | Completed | ||
| Immunization With Plasmodium Falciparum Sporozoites Under Chloroquine Versus Mefloquine Prophylaxis [NCT01422954] | 20 participants (Actual) | Interventional | 2012-01-31 | Completed | |||
| Chloroquine for Patients With Symptomatic Persistent Atrial Fibrillation: A Prospective Pilot Study [NCT02932007] | Phase 2 | 40 participants (Anticipated) | Interventional | 2017-03-28 | Recruiting | ||
| Etude de l'Activite (Efficacite et Tolerance) de l'Association de la Chloroquine Avec la Dehydroepiandrosterone-Sulfate (Dheas) Dans le Traitement de l'Acces Palustre Simple A Plasmodium Falciparum [NCT00442403] | Phase 3 | 200 participants | Interventional | 2002-04-30 | Suspended(stopped due to At the end of the year 2002, Cameroon switched from chloroquine to amodiaquine as first-line therapy for of uncomplicated malaria.) | ||
| Clinical Trial to Evaluate Intermittent Screening and Treatment and Intermittent Preventive Treatment of Malaria in Asymptomatic Schoolchildren to Decrease P. Falciparum Infection and Transmission [NCT05244954] | Phase 4 | 746 participants (Actual) | Interventional | 2022-02-01 | Completed | ||
| A Randomized, Active-control, Double-blind, Double-dummy Study to Evaluate the Efficacy and Safety of Tafenoquine for the Treatment of Plasmodium Vivax in Adults [NCT01290601] | Phase 2 | 70 participants (Actual) | Interventional | 2003-09-15 | Terminated(stopped due to Failure to meet pre-specified endpoint for the day 28 cure rate) | ||
| Does Artemisinin Combination Treatment Reduce the Radical Curative Efficacy of High Dose Tafenoquine for Plasmodium Vivax Malaria? [NCT05788094] | Phase 4 | 388 participants (Anticipated) | Interventional | 2023-06-26 | Recruiting | ||
| Preventing Invasive Breast Neoplasia With Chloroquine (PINC) Trial [NCT01023477] | Phase 1/Phase 2 | 12 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
| Comprehensive in Vitro Proarrhythmia Assay (CiPA) Clinical Phase 1 ECG Biomarker Validation Study (CiPA Phase 1 ECG Biomarker Study) [NCT03070470] | Phase 1 | 60 participants (Actual) | Interventional | 2017-03-14 | Completed | ||
| A Phase Ii/Iii, Randomized, Double Blind, Comparative Trial Of Azithromycin Plus Chloroquine Versus Atovaquone-Proguanil For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria In South America [NCT00084227] | Phase 2/Phase 3 | 244 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
| Development of a Ready-to-use Nutraceutical Food for Patients With Sickle Cell Disease (SCD): Testing of Vascular Support Components [NCT01718054] | Phase 2/Phase 3 | 120 participants (Anticipated) | Interventional | 2012-08-31 | Active, not recruiting | ||
| Characterization of Novel Molecular Tools for the Epidemiological Surveillance of Antimalarial Drug Resistance in Mali [NCT00127998] | 1,011 participants | Interventional | 2005-07-31 | Completed | |||
| Chloroquine and Coartem for Treatment of Symptomatic Children With Plasmodium Falciparum in Guinea Bissau. [NCT00426439] | Phase 4 | 300 participants (Anticipated) | Interventional | 2006-12-31 | Completed | ||
| A Randomised Double Blind Clinical Trial of Amodiaquine (AQ) and Sulphadoxine-pyrimethamine (SP) Used Singly and in Combination (AQ+SP) Compared With Chloroquine (CQ) in the Treatment of Falciparum Malaria Infection in Pregnancy [NCT00131703] | Phase 3 | 900 participants | Interventional | 2003-03-31 | Completed | ||
| Chloroquine and Amodiaquine for Treatment of Symptomatic Children With Plasmodium Malaria in Guinea-Bissau [NCT00137514] | Phase 4 | 720 participants | Interventional | 2001-03-31 | Completed | ||
| A Randomised Non-Inferiority Trial of Sulfadoxine-Pyrimethamine Plus Artesunate Compared to Chloroquine for the Treatment of Vivax Malaria in Eastern Afghanistan. [NCT00486694] | Phase 2 | 190 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
| Relationships Between the Use of Antimalarial Drugs in Pregnancy and Plasmodium Falciparum Resistance [NCT00140517] | 700 participants | Interventional | 2002-10-31 | Completed | |||
| Prednisone Plus Chloroquine Versus Chloroquine for the Treatment of Hyper-reactive Malarial Splenomegaly in Papua New Guinea: a Randomized Open-label Trial [NCT01785979] | Phase 3 | 0 participants (Actual) | Interventional | 2016-01-31 | Withdrawn(stopped due to Lack of funding) | ||
| Clinical Study Evaluating the Efficacy of Chloroquine or Hydroxychloroquine in COVID-19 Treatment [NCT04353336] | Phase 2/Phase 3 | 194 participants (Actual) | Interventional | 2020-03-23 | Completed | ||
| Phase IIb Study to Evaluate the Efficacy and Safety of Chloroquine Diphosphate in the Treatment of Patients With Comorbidities, Without Severe Acute Respiratory Syndrome, Under the New Coronavirus (SARS-CoV2): a Double-blind, Randomized, Placebo-controlle [NCT04342650] | Phase 2 | 152 participants (Actual) | Interventional | 2020-04-08 | Completed | ||
| The Efficacy and Safety of Carrimycin Treatment in Patients With Novel Coronavirus Infectious Disease (COVID-19) : A Multicenter, Randomized, Open-controlled Study [NCT04286503] | Phase 4 | 520 participants (Anticipated) | Interventional | 2020-02-23 | Not yet recruiting | ||
| A Phase 2a Open Label Study of the Safety and Efficacy of a Single Dose of Weekly Chloroquine (CQ) and Azithromycin (AZ) Administered in Combination for Malaria Prophylaxis in Healthy Adults Challenged With 7G8 Chloroquine-Resistant Plasmodium Falciparum [NCT03278808] | Phase 2 | 0 participants (Actual) | Interventional | 2018-09-17 | Withdrawn(stopped due to The IND has been withdrawn from FDA) | ||
| Effect of Antimalarial Drugs on the Immune Response to Rabies Vaccine for Post-exposure Prophylaxis. A Randomized, Open Label, Trial in Healthy US Adults Age 18-60 Years [NCT02564471] | Phase 4 | 103 participants (Actual) | Interventional | 2016-11-11 | Completed | ||
| A Phase I, Randomized Malaria Challenge Study of Intradermally-Administered Infectious (Replication-intact), Cryopreserved Plasmodium Falciparum Sporozoites (PfSPZ Challenge) in Malaria-Naïve Adults [NCT01546389] | Phase 1 | 30 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
| The Population Pharmacokinetics of Chloroquine for the Treatment of Uncomplicated P.Vivax Malaria in Pre- and Post-partum Women. [NCT01546961] | 49 participants (Actual) | Interventional | 2011-06-30 | Completed | |||
| Randomized Trial of the Effectiveness of Amodiaquine-Artesunate, Amodiaquine-Sulfadoxine-Pyrimethamine, and Chloroquine-Sulfadoxine-Pyrimethamine, for Treatment of Uncomplicated Malaria in Gambian Children [NCT00118807] | Phase 3 | 1,800 participants | Interventional | 2003-08-31 | Completed | ||
| A Phase II/III, Randomized, Double-Blind, Comparative Trial Of Azithromycin Plus Chloroquine Versus Mefloquine For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria In Africa [NCT00082576] | Phase 2/Phase 3 | 238 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
| CuraChik : Double Blind Placebo-controlled Randomized Trial : Efficacy and Safety of Chloroquine as Therapeutic Treatment of Chikungunya Disease. [NCT00391313] | Phase 3 | 0 participants | Interventional | 2006-05-31 | Terminated(stopped due to Terminated Chikungunya diseases has regressed and no more patients was suffering) | ||
| A Study to Evaluate the Safety and Immunogenicity of a Booster Dose of GSK Biologicals' HIV Candidate Vaccine (732461) After Administration of Chloroquine in Healthy Adults. [NCT00972725] | Phase 2 | 28 participants (Actual) | Interventional | 2009-12-01 | Completed | ||
| A Phase II/III, Randomized, Comparative Trial of Azithromycin Plus Chloroquine Versus Sulfadoxine-Pyrimethamine Plus Chloroquine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in India [NCT00074841] | Phase 2/Phase 3 | 230 participants (Actual) | Interventional | 2003-09-30 | Completed | ||
| Influence of HIV Infection on the Effectiveness of Malaria Prevention During Pregnancy, With Emphasis on the Effect of Chloroquine on HIV Viral Load Among Pregnant Women in Uganda [NCT00132535] | 2,548 participants | Interventional | 2003-08-31 | Completed | |||
| A Phase II, Randomized, Comparative Trial Of Azithromycin In Combination With Chloroquine Versus Chloroquine In The Eradication Of Asymptomatic Plasmodium Falciparum Infection In Semi-Immune Adults [NCT00082563] | Phase 2 | 14 participants (Actual) | Interventional | 2004-08-31 | Terminated | ||
| Studies on Adding Artesunate to Existing Antimalarial Therapies With Chloroquine, Amodiaquine & Sulphadoxine-pyrimethamine in Pakistan [NCT00158548] | Phase 3 | 650 participants (Actual) | Interventional | 2001-06-30 | Completed | ||
| A Study of the Impact of Insecticide-treated Curtains on the Prevalence of Antimalarial Drug Resistance in Children With Uncomplicated Malaria in Burkina Faso [NCT00169078] | 1,035 participants | Interventional | 2002-07-31 | Completed | |||
| A Phase 2/3, Randomized, Comparative, Double Blind Trial Of Azithromycin Plus Chloroquine Versus Sulfadoxine-Pyrimethamine Plus Chloroquine For The Treatment Of Uncomplicated, Symptomatic Falciparum Malaria In Southeast Asia [NCT00084240] | Phase 2/Phase 3 | 32 participants (Actual) | Interventional | 2004-03-31 | Terminated(stopped due to See Detailed Description) | ||
| Chloroquine as a Therapeutic Option for Mild Post Malaria Anaemia [NCT00473837] | 96 participants (Actual) | Interventional | 2007-07-31 | Completed | |||
| Safety, Tolerability, Immunogenicity and Protective Efficacy Against Naturally-Transmitted Malaria of Infectious, Cryopreserved Plasmodium Falciparum Sporozoites (PfSPZ Challenge) Administered by Direct Venous Inoculation Under Chloroquine Chemoprophylaxi [NCT02996695] | Phase 1 | 62 participants (Actual) | Interventional | 2017-04-06 | Completed | ||
| Preventing Malaria in School Children to Protect the Whole Community in Rural Blantyre District, Malawi [NCT06083688] | Phase 4 | 1,000 participants (Anticipated) | Interventional | 2024-10-31 | Not yet recruiting | ||
| Efficacy of Chloroquine + Sulfadoxine Pyrimethamine Versus Artemether + Lumefantrine for the Treatment of Uncomplicated Plasmodium Falciparum Malaria in the Philippines [NCT00229775] | 560 participants (Actual) | Interventional | 2003-07-31 | Completed | |||
| Ethiopia Antimalarial in Vivo Efficacy Study 2012: Evaluating the Efficacy of Artemether-lumefantrine Alone Compared to Artemether-lumefantrine Plus Primaquine and Chloroquine Alone Compared to Chloroquine Plus Primaquine for Plasmodium Vivax Infection [NCT01680406] | Phase 4 | 398 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| Community Acceptability and Cost-effectiveness of Two Drug Distribution Methods for Home Based Management of Fevr in Kayunga District, Uganda [NCT00259142] | 1,314 participants (Anticipated) | Interventional | 2005-11-30 | Terminated(stopped due to Study never started) | |||
| Prevention of P. Vivax Malaria During Pregnancy: Effects on Mother and Child Health in Santa Cruz, Bolivia. Open, Multicentric, Randomized Clinical Trial, Comparing Prophylaxis Once a Week to Malaria Attack Treatment, Both by Chloroquine. [NCT00290420] | Phase 4 | 0 participants (Actual) | Interventional | 2006-03-31 | Withdrawn(stopped due to important delays and malaria season missed, due to political changes) | ||
| Infection-Treatment-Vaccination for Plasmodium Falciparum [NCT01500980] | Phase 1 | 36 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
| Multicenter, Randomized, Open-label, Non-commercial, Investigator-initiated Study to Evaluate the Efficacy and Safety of Chloroquine Phosphate in Combination With Telemedicine Care in the Risk Reduction of COVID-19 Related Hospitalization or Death, in Amb [NCT04331600] | Phase 4 | 16 participants (Actual) | Interventional | 2020-04-16 | Completed | ||
| An Open Label Randomized Comparison of Two Antimalarial Drugs Regimens in Patient With Plasmodium Vivax Malaria in Thailand [NCT01662700] | Phase 4 | 120 participants (Anticipated) | Interventional | 2012-10-31 | Recruiting | ||
| Randomized Trial of ACEIs in Treatment of COVID-19 [NCT04345406] | Phase 3 | 60 participants (Anticipated) | Interventional | 2020-04-15 | Not yet recruiting | ||
| Artesunate-mefloquine vs Chloroquine in Patients With Acute Uncomplicated P. Knowlesi and P. Vivax Malaria: a Randomized Open Label Trial in Sabah, Malaysia [NCT01708876] | Phase 3 | 250 participants (Anticipated) | Interventional | 2012-10-31 | Completed | ||
| A Randomized, Controlled Clinical Trial of Chloroquine as Chemoprophylaxis Versus Intermittent Preventive Therapy to Prevent Malaria in Pregnancy in Malawi [NCT01443130] | Phase 3 | 900 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| Parasitic Clearance and Recurrence Rates Among Patients With Vivax Malaria on Chloroquine and Primaquine Therapy [NCT01716260] | 24 participants (Actual) | Observational | 2013-01-31 | Completed | |||
| Gemcitabine Combined With Chloroquine in Patients With Metastatic or Unresectable Pancreatic Cancer. A Dose Finding Single Center Phase I Study [NCT01777477] | Phase 1 | 9 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
| PARASITIC CLEARANCE AND RECURRENCE RATES AMONG PATIENTS WITH VIVAX MALARIA ON CHLOROQUINE AND PRIMAQUINE THERAPY [NCT01784315] | 50 participants (Anticipated) | Observational [Patient Registry] | 2013-03-31 | Recruiting | |||
| Pharmacokinetic Study of Multi-dose Chloroquine [NCT01814423] | Phase 4 | 30 participants (Actual) | Interventional | 2013-04-30 | Completed | ||
| Randomized, Open-label Controlled Trial of Daily Trimethoprim-sulfamethoxazole or Weekly Chloroquine Among Adults on Anti-retroviral Therapy in Malawi [NCT01650558] | 1,499 participants (Actual) | Interventional | 2012-11-30 | Completed | |||
| A Multicenter, Randomized, Active Controlled, Open Label, Platform Trial on the Efficacy and Safety of Experimental Therapeutics for Patients With COVID-19 (Caused by Infection With Severe Acute Respiratory Syndrome Coronavirus-2) [NCT04351724] | Phase 2/Phase 3 | 500 participants (Anticipated) | Interventional | 2020-04-16 | Recruiting | ||
| A Phase 3, Randomized, Open-Label, Comparative Trial Of Azithromycin Plus Chloroquine Versus Mefloquine For The Treatment Of Uncomplicated Plasmodium Falciparum Malaria In Africa [NCT00367653] | Phase 3 | 397 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| Hydroxychloroquine for the Management of CVD in CKD [NCT03636152] | Phase 2 | 100 participants (Anticipated) | Interventional | 2018-12-14 | Recruiting | ||
| An Open-label, Phase I Trial With Expansion Cohort of Nab-Paclitaxel + Gemcitabine + Cisplatin + Botensilimab (AGEN1811) + Balsilimab (AGEN2034) + Chloroquine + Celecoxib in Patients With Previously Untreated Metastatic Pancreatic Cancer [NCT06076837] | Phase 1 | 12 participants (Anticipated) | Interventional | 2023-12-31 | Not yet recruiting | ||
| Evaluation of Efficacy of Pharmacotherapy Treatment of COVID- 19 Infection Using Oral Levamisole and Formoterol+Budesonide Inhaler and Comparison of This Treatment Protocol With Standard National Treatment of the Disease [NCT04331470] | Phase 2/Phase 3 | 30 participants (Anticipated) | Interventional | 2020-04-04 | Recruiting | ||
| Treatment of Adults With Newly Diagnosed Glioblastoma With Partial Brain Radiation Therapy Plus Temozolomide and Chloroquine Followed by Tumor Treating Fields Plus Temozolomide and Chloroquine -- A Pilot Study [NCT04397679] | Phase 1 | 10 participants (Anticipated) | Interventional | 2021-08-12 | Recruiting | ||
| Phase II Randomized, Double Blind, Placebo Controlled Study of Whole-brain Irradiation With Concomitant Daily-dose Chloroquine for Brain Metastases. [NCT01894633] | Phase 2 | 73 participants (Actual) | Interventional | 2011-05-31 | Terminated(stopped due to terminated) | ||
| Use and Dosage of Hydroxychloroquine and Chloroquine to Convert Symptomatic RT-PCR Positive Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Coronavirus Infectious Disease 2019 (COVID-19) Patients to RT- PCR-Negative as a Means to Reduce Hospi [NCT04351191] | Phase 4 | 137 participants (Actual) | Interventional | 2020-04-15 | Terminated(stopped due to Poor accrual) | ||
| IDO2 Genetic Status Informs the Neoadjuvant Efficacy of Chloroquine in Brain Metastasis Radiotherapy. [NCT01727531] | 20 participants (Actual) | Interventional | 2008-12-31 | Completed | |||
| Multi-centre Randomised Controlled Trial of Chloroquine/Hydroxychloroquine Versus Standard of Care for Treatment of Mild Covid-19 in HIV-positive Outpatients in South Africa [NCT04360759] | Phase 3 | 0 participants (Actual) | Interventional | 2020-05-01 | Withdrawn(stopped due to Equipoise for hydroxychloquine was lost) | ||
| Chloroquine as an Anti-autophagic Radiosensitizing Drug in Stage I-III Small Cell Lung Cancer (SCLC) Patients: a Phase I Trial. [NCT01575782] | Phase 1 | 5 participants (Actual) | Interventional | 2014-05-31 | Terminated(stopped due to Poor accrual) | ||
| An Open Label, Non-comparative, Multicenter Study to Assess the Pharmacokinetics, Safety and Efficacy of Tafenoquine (SB-252263, WR238605) in the Treatment of Pediatric Subjects With Plasmodium Vivax Malaria [NCT02563496] | Phase 2 | 60 participants (Actual) | Interventional | 2017-02-06 | Completed | ||
| Randomized Controlled Trial of AQ-13, a Candidate Aminoquinoline Antimalarial, in Comparison With Chloroquine [NCT00323375] | Phase 1 | 122 participants (Actual) | Interventional | 1999-08-01 | Completed | ||
| Induction of Remission in RA Patients at Low Disease Activity by Additional Infliximab-therapy [NCT00521924] | Phase 3 | 8 participants (Actual) | Interventional | 2007-06-30 | Terminated(stopped due to Slow Enrollment) | ||
| WU 352: Open-label, Randomized Controlled Trial of Hydroxychloroquine Alone or Hydroxychloroquine Plus Azithromycin or Chloroquine Alone or Chloroquine Plus Azithromycin in the Treatment of SARS CoV-2 Infection [NCT04341727] | Phase 3 | 31 participants (Actual) | Interventional | 2020-04-04 | Terminated(stopped due to DSMB recommended study suspension slow accrual) | ||
| Chloroquine for Mild Symptomatic and Asymptomatic COVID-19 in A Two Staged, Multicenter, Open Label and Randomized Trial [NCT04333628] | Phase 2/Phase 3 | 5 participants (Actual) | Interventional | 2020-06-01 | Terminated(stopped due to Teminated due to changes in treatment guidelines .) | ||
| A Phase I Trial for the Addition of Chloroquine, an Autophagy Inhibitor, to Concurrent Chemoradiation for Newly Diagnosed Glioblastoma [NCT02378532] | Phase 1 | 13 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
| A Longitudinal Study of Chloroquine as Monotherapy or in Combination With Artesunate, Azithromycin or Atovaquone-Proguanil to Treat Malaria in Children in Blantyre, Malawi [NCT00379821] | Phase 3 | 640 participants (Actual) | Interventional | 2007-02-28 | Completed | ||
| Comparison of the Effectiveness of Two Scheme Treatments to Treat Plasmodium Vivax Cases in Patients Living in Communities With Persistence of Transmission in Oaxaca and Chiapas, Mexico [NCT02394197] | Phase 4 | 153 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| Clinical Study Evaluating the Efficacy of Faviprevir in COVID-19 Treatment [NCT04351295] | Phase 2/Phase 3 | 92 participants (Actual) | Interventional | 2020-04-20 | Completed | ||
| A Phase II, Trial of Chloroquine in Combination With VELCADE and Cyclophosphamide in Patients With Relapsed and Refractory Myeloma [NCT01438177] | Phase 2 | 11 participants (Actual) | Interventional | 2011-10-31 | Terminated(stopped due to PI left institution.) | ||
| An Open Label Cluster Randomized Controlled Trial of Chloroquine, Hydroxychloroquine or Only Supportive Care in Patients AdmItted With Moderate to Severe COVID-19 [NCT04362332] | Phase 4 | 25 participants (Actual) | Interventional | 2020-04-14 | Terminated(stopped due to Currently, almost no patients admitted to Dutch hospitals. If any effect of HCQ is to be expected we need more than 1000 inclusions) | ||
| Chloroquine Phosphate Against Infection by the Novel Coronavirus SARS-CoV-2 (COVID-19): The HOPE Open-Label, Non Randomized Clinical Trial [NCT04344951] | Phase 2 | 29 participants (Actual) | Interventional | 2020-04-06 | Terminated(stopped due to No clinical efficacy against SARS-CoV-2 recorded) | ||
| Multicenter, Open Label, Phase IIIb Study to Evaluate the Safety and Tolerability of Subcutaneous Tocilizumab as Monotherapy and/or in Combination With Methotrexate or Other Non-Biologic Disease-Modifying Antirheumatic Drugs in Patients With Rheumatoid Ar [NCT01941095] | Phase 3 | 100 participants (Actual) | Interventional | 2013-11-20 | Completed | ||
| Does Zinc Supplementation Enhance the Clinical Efficacy of Chloroquine/Hydroxychloroquine in Treatment of COVID-19? [NCT04447534] | Phase 3 | 191 participants (Actual) | Interventional | 2020-06-23 | Completed | ||
| An Investigator-Initiated, Phase II, Randomized, Withdrawal Study of Mycophenolate Mofetil (MMF) in Patients With Stable, Quiescent Systemic Lupus Erythematosus (SLE) [NCT01946880] | Phase 2 | 102 participants (Actual) | Interventional | 2013-11-20 | Terminated(stopped due to Slow enrollment.) | ||
| Efficacy of Chloroquine Phosphate Prophylactic Use in First-line Health Personnel Exposed to COVID-19 Patients [NCT04443270] | Phase 1 | 200 participants (Anticipated) | Interventional | 2020-07-27 | Not yet recruiting | ||
| Sanaria PfSPZ Challenge With Pyrimethamine Chemoprophylaxis (PfSPZ-CVac Approach): Phase 1 Trial to Determine Safety and Protective Efficacy of Sanaria PfSPZ Challenge With Concurrent Pyrimethamine Treatment That Inhibits Development of Asexual Blood Stag [NCT02511054] | Phase 1 | 57 participants (Actual) | Interventional | 2015-07-21 | Completed | ||
| Use and Dosage of Hydroxychloroquine and Chloroquine to Convert Real Time Polymerase Chain Reaction (RT-PCR) Positive Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Coronavirus Infectious Disease 2019 (COVID-19) Patients to RT- PCR-Negative [NCT04346667] | Phase 4 | 125 participants (Actual) | Interventional | 2020-04-14 | Terminated(stopped due to Poor accrual.) | ||
| Phase II Clinical Study of Hydroxychloroquine Combined With Gemcitabine in the Treatment of Advanced Non-small Cell Lung Cancer [NCT05647330] | Phase 2 | 55 participants (Anticipated) | Interventional | 2022-12-15 | Not yet recruiting | ||
| A Randomized, Double-Blind, Double Dummy, Comparative, Multicenter Study to Assess the Incidence of Hemolysis, Safety, and Efficacy of Tafenoquine (SB-252263, WR238605) Versus Primaquine in the Treatment of Subjects With Plasmodium Vivax Malaria [NCT02216123] | Phase 3 | 251 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| A Multi-centre, Double-blind, Randomised, Parallel-group, Active Controlled Study to Evaluate the Efficacy, Safety and Tolerability of Tafenoquine (SB-252263, WR238605) in Subjects With Plasmodium Vivax Malaria. [NCT01376167] | Phase 2 | 851 participants (Actual) | Interventional | 2014-04-24 | Completed | ||
| Efficacy of Chloroquine and Primaquine for the Treatment of Plasmodium Vivax Malaria in Cruzeiro do Sul, Acre, Brazil [NCT02043652] | 119 participants (Actual) | Interventional | 2014-02-28 | Completed | |||
| Possible Role of Chloroquine in Conjunction to Prednisone to Induce a Complete Remission in the Treatment of Autoimmune Hepatitis: a Randomized Trial [NCT02463331] | Phase 4 | 57 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
| Multicentric Pragmatic Randomized Controled Trial to Evaluate the Efficacy Chloroquine or Hydroxychloroquine for Five Days in Treating Pneumonia Caused by SARS-Cov-2 - COVID-19 [NCT04420247] | Phase 3 | 142 participants (Actual) | Interventional | 2020-04-16 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||