Melarsoprol is an arsenic-containing drug used to treat the late-stage, neurological form of African trypanosomiasis (sleeping sickness) caused by Trypanosoma brucei gambiense. It is synthesized through a complex multi-step process involving the reaction of 4-amino-phenylarsonic acid with 3-hydroxypropanal in the presence of hydrochloric acid and sodium chloride. Melarsoprol exhibits trypanocidal activity by inhibiting the enzyme trypanothione reductase, which is essential for the survival of Trypanosoma brucei. The drug has been effective in treating late-stage sleeping sickness, but it can cause severe side effects, including encephalopathy, coma, and death. Due to its toxicity, melarsoprol is typically reserved for cases where other treatments have failed. The high toxicity of melarsoprol has led to research efforts aimed at developing safer and more effective trypanocidal drugs. Research on melarsoprol focuses on understanding its mechanism of action, developing safer analogs, and exploring potential alternative treatments for African trypanosomiasis.'
Melarsoprol: Arsenical used in trypanosomiases. It may cause fatal encephalopathy and other undesirable side effects.
ID Source | ID |
---|---|
PubMed CID | 10311 |
CHEMBL ID | 166 |
CHEBI ID | 6729 |
SCHEMBL ID | 61707 |
MeSH ID | M0013318 |
Synonym |
---|
chebi:6729 , |
CHEMBL166 |
melarsoprolum |
unii-zf3786q2e8 |
zf3786q2e8 , |
1,3,2-dithiarsolane-4-methanol, 2-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)- |
2-(p-(4,6-diamino-s-triazin-2-ylamino)phenyl)-1,3,2-dithiarsolane-4-methanol |
melarsoprol [inn:ban:dcf] |
einecs 207-793-4 |
melarsoprolum [inn-latin] |
rp 3854 |
2-[4-{(4,6-diamino-1,3,5-triazin-2-yl)amino}phenyl]-1,3,2-dithiarsolan-e-4-methanol |
[2-[4-[(4,6-diamino-1,3,5-triazin-2-yl)amino]phenyl]-1,3,2-dithiarsolan-4-yl]methanol |
494-79-1 |
melarsoprol |
C08001 |
D00832 |
melarsoprol (inn) |
mel b (tn) |
arsobal |
specia |
rp-3854 |
mel b |
SCHEMBL61707 |
DB12864 |
(2-{4-[(4,6-diamino-1,3,5-triazin-2-yl)amino]phenyl}-1,3,2-dithiarsolan-4-yl)methanol |
DTXSID90862033 |
Q419753 |
(2-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)-1,3,2-dithiarsolan-4-yl)methanol |
melarsoprol [mart.] |
melarsoprol [mi] |
melarsoprol [who-dd] |
melarsoprol [inn] |
AKOS040752991 |
Melarsoprol is an arsenic-containing drug, and has been applied in the treatment of human African trypanosomiasis at the late stage.
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"Melarsoprol (MEL) is an arsenic-containing drug, and has been applied in the treatment of human African trypanosomiasis at the late stage." | ( Delivery of melarsoprol using folate-targeted PEGylated cyclodextrin-based nanoparticles for hepatocellular carcinoma. Guo, J; Han, S; Li, Y; Li, YN; O'Driscoll, CM; Shi, X; Shi, Y; Sun, D; Wang, L; Yang, L; Zou, Y, 2023) | 2.01 |
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"Melarsoprol has been used for many decades." | ( Cost-effectiveness analysis of alternative treatments of African gambiense trypanosomiasis in Uganda. Carrín, G; Cattand, PD; Evans, D; Kuzoe, FA; Politi, C, ) | 0.85 |
Melarsoprol treatment was feared for its side effects. Treatment with melarsopol in two cases and eflornithine in one case led to complete recovery.
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"Melarsoprol treatment was undertaken." | ( Polysomnography as a diagnosis and post-treatment follow-up tool in human African trypanosomiasis: a case study in an infant. Bandzouzi, B; Bouteille, B; Buguet, A; Cespuglio, R; Mpandzou, G; Ngampo, S; Vincendeau, P, 2011) | 1.09 |
"Melarsoprol treatment was feared for its side effects." | ( Drug toxicity and cost as barriers to community participation in HAT control in the Democratic Republic of Congo. Boelaert, M; Kande Betu Ku Mesu, V; Lefèvre, P; Lubanza, S; Lutumba, P; Robays, J; Van der Stuyft, P, 2007) | 1.06 |
"Treatment with melarsoprol in two cases and eflornithine in one case led to complete recovery." | ( [Sleeping sickness in children at Bobo-Dioulasso Hospital Center: apropos of 3 cases]. Bonkoungou, P; Millogo, A; Nacro, B; Sanou, M; Tall, F; Traoré, H; Traoré, S, 1999) | 0.64 |
A large number of patients refractory to melarsoprol treatment was recently reported from northern Uganda and northern Angola. We investigated in northern Angola whether interpatient pharmacokinetic differences influence the outcome of melarsOProl treatment. Mean terminal elimination half-life of melARSoprol was about 35 h.
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" The 'terminal' elimination rate constant could be determined in six patients and subsequent kinetic calculations showed a three to fourfold variation in plasma clearance and 'terminal' half-life (median 1126 (range 553-2036) ml min-1 and 265 (107-446) h, respectively)." | ( Pharmacokinetics and adverse reactions after a single dose of pentamidine in patients with Trypanosoma gambiense sleeping sickness. Bronner, U; Doua, F; Ericsson, O; Gustafsson, LL; Miézan, T; Rais, M; Rombo, L, 1995) | 0.29 |
" The results of this study are compared with recent pharmacokinetic data from human patients, and discussed in the context of the problem of relapses and reactive encephalopathy occurring after treatment of sleeping sickness." | ( Pharmacokinetics of melarsoprol in uninfected vervet monkeys. Auma, JE; Brun, R; Burri, C; Burudi, EM; Onyango, JD, 1994) | 0.61 |
" Mean terminal elimination half-life of melarsoprol was about 35 h, volume of distribution was about 100 l and total clearance was about 50 ml/min." | ( Pharmacokinetic properties of the trypanocidal drug melarsoprol. Baltz, T; Brun, R; Burri, C; Doua, F; Giroud, C; Welker, HA, ) | 0.65 |
" As a large number of patients refractory to melarsoprol treatment was recently reported from northern Uganda and northern Angola, we investigated in northern Angola whether interpatient pharmacokinetic differences influence the outcome of melarsoprol treatment." | ( Pharmacokinetic investigations in patients from northern Angola refractory to melarsoprol treatment. Burri, C; Keiser, J, 2001) | 0.8 |
megazol gel, when used in combination with melarsoprol (3.5%) is capable of curing experimental murine CNS-trypanosomiasis with a one-day treatment.
melarsoprol-cyclodextrin complexes are developed to improve tolerability and the bioavailability of the drug. These complexes increase the oral bioavailability, making them effective orally and both curative and nontoxic in doses that are equivalent to those of intravenous melarso.
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" The aim of our work was to develop melarsoprol-cyclodextrin complexes in order to improve the tolerability and the bioavailability of melarsoprol." | ( Melarsoprol-cyclodextrins inclusion complexes. Astier, A; Fries, I; Gibaud, S; Mutzenhardt, P; Zirar, SB, 2005) | 2.05 |
" These complexes increase the oral bioavailability of melarsoprol making them effective orally and both curative and nontoxic in doses that are equivalent to those of intravenous melarsoprol." | ( An alternative form of melarsoprol in sleeping sickness. Kennedy, PG, 2012) | 0.94 |
" The 7-nitroquinoxalin-2-one and 5-nitroindazole scaffold derivatives 58 and 35, respectively, are particularly interesting because of their established oral bioavailability in mice." | ( Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies. Arán, VJ; Dardonville, C; Kaiser, M, 2012) | 0.38 |
" Our compound optimization that has led to synthesis of several potent 4-anilinoquinazolines, including NEU617, 23a, a highly potent, orally bioavailable inhibitor of trypanosome replication." | ( Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis. Behera, R; Edwards, P; Guyett, PJ; Karver, CE; Mensa-Wilmot, K; Patel, G; Pollastri, MP; Roncal, NE; Sullenberger, C, 2013) | 0.39 |
The higher frequency of relapses in 1994 to 1997 was associated with an incremental dosage regimen of melarsoprol. The introduction of the combination of nifurtimox and eflornithine (NECT) has accelerated the shift from melar's to the best treatment available.
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" Optimum dosage and duration of therapy, modes of administration and potential for large scale use are discussed." | ( Advances in sleeping sickness therapy. Van Nieuwenhove, S, 1992) | 0.28 |
" A (donor) mouse, infected for 28 days, is dosed with a drug, or combination of drugs, and samples of blood, cerebral cortex, choroid plexus and lining of ventricle are injected into clean (recipient) mice." | ( Screening compounds for sleeping sickness therapy without relapse. Ormerod, WE; Raseroka, BH, 1988) | 0.27 |
" Two other goats appeared to be cured with this dosage of suramin but later developed abnormal central nervous system (CNS) signs and parasitaemia." | ( Experimental infection of goats with Trypanosoma brucei ssp. and effects of treatment with suramin and Mel-B. Chumo, DA; Muriithi, RM; Mwangi, J; Reardon, MJ; Towett, S; Wellde, BT, 1989) | 0.28 |
" The prolonged elimination of pentamidine seems inconsistent with the present recommended dosage regimen of pentamidine for treatment of trypanosomiasis of 7 to 10 parenteral doses given once daily or every second day." | ( Pharmacokinetics and adverse reactions after a single dose of pentamidine in patients with Trypanosoma gambiense sleeping sickness. Bronner, U; Doua, F; Ericsson, O; Gustafsson, LL; Miézan, T; Rais, M; Rombo, L, 1995) | 0.29 |
" The remaining animal in this group, that displayed persistent antigenaemia, had been treated with a sub-curative drug dosage level." | ( Trypanosoma brucei rhodesiense: use of an antigen detection enzyme immunoassay for evaluation of response to chemotherapy in infected vervet monkeys (Cercopithecus aethiops). Gichuki, CW; Nantulya, VM; Sayer, PD, 1994) | 0.29 |
" Dose-response experiments with melarsoprol (10(-7) to 10(-9) mol/L) were performed over 96 hours." | ( Comparative activity of melarsoprol and arsenic trioxide in chronic B-cell leukemia lines. Gabrilove, JL; Jakubowski, A; König, A; Pandolfi, PP; Rivi, R; Warrell, RP; Wrazel, L, 1997) | 0.89 |
" The higher frequency of relapses in 1994 to 1997 was associated with an incremental dosage regimen of melarsoprol." | ( Trypanosomiasis relapse after melarsoprol therapy, Democratic Republic of Congo, 1982-2001. Mpia, B; Pépin, J, 2005) | 0.83 |
" injections separated by 1-week intervals, but with graded dosing (1." | ( Randomized controlled trial of three regimens of melarsoprol in the treatment of Trypanosoma brucei gambiense trypanosomiasis. Mpia, B; Pépin, J, 2006) | 0.59 |
" 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 |
" A combination chemotherapy, eflornithine alongside nifurtimox, has been introduced to decrease the time frame and overall dosing of eflornithine and reducing the risk of drug resistance emerging." | ( Potential new drugs for human African trypanosomiasis: some progress at last. Barrett, MP, 2010) | 0.36 |
" The introduction of the combination of nifurtimox and eflornithine (NECT) has accelerated the shift from melarsoprol to the best treatment available, due to reduced dosage and treatment time for eflornithine that has significantly lessened the cost and improved the burden of logistics encountered during treatment and distribution." | ( Update on field use of the available drugs for the chemotherapy of human African trypanosomiasis. Diarra, A; Franco, J; Jannin, J; Postigo, JA; Simarro, PP, 2012) | 0.59 |
" 28DAP010 showed efficacy similar to that of DB829 in dose-response studies in mouse models of first- and second-stage African sleeping sickness." | ( In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness. Boykin, DW; Braissant, O; Brun, R; Ismail, MA; Patrick, DA; Tidwell, RR; Wang, MZ; Wenzler, T; Yang, S, 2014) | 0.4 |
"We have shown that drug dose-response can be evaluated using bioluminescence imaging and confirmed quantification of tissue parasite load using qPCR." | ( A sensitive and reproducible in vivo imaging mouse model for evaluation of drugs against late-stage human African trypanosomiasis. Bradley, B; Burrell-Saward, H; Croft, SL; Rodgers, J; Ward, TH, 2015) | 0.42 |
"Current treatments for Human African Trypanosomiasis (HAT) are limited in their application, have undesirable dosing regimens and unsatisfactory toxicities highlighting the need for the development of a safer drug pipeline." | ( Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes. Arroo, RRJ; Bhambra, AS; Burrell-Saward, H; Edgar, M; Elsegood, MRJ; Krystof, V; Li, Y; Weaver, GW; Yardley, V, 2016) | 0.43 |
Class | Description |
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triazines | Compounds based on a triazine skeleton. |
[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] |
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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 | |||
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AID389450 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream trypomastigotes | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID748437 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes after 72 hrs by Alamar blue assay | 2013 | ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6 | New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi. |
AID274295 | Antiprotozoal activity against chloroquine-, pyrimethamine-resistant Plasmodium falciparum K1 | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
AID1196797 | Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar Blue assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3 | Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents. |
AID433913 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by alamar blue based microplate assay | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis of a series of N6-substituted adenosines with activity against trypanosomatid parasites. |
AID419759 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as parasite free mouse survival at 2 mg/kg, ip administered for 4 consecutive days from day 3 to 6 postinfection measured up to 60 days | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
AID1156609 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 trypomastigotes | 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. |
AID1163232 | Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth 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. |
AID214465 | 50% antitrypanosomal activity against Trypanosoma rhodesiense | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Lepadins D-F: antiplasmodial and antitrypanosomal decahydroquinoline derivatives from the tropical marine tunicate Didemnum sp. |
AID635852 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by resazurin-based spectrophotometric assay | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24 | Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents. |
AID215328 | Evaluated in vitro for antitrypanosomal activity against Trypanosoma brucei | 2002 | Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24 | Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides. |
AID264014 | Cytotoxicity against J774.1 cell line after 48 hrs | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents. |
AID1483953 | Antiprotozoal activity against patient derived Trypanosoma brucei rhodesiense STIB 900 bloodstream form after 72 hrs by Alamar Blue assay | 2017 | Journal of natural products, 02-24, Volume: 80, Issue:2 | Dioncophyllines C |
AID253516 | In vitro inhibitory concentration against blood stream Trypanosoma brucei brucei AT1 wild type incubated for 72 h at 37 degree C | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID235941 | In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as cured/infected; 4/4 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID1578097 | Antitrypanosomal activity against Leishmania donovani | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 | Antiprotozoal alkaloid principles of the plant family Amaryllidaceae. |
AID341606 | Antimicrobial activity against Babesia divergens 1903B | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID1578095 | Antitrypanosomal activity against Trypanosoma cruzi after 48 hrs by [3H]-hypoxanthine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 | Antiprotozoal alkaloid principles of the plant family Amaryllidaceae. |
AID286669 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID597077 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream form after 72 hrs by microplate fluorimetry | 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. |
AID1306906 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB 900 bloodstream forms | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead. |
AID322077 | Cytotoxicity against human HL60 cells | 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. |
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] | |||
AID303244 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations. |
AID1062627 | Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID1612294 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 72 hrs by Alamar blue staining-based fluorometric analysis | 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. |
AID341602 | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID419754 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream Trypanosoma brucei rhodesiense STIB900 | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
AID562491 | Antitrypanosomal activity against Trypanosoma brucei brucei AT1KO by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID300098 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16 | Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID274299 | Survival of NMRI mouse infected with Trypanosoma brucei brucei at 0.5 mg/kg, ip | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
AID432059 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected NMRI mouse assessed mean survival time at 4 mg/kg, ip dosed for 4 days | 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. |
AID1068803 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition after 70 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Activity of diimidazoline amides against African trypanosomiasis. |
AID322076 | Antimicrobial activity against Trypanosoma brucei brucei clone 427-221a after 48 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. |
AID1240950 | Toxicity in late-stage human african trypanosomiasis patient assessed as mortality rate following 10-day schedule | 2015 | Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17 | 6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors. |
AID562487 | Antitrypanosomal activity against Trypanosoma brucei gambiense K03048 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID596419 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes | 2011 | Journal of natural products, Apr-25, Volume: 74, Issue:4 | Marinoquinolines A-F, pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes). |
AID1062626 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID1410115 | Antiplasmodial activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote after 72 hrs by Alamar blue assay | 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. |
AID1126157 | Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB900 | 2014 | Journal of natural products, Apr-25, Volume: 77, Issue:4 | Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4. |
AID1163241 | Metabolic stability in mouse plasma assessed as compound remaining after 1 hr | 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. |
AID582593 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense ST1B900 trypomastigote infected in NMR1 mouse assessed as inhibition of parasitemia at 50 mg/kg, ip administered on day 3 post infection for 4 days | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives. |
AID1068802 | Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3 | Activity of diimidazoline amides against African trypanosomiasis. |
AID1254914 | Antitrypanosomal activity against bloodstream trypomastigote forms of Trypanosoma brucei rhodesiense STIB 900 assessed as inhibition of growth | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents. |
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. |
AID616288 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes 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. |
AID251291 | In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain, measured as survival days (control 7 days) | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
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. |
AID1779353 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 incubated for 70 hrs by resazurin dye-based fluorometric analysis | 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. |
AID372430 | Antileishmanial activity against Leishmania donovani MHOMET-67/L82 amastigotes 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. |
AID1177050 | Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3 | Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite. |
AID562486 | Antitrypanosomal activity against melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID400721 | Cytotoxicity against human HT-29 cells | 1998 | Journal of natural products, May, Volume: 61, Issue:5 | Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers. |
AID671047 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by Alamar blue growth inhibition assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14 | Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies. |
AID692982 | Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | 1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis. |
AID264012 | Inhibition of Trypanosoma brucei rhodesiense rhodesain at 200 uM | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents. |
AID482888 | Inhibition of human liver cathepsin B at 100 uM | 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. |
AID1500573 | Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 72 hrs by Alamar Blue assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines. |
AID311643 | Antiparasitic activity against Trypanosoma brucei rhodesiense by Alamar blue assay | 2007 | Journal of natural products, Oct, Volume: 70, Issue:10 | Antiprotozoal polyacetylenes from the Tanzanian medicinal plant Cussonia zimmermannii. |
AID482887 | Antitrypanosomal activity against Trypanosoma brucei brucei | 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. |
AID341604 | Antimicrobial activity against Giardia duodenalis WB | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID1313991 | Antiparasitic activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 assessed as growth inhibition after 72 hrs by resazurin 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. |
AID562495 | Ratio of IC50 for Trypanosoma brucei gambiense ITMAP141267 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB903 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID1062624 | Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as decrease in parasitemia at 5 mg/kg, ip qd administered for 4 days measured once per week until 60 days by microscopic analysis | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID432044 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 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. |
AID378568 | Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes | 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. |
AID482885 | Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain at 100 uM | 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. |
AID439872 | Antimicrobial activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote forms | 2009 | Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21 | Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles. |
AID774788 | Antiprotozoal activity against Trypanosoma brucei rhodesiense 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. |
AID562498 | Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for Trypanosoma brucei gambiense STIB930 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID1546292 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 amastigotes assessed as growth inhibition after 72 hrs by Alamar Blue dye-based fluorometric analysis | 2020 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1 | A new chemotype with promise against Trypanosoma cruzi. |
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] | |||
AID1743672 | Trypanocidal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes incubated for 72 hrs by Alamar blue assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Palladium-catalysed synthesis of arylnaphthoquinones as antiprotozoal and antimycobacterial agents. |
AID404375 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives. |
AID723217 | Trypanocidal activity against Trypanosoma brucei rhodesiense Z310 after 72 hrs by Alamar blue assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro. |
AID322078 | Selectivity index, ratio of EC50 for HL60 cells to EC50 for Trypanosoma brucei brucei clone 427-221a | 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. |
AID644196 | Antitrypanosomal activity against blood stream form of Trypanosoma brucei after 69 hrs by resazurin-based fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinol derivatives as potential trypanocidal agents. |
AID384321 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity. |
AID710596 | Antitrypanosomal activity against trypomastigote form of Trypanosoma brucei rhodesiense STIB 900 assessed as growth inhibition after 72 hrs by microplate fluorometry | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile. |
AID1271906 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by alamar blue assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes. |
AID1240903 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | 2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile. |
AID692981 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms assessed as reduction in cell viability after 70 hrs by alamar blue assay | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | 1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis. |
AID509507 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 at 4.8 ug/mL by microplate alamar blue assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Synthesis and preliminary bioactivity assays of 3,4-dichloro-5-(omega-hydroxyalkylamino)-2(5H)-furanones. |
AID235934 | In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as survival days (control 7 days); ND is not determined | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID418759 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as mouse survival at 8 mg/kg, ip administered from day 3 to day 6 postinfection | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
AID473011 | Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain 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. |
AID400720 | Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 | 1998 | Journal of natural products, May, Volume: 61, Issue:5 | Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers. |
AID1359978 | Antitrypanosomal activity against Trypanosoma brucei gambiense GUTat 3.1 after 72 hrs by Alamar Blue assay | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent. |
AID231796 | Ratio of cytotoxicity against L6 cells to that of antitrypanosomal activity against Trypanosoma brucei rhodesiense | 2004 | Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9 | Bisguanidine, bis(2-aminoimidazoline), and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation. |
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. |
AID260370 | Antiprotozoal activity against Trypanosoma brucei brucei GVR35 | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines. |
AID341607 | Antimicrobial activity against Babesia divergens 4201 | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID247964 | Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID1306903 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms 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. |
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. |
AID351791 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense 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. |
AID445257 | Toxicity in NMRI mouse infected with Trypanosoma brucei rhodesiense STIB900 assessed as survival at 8 mg/kg, ip after administered for 4 consecutive days from day 3 postinfection measured after 7 to 30 days | 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. |
AID1728297 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 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. |
AID634012 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 72 hrs by serial dilution Alamar blue assay | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds. |
AID418755 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as survival and aparasitemic condition at 2 mg/kg, ip administered from day 3 to day 6 postinfection measured after 60 days postinfect | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
AID666698 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6 | Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes. |
AID1298168 | Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11 | Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense. |
AID1405620 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigote after 72 hrs by Alamar Blue assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents. |
AID1177591 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 | 2014 | Journal of natural products, Aug-22, Volume: 77, Issue:8 | Xenortide Biosynthesis by Entomopathogenic Xenorhabdus nematophila. |
AID260369 | Antiprotozoal activity against Leishmania donovani MHOM/ET/L82/LV9 | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines. |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID765716 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 2 mg/kg, ip administered for 4 days | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID562484 | Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID418748 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes 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. |
AID335551 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by alamar blue assay | 2002 | Journal of natural products, Aug, Volume: 65, Issue:8 | Ancistrocongolines A-D, new naphthylisoquinoline alkaloids from ancistrocladus congolensis. |
AID475977 | Inhibition of Trypanosoma brucei brucei recombinant cathepsin B assessed after 5 mins by spectrofluorimetry | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi. |
AID106021 | Tested for cytotoxicity towards human MRC-5 cells | 2002 | Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24 | Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides. |
AID562489 | Antitrypanosomal activity against Trypanosoma brucei gambiense STIB930 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID473010 | Inhibition of Plasmodium falciparum recombinant falcipain-3 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. |
AID336751 | Antitrypanosomal activity against Trypanosoma brucei brucei Lab110 EATRO after 48 hrs | 2003 | Journal of natural products, Mar, Volume: 66, Issue:3 | Trypanocidal diarylheptanoids from Aframomum letestuianum. |
AID475975 | Antitrypanosomal activity against Trypanosoma brucei brucei 427-221a after 40 hrs by bioluminescence assay | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi. |
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. |
AID341601 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID720847 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 70 hrs by resazurin reduction assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3 | Aminoalkyl derivatives of guanidine diaromatic minor groove binders with antiprotozoal activity. |
AID1541166 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes assessed as growth inhibition after 72 hrs by Alamar Blue dye-based fluorometric analysis | |||
AID764882 | Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom. |
AID264016 | Selectivity index, IC50 for J774.1/IC50 for Trypanosoma brucei brucei | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents. |
AID765710 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as cured animal at 2 mg/kg, ip administered for 4 days | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID552695 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation. |
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. |
AID1163238 | Metabolic stability in human liver microsomes assessed as compound remaining after 15 mins by UPLC analysis | 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. |
AID1462698 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote bloodstream form assessed as growth inhibition at 0.8 ug/ml after 72 hrs by resazurin dye-based fluorometric analysis relative to control | 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. |
AID441747 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives. |
AID562488 | Antitrypanosomal activity against Trypanosoma brucei gambiense ITMAP141267 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID728609 | Antitrypanosomal activity against bloodstream forms of wild type Trypanosoma brucei rhodesiense STIB900 after 70 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT). |
AID453254 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense | 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. |
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. |
AID243451 | In vitro inhibitory concentration against P2 aminopurine transporter of Trypanosoma brucei brucei 427 adenosine (0.5 uM) uptake in presence of 1 mM inosine | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID300097 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense 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. |
AID725218 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by Alamar blue assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2 | Discovery and preliminary structure-activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds. |
AID562493 | Ratio of IC50 for melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB901 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID621153 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 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. |
AID756883 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as host mean survival days at 5 mg/kg, ip qd for 4 days | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID215678 | Minimum concentration producing complete lysis of all trypanosomes within 30 min at 37 degrees C in vitro | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Potential antitrypanosomal agents. 1,N2-Disubstituted 2-amino-5-hydroxy-4-methylnaphtho[1,2-d]thiazolium salts and related compounds. |
AID1432876 | Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis and activity of nucleoside-based antiprotozoan compounds. |
AID1163240 | Metabolic stability in human plasma assessed as compound remaining after 1 hr | 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. |
AID677571 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing tet-inducible NTR in presence of tetracycline after 3 days | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents. |
AID372438 | Antitrypanosomal activity against wild type Trypanosoma cruzi BS221 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. |
AID727321 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms incubated for 70 hrs by Alamar blue assay | 2013 | Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4 | Synthesis and in vitro antimalarial testing of neocryptolepines: SAR study for improved activity by introduction and modifications of side chains at C2 and C11 on indolo[2,3-b]quinolines. |
AID373520 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 | 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. |
AID252610 | In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as cured/infected; 0/4 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID1163231 | Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth 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. |
AID1163237 | Stability of the compound in PBS buffer assessed as recovery at pH 7.4 measured after 24 hrs by UPLC analysis | 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. |
AID562490 | Antitrypanosomal activity against Trypanosoma brucei brucei BS221 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID1480085 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 6 hrs by Alamar blue assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | 2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design. |
AID456259 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense 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. |
AID1586758 | Antiprotozoal activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay | 2018 | Journal of natural products, 12-28, Volume: 81, Issue:12 | Antiprotozoal Isoprenoids from Salvia hydrangea. |
AID1617101 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes incubated for 72 hrs by Alamar blue staining-based fluorometric analysis | 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 |
AID1727700 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition measured after 70 hrs by Alamar blue assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | The discovery of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines. |
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. |
AID1653740 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition measured after 70 hrs by Alamar blue assay | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives. |
AID562485 | Antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID664487 | Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania. |
AID1165097 | Ratio of IC50 for bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase in absence of tetracycline to IC50 for bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I n | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents. |
AID372440 | Resistance factor, ratio of IC50 for tbat1 knock out Trypanosoma cruzi BS221 to IC50 for wild type Trypanosoma cruzi BS221 | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | 2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. |
AID562494 | Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB902 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID764881 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream form of Trypanosoma brucei rhodesiense STIB 900 | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID124568 | The compound was tested for in vivo activity against a rodent model of Trypanosoma brucei at the specified dose: 5 mg/kg, ip no. of days dosing = 1; All servived | 1999 | Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21 | Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase. |
AID626317 | Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue 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). |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
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. |
AID274294 | Selectivity index, IC50 for L6 cells/ IC50 for Trypanosoma brucei rhodesience | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20 | Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes. |
AID213651 | 50% antitrypanosomal activity against Trypanosoma cruzi | 2002 | Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14 | Lepadins D-F: antiplasmodial and antitrypanosomal decahydroquinoline derivatives from the tropical marine tunicate Didemnum sp. |
AID552697 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation. |
AID779145 | Antimicrobial activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by Alamar blue assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents. |
AID1462699 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote bloodstream form assessed as growth inhibition at 4.8 ug/ml after 72 hrs by resazurin dye-based fluorometric analysis relative to control | 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. |
AID418760 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as mouse survival at 2 mg/kg, ip administered from day 3 to day 6 postinfection | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
AID401527 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense | 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. |
AID626322 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream form of Trypanosoma brucei rhodesiense STIB 900 | 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). |
AID728605 | Antitrypanosomal activity against Trypanosoma brucei gambiense DAL 898R after 70 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1504891 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms after 72 hrs by alamar blue staining based fluorescence assay | 2018 | Journal of natural products, 01-26, Volume: 81, Issue:1 | Antiprotozoal Sesquiterpene Lactones and Other Constituents from Tarchonanthus camphoratus and Schkuhria pinnata. |
AID1298166 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 measured after 70 hrs by alamar blue staining based fluorescence analysis | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11 | Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense. |
AID389457 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as cured mouse at 2 mg/kg, ip daily for 4 days | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID1846640 | Antiprotozoal activity against patient-derived Trypanosoma brucei rhodesiense STIB assessed as parasite growth inhibition incubated for 70 hrs by resazurin dye based fluorometry | 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. |
AID336753 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense KETRI 243 As 10-3 isolate after 48 hrs | 2003 | Journal of natural products, Mar, Volume: 66, Issue:3 | Trypanocidal diarylheptanoids from Aframomum letestuianum. |
AID1165096 | Trypanocidal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase assessed as inhibition of proliferation after 3 days by resazurin assay in presence of tetracycline | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents. |
AID1679082 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 incubated for 70 hrs by Alamar blue dye-based fluorometric analysis | 2020 | RSC medicinal chemistry, Dec-17, Volume: 11, Issue:12 | Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness. |
AID1163230 | Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth 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. |
AID1480087 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 24 hrs by Alamar blue assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | 2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design. |
AID1176975 | Antiplasmodial activity against Trypanosoma brucei rhodesiense 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. |
AID445252 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 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. |
AID1355403 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 70 hrs by Alamar blue assay | 2018 | Journal of natural products, 06-22, Volume: 81, Issue:6 | Phytochemical Study of Salvia leriifolia Roots: Rearranged Abietane Diterpenoids with Antiprotozoal Activity. |
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. |
AID473012 | Antiplasmodial activity against Plasmodium falciparum W2 by flow cytometry | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID1193501 | Antiprotozoal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by Alamar blue assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Anti-trypanosomal cadinanes synthesized by transannular cyclization of the natural sesquiterpene lactone nobilin. |
AID482886 | Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain | 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. |
AID764884 | Antiprotozoal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by microplate fluorometry | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom. |
AID634014 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds. |
AID578277 | Antitrypanosomal activity against TbAT1 and HAPT1-deficient Trypanosoma brucei brucei B48 after 48 hrs by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5 | Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. |
AID322079 | Selectivity index, ratio of MIC for HL60 cells to MIC for Trypanosoma brucei brucei clone 427-221a | 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. |
AID558400 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7 | Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity. |
AID401652 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense | 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. |
AID1653746 | 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 bloodstream Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth in | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives. |
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. |
AID1348367 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB-900 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. |
AID432054 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected NMRI mouse assessed as infection cure rate at 4 mg/kg, ip dosed for 4 days | 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. |
AID389464 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as survival time at 1 mg/kg, ip administered daily for 4 days | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID416485 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by microplate assay | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates. |
AID315105 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes by microplate assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity. |
AID1614010 | Selectivity index, ratio of CC50 for rat L6 cels to IC50 for Trypanosoma brucei rhodesiense STIB900 trypomastigotes | 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. |
AID248973 | In vitro inhibitory concentration against intracellular amastigotes of Trypanosoma cruzi in rat skeletal myoblasts incubated for 37 degree C for 4 days | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID736304 | Antiparasitic activity against Trypanosoma brucei assessed as growth inhibition | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4 | Examination of the mode of action of the almiramide family of natural products against the kinetoplastid parasite Trypanosoma brucei. |
AID710591 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for trypomastigote form of Trypanosoma brucei rhodesiense strain STIB 900 | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1165095 | Trypanocidal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase assessed as inhibition of proliferation after 3 days by resazurin assay in absence of tetracycline | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents. |
AID389451 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB 900 | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID464872 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream form | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi. |
AID303262 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 in procyclic stage | 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. |
AID637699 | Trypanocidal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms after 72 hrs by resazurin assay | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anti-protozoal activity of novel dihydropyrrolo[3,4-d][1,2,3]triazoles. |
AID253519 | In vitro inhibitory concentration against blood stream Trypanosoma brucei brucei AT1 knockout mutant with a non functional P2 transporter incubated for 72 h at 37 degree C | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID445268 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean parasitemia relaps day at 1 mg/kg, ip | 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. |
AID1163235 | Solubility of the compound in 10 mM PBS buffer solution at pH7.4 at 3.125 to 200 uM after 2 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. |
AID106020 | In Vitro cytotoxicity on MRC-5 cells | 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. |
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] | |||
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID677575 | Selectivity ratio of IC50 for Trypanosoma brucei brucei Lister 427 clone 221a overexpressing tet-inducible NTR in presence of tetracycline to IC50 for Trypanosoma brucei brucei overexpressing tet-inducible NTR in absence of tetracyclin | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents. |
AID756894 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID677572 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing tet-inducible NTR in absence of tetracycline after 3 days | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents. |
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. |
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. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID525502 | Antiparasitic activity against Trypanosoma brucei BSF overexpressing NTR gene after 3 days by Alamar blue assay | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Exploiting the drug-activating properties of a novel trypanosomal nitroreductase. |
AID1165094 | Trypanocidal activity against wild type bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a assessed as inhibition of proliferation after 3 days by resazurin assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents. |
AID1359979 | Toxicity in ip dosed mouse measured over 72 hrs | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent. |
AID482884 | Inhibition of Trypanosoma brucei rhodesiense rhodesain 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. |
AID303247 | Selectivity index, ratio for IC50 of rat L6 cells to IC50 of Trypanosoma brucei rhodesiense STIB900 | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID475983 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi. |
AID1143878 | Selectivity index, ratio of CC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Antiprotozoal activity and DNA binding of N-substituted N-phenylbenzamide and 1,3-diphenylurea bisguanidines. |
AID356389 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense | 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. |
AID1348066 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 70 hrs by Alamar blue staining-based fluorometric analysis | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Synthesis of new 1-benzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities. |
AID215356 | In Vitro inhibition concentration against Trypomastigote form of Trypanosoma brucei | 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. |
AID1503756 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense bloodstream forms after 72 hrs by alamar blue staining based fluorescence assay | 2017 | Journal of natural products, 10-27, Volume: 80, Issue:10 | Jozilebomines A and B, Naphthylisoquinoline Dimers from the Congolese Liana Ancistrocladus ileboensis, with Antiausterity Activities against the PANC-1 Human Pancreatic Cancer Cell Line. |
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. |
AID1541616 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STI B900 measured after 72 hrs by alamar blue dye based fluorimetry analysis | 2019 | Journal of natural products, 12-27, Volume: 82, Issue:12 | Structure, Biosynthesis, and Bioactivity of Photoditritide from |
AID1240908 | Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | 2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile. |
AID389459 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as cured mouse at 1 mg/kg, ip daily for 4 days | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID1240902 | Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by alamar blue assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | 2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile. |
AID389462 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as survival time at 8 mg/kg, ip administered daily for 4 days | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID341600 | Antiplasmodial activity against Plasmodium falciparum NF54 | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID264013 | Trypanocidal activity against Trypanosoma brucei brucei after 48 hrs | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents. |
AID1348366 | Antitrypanosomal activity against suramin-sensitive Trypanosoma brucei brucei Squib 427 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. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1062629 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as growth inhibition after 70 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID389456 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as cured mouse at 8 mg/kg, ip daily for 4 days | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID646379 | Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse assessed as increase in survival time at 20 mg/kg, ip qd for 5 days measured after 180 days | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors. |
AID562496 | Ratio of IC50 for Trypanosoma brucei gambiense STIB930 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB904 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID419680 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense bloodstream trypomastigotes | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase. |
AID536810 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | QSAR guided synthesis of simplified antiplasmodial analogs of naphthylisoquinoline alkaloids. |
AID341605 | Antimicrobial activity against Giardia duodenalis G1 | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160). |
AID1432875 | Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 72 hrs by alamar blue assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Synthesis and activity of nucleoside-based antiprotozoan compounds. |
AID1062617 | Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 5 mg/kg, ip qd administered for 4 days | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID562492 | Ratio of IC50 for pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB900 | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289. |
AID419753 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 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. |
AID728606 | Antitrypanosomal activity against Trypanosoma brucei gambiense STIB930 after 70 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1578096 | Antitrypanosomal activity against Leishmania donovani after 48 hrs by [3H]-hypoxanthine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 | Antiprotozoal alkaloid principles of the plant family Amaryllidaceae. |
AID251297 | In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as survival days (control 7 days); ND is not determined | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID418761 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as mouse survival at 1 mg/kg, ip administered from day 3 to day 6 postinfection | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
AID235940 | In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain; Not determined | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID1163236 | Octanol-phosphate buffer partition coefficient, log D of the compound at pH 7.4 after 2 hrs of shaking after 2 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. |
AID445258 | Toxicity in NMRI mouse infected with Trypanosoma brucei rhodesiense STIB900 assessed as survival at 2 mg/kg, ip after administered for 4 consecutive days from day 3 postinfection measured after 7 to 30 days | 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. |
AID756895 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue 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. |
AID710592 | Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile. |
AID621158 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives. |
AID404597 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 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. |
AID260371 | Antiprotozoal activity against Trichomonas vaginalis CMP | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4 | Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines. |
AID728604 | Antitrypanosomal activity against Trypanosoma brucei gambiense KO48 after 70 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1480082 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar blue assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | 2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design. |
AID274745 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 | 2007 | Journal of natural products, Jan, Volume: 70, Issue:1 | Limonoid orthoacetates and antiprotozoal compounds from the roots of Pseudocedrela kotschyi. |
AID482889 | Inhibition of human liver cathepsin B | 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. |
AID1578093 | Antitrypanosomal activity against Trypanosoma cruzi | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 | Antiprotozoal alkaloid principles of the plant family Amaryllidaceae. |
AID362548 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 | 2008 | Journal of natural products, Sep, Volume: 71, Issue:9 | Antiprotozoal activities of heterocyclic-substituted xanthones from the marine-derived fungus Chaetomium sp. |
AID235933 | In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain, measured as survival days (control 7 days) | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID632296 | Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | Novel 3-nitro-1H-1,2,4-triazole-based aliphatic and aromatic amines as anti-chagasic agents. |
AID728616 | Antitrypanosomal activity against Trypanosoma brucei brucei 221 after 48 hrs by Cell Titre Glo assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT). |
AID1181596 | Antimicrobial activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by alamar blue assay | 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. |
AID578276 | Antitrypanosomal activity against TbAT1-deficient Trypanosoma brucei brucei after 48 hrs by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5 | Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. |
AID377196 | Antitrypanosomal activity against Trypanosoma rhodesiense | 2000 | Journal of natural products, Aug, Volume: 63, Issue:8 | Pelorol from the tropical marine sponge Dactylospongia elegans. |
AID372431 | Trypanocidal activity against Trypanosoma brucei rhodesiense STIB 900 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. |
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. |
AID767873 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 by Alamar Blue assay | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Antitrypanosomal triterpenoid with an ε-lactone E-ring from Salvia urmiensis. |
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. |
AID351794 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense | 2009 | Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10 | Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids. |
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. |
AID765724 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
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. |
AID419764 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival rate at 1 mg/kg, ip administered 4 consecutive days from day 3 to 6 postinfection | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
AID483199 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream form after 72 hrs by LILIT method | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei. |
AID759435 | Resistant factor, ratio of IC50 for bloodstream form of Trypanosoma brucei brucei expressing TbMRPA protein to IC50 for bloodstream form of wild type Trypanosoma brucei 247 | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | N-Benzyloxycarbonyl-S-(2,4-dinitrophenyl)glutathione dibutyl diester is inhibitory to melarsoprol resistant cell lines overexpressing the T. bruceiMRPA transporter. |
AID419763 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival rate at 2 mg/kg, ip administered 4 consecutive days from day 3 to 6 postinfection | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine. |
AID248971 | Inhibitory concentration in vitro against intracellular amastigotes of Leishmania donovani in rat skeletal myoblasts incubated for 96 hr at 27 degree C | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17 | Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites. |
AID1455940 | Antiprotozoal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay | |||
AID309300 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by Alamar blue assay | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21 | Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli. |
AID552696 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei s427 after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation. |
AID739090 | Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei Lister 427 after 48 hrs by hemocytometer | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis. |
AID762348 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream form after 70 hrs by Alamar blue assay | 2013 | European journal of medicinal chemistry, Aug, Volume: 66 | 3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis. |
AID1728296 | Trypanocidal activity against Trypanosoma brucei rhodesiense STIB900 incubated for 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. |
AID389463 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as survival time at 2 mg/kg, ip administered daily for 4 days | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans. |
AID445250 | Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay | 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. |
AID1300851 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 trypomastigotes assessed as inhibition of parasite growth after 72 hrs by Alamar blue assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds. |
AID1169287 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigote forms | 2014 | Journal of natural products, Oct-24, Volume: 77, Issue:10 | Antitrypanosomal quinoline alkaloids from the roots of Waltheria indica. |
AID378201 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 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. |
AID400722 | Selectivity index, ratio of IC50 for human HT29 cells to IC50 for Trypanosoma brucei rhodesiense STIB 900 | 1998 | Journal of natural products, May, Volume: 61, Issue:5 | Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers. |
AID527276 | Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs | 2010 | Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21 | 2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. |
AID661007 | Antitrypanosomal activity against Trypanosoma brucei brucei TC221 infected in mouse J774.1 cells after 48 hrs by alamar blue assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6 | Synthesis and structure-activity relationships of new quinolone-type molecules against Trypanosoma brucei. |
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. |
AID1578094 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 48 hrs by [3H]-hypoxanthine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20 | Antiprotozoal alkaloid principles of the plant family Amaryllidaceae. |
AID1439212 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar blue assay | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | Synthesis and antitrypanosomal activities of novel pyridylchalcones. |
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. |
AID418749 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 trypomastigotes | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Structure-activity study of pentamidine analogues as antiprotozoal agents. |
AID1245578 | Antiparasitic activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar blue assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID1193546 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms 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. |
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] | |||
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID475976 | Inhibition of Trypanosoma brucei brucei recombinant rhodesain after 5 mins by spectrofluorimetry | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi. |
AID634013 | Cytotoxicity against rat L6 cells | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds. |
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. |
AID1199917 | Antiprotozoal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 trypomastigote by alamar-blue assay | 2015 | Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4 | Antiprotozoal activity and DNA binding of dicationic acridones. |
AID441746 | Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by alamar blue assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 80 (18.52) | 18.7374 |
1990's | 65 (15.05) | 18.2507 |
2000's | 130 (30.09) | 29.6817 |
2010's | 143 (33.10) | 24.3611 |
2020's | 14 (3.24) | 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 (57.02) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 21 (4.58%) | 5.53% |
Reviews | 22 (4.79%) | 6.00% |
Case Studies | 26 (5.66%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 390 (84.97%) | 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 | ||
---|---|---|---|---|---|---|---|
Clinical Trial Comparing the Therapeutic Combinations Melarsoprol-Nifurtimox, Melarsoprol-Eflornithine and Eflornithine-Nifurtimox in the Treatment of Gambiense Human African Trypanosomiasis in the Meningo-Encephalitic Phase [NCT00330148] | Phase 3 | 435 participants | Interventional | 2001-03-31 | Terminated | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |