Diminazene: An effective trypanocidal agent.
diminazene : A triazene derivative that is triazene in which each of the terminal nitrogens is substituted by a 4-carbamimidoylphenyl group.
ID Source | ID |
---|---|
PubMed CID | 2354 |
CHEMBL ID | 35241 |
CHEBI ID | 81724 |
SCHEMBL ID | 120719 |
MeSH ID | M0006470 |
Synonym |
---|
diminazeno |
diminazenum |
536-71-0 |
diminazine |
benzenecarboximidamide, 4,4'-(1-triazene-1,3-diyl)bis- |
4-[(2e)-2-(4-carbamimidoylphenyl)iminohydrazino]benzamidine |
diminazene |
berenil (aceturate 2:1) |
4,4'-(1-triazene-1,3-diyl)bis-benzenecarboximidamide |
4,4'-(diazoamino)benzamidine |
DB03608 |
BRN , |
diminazene [inn:ban] |
diminazeno [inn-spanish] |
diminazenum [inn-latin] |
einecs 208-644-6 |
CHEMBL35241 |
chebi:81724 , |
diminazen |
FT-0655564 |
bdbm50000999 |
4-[2-(4-carbamimidoylphenyl)iminohydrazinyl]benzenecarboximidamide |
C18388 |
4-[2-(4-carbamimidoylphenyl)iminohydrazino]benzamidine;4,4'-(triaz-1-ene-1,3-diyl)dibenzimidamide |
A829723 |
pirocide |
AKOS015895569 |
RB8007 |
SCHEMBL120719 |
4-(2-(4-carbamimidoylphenyl)iminohydrazinyl)benzenecarboximidamide |
diminazene [inn] |
1443105-71-2 |
Y5G36EEA5Z , |
diminazene [who-dd] |
4,4'-triaz-1-ene-1,3-diyldibenzenecarboximidamide |
DTXSID7043792 |
AC-22588 |
AB01563384_01 |
AB01563384_02 |
unii-y5g36eea5z |
4,4'-(1-triazene-1,3-diyl)bisbenzenecarboximidamide |
4-[(1e)-3-(4-carbamimidoylphenyl)triaz-1-en-1-yl]benzenecarboximidamide |
diminazine aceturate; 1,3-tris-(4'amidinophenyl)triazine |
Q410958 |
4,4'-(triaz-1-ene-1,3-diyl)dibenzimidamide |
BCP13959 |
gtpl10307 |
4,4'-(1-triazene-1,3-diyl)bis[benzenecarboximidamide] |
diminazene-aceturate |
diminazene [inn:who-dd] |
GLXC-25308 |
CS-0453371 |
AS-75445 |
Dimonazene diaceturate is an anti-protozoal therapy that has been suggested for use in the treatment of acute cytauxzoonosis. Diminazene aceturate is a commonly used antibabesial agent.
Excerpt | Reference | Relevance |
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"Diminazene aceturate is a small-molecule inhibitor of ASICs with a reported apparent affinity in the low micromolar range, making it an interesting lead compound." | ( Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a). Gründer, S; Joussen, S; Rossetti, G; Schmidt, A, 2017) | 2.62 |
"Diminazene diaceturate is an anti-protozoal therapy that has been suggested for use in the treatment of acute cytauxzoonosis, but which failed to clear the carrier state at the dose used in acute illness." | ( Failure of efficacy and adverse events associated with dose-intense diminazene diaceturate treatment of chronic Cytauxzoon felis infection in five cats. Birkenheuer, AJ; Cohn, LA; Lewis, KM; Marr, HS, 2014) | 1.36 |
"Diminazene aceturate is a commonly used antibabesial agent. " | ( The effects of diminazene aceturate on systemic blood pressure in clinically healthy adult dogs. Joubert, KE; Kettner, F; Lobetti, RG; Miller, DM, 2003) | 2.11 |
Excerpt | Reference | Relevance |
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"Diminazene aceturate has remained a very important therapeutic drug for trypanosomosis in cattle, sheep and goats since its introduction into the market in 1955. " | ( A competitive enzyme-linked immunosorbent assay for diminazene. Karanja, WM; Mdachi, RE; Murilla, GA, 2002) | 2.01 |
Dinazene aceturate treatment (15 mg/kg/day) activated ACE2, increased the circulating Ang (1-7) level, and augmented EDR and FMD in mouse arteries. Treatment did not change the lesion size, but ameliorated the composition of aortic root and low SS-induced carotid plaques.
The pharmacokinetic aspects of diminazene aceturate were studied in lactating goats and sheep after single intravenous and intramuscular administrations.
Excerpt | Reference | Relevance |
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" Pharmacokinetic parameters were calculated in which bioequivalence data (n = 10) together with data from an additional four cattle were used." | ( A bioequivalence and pharmacokinetic evaluation of two commercial diminazene aceturate formulations administered intramuscularly to cattle. Du Preez, JL; Gummow, B; Swan, GE, 1994) | 0.53 |
The study evaluated the effectiveness of oral administration of a doxycycline-enrofloxacin-metronidazole combination with and without injections of diminazene diaceturate. Susceptibility patterns of sensitive and resistant parasites were evaluated against calcium antagonists.
Excerpt | Reference | Relevance |
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"0 micrograms/ml in combination with diminazene aceturate or isometamidium chloride." | ( The effect of verapamil alone and in combination with trypanocides on multidrug-resistant Trypanosoma brucei brucei. Kaminsky, R; Zweygarth, E, 1991) | 0.56 |
" Susceptibility patterns of sensitive and resistant parasites were evaluated against calcium antagonists of several chemical classes (verapamil, cyproheptidine, desipramine and chlopromazine), alone and in combination with suramin, diminazene aceturate or melarsen oxide cyteamine." | ( Trypanocidal resistance in Trypanosoma evansi in vitro: effects of verapamil, cyproheptidine, desipramine and chlorpromazine alone and in combination with trypanocides. Anene, BM; Anika, SM; Chukwu, CC; Ross, CA, 1996) | 0.48 |
Excerpt | Reference | Relevance |
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" It therefore appears that drug bioavailability is altered or drug biotransformation occurs during the in vivo test." | ( In vivo and in vitro sensitivity of Trypanosoma evansi and T. equiperdum to diminazene, suramin, MelCy, quinapyramine and isometamidium. Baltz, T; Giroud, C; Zhang, ZQ, 1991) | 0.51 |
"The disposition kinetics and bioavailability of diminazene in five healthy heifers were determined after single intravenous (i." | ( Pharmacokinetics of diminazene in female Boran (Bos indicus) cattle. Aliu, YO; Mamman, M; Peregrine, AS, 1993) | 0.87 |
"Ingestion of proteinase inhibitors leads to hyperproduction of digestive proteinases, limiting the bioavailability of essential amino acids for protein synthesis, which affects insect growth and development." | ( Enzymatic response of the eucalypt defoliator Thyrinteina arnobia (Stoll) (Lepidoptera: Geometridae) to a bis-benzamidine proteinase Inhibitor. i. Guedes, RN; Lourenção, AL; Marinho-Prado, JS; Oliveira, JA; Oliveira, MG; Pallini, A, 2012) | 0.38 |
" In accordance with that, pharmacological ACE2 activation by DIZE treatment reduced ROS production and NADPH oxidase expression, and elevated nNOS and eNOS expression and NO bioavailability in the penis of ApoE(-/-) mice." | ( Diminazene protects corpus cavernosum against hypercholesterolemia-induced injury. Costa-Fraga, FP; da Silva, RF; Faye, Y; Fraga-Silva, RA; Mach, F; Montecucco, F; Pelli, G; Raizada, MK; Santos, RA; Shenoy, V; Stergiopulos, N; Sturny, M, 2015) | 1.86 |
"Endogenous ACE2-Ang (1-7) activation or ACE2 overexpression preserves endothelial function in diabetic mice through increasing nitric oxide bioavailability and inhibiting oxidative stress, suggesting the therapeutic potential of ACE2-Ang(1-7) axis activation against diabetic vasculopathy." | ( Upregulation of Angiotensin (1-7)-Mediated Signaling Preserves Endothelial Function Through Reducing Oxidative Stress in Diabetes. Cheang, WS; Huang, Y; Lan, HY; Lau, CW; Liu, J; Luo, JY; Raizada, MK; Tian, XY; Wang, L; Wong, CM; Wong, WT; Xu, J; Yao, X; Zhang, Y, 2015) | 0.42 |
The pharmacokinetics, urinary excretion and dosage regimen of diminazene were investigated in crossbred male calves following a single intramuscular dose (3.5 mg) The study shows that low doses of diminishazene at rates of 2 mg/kg and 1mg/kg were encountered in the infected untreated controls and those treated at day 8 post-infection with a sub-optimal dosage of Berenil.
Excerpt | Relevance | Reference |
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" The activity of each drug was expressed as: 1) in vitro: the minimal effective concentration which killed trypanosome population by 100% within 24 h of drug exposure (MEC100); the maximum tolerated concentration in which trypanosomes could propagate at the same rate as the controls during 48 h of drug exposure (MTC100); 2) in vivo: the curative dosage in 100% of infected mice (CD100); the highest ineffective dosage: 100% of infected mice remain infected (ID100)." | ( In vivo and in vitro sensitivity of Trypanosoma evansi and T. equiperdum to diminazene, suramin, MelCy, quinapyramine and isometamidium. Baltz, T; Giroud, C; Zhang, ZQ, 1991) | 0.51 |
" These finding indicate that the majority of the relapse trypanosomes were susceptible the the drug dosage used for selecting the population and that, surprisingly, the calculated proportion of organisms which survived drug exposure varied inversely with the inoculum size." | ( Frequency of diminazene-resistant trypanosomes in populations of Trypanosoma congolense arising in infected animals following treatment with diminazene aceturate. Gettinby, G; Kemei, S; Mamman, M; Murphy, NB; Peregrine, AS, 1995) | 0.66 |
" When this third group was treated, the frequency of trypanosomes resistant to the drug dosage was estimated to be less than 1 in 10(3)." | ( Apparent rarity of diminazene-resistant trypanosomes in goats infected with a diminazene-resistant population of Trypanosoma congolense. Mamman, M; Murphy, NB; Peregrine, AS; Williams, DJ, 1995) | 0.62 |
" The EC50 values calculated by means of dose-response curves were 45, 80, 165, 259 and 600 microM for 4', 6-diamidino-2-phenylindole (DAPI), dibromo propamidine, pentamidine 2-hydroxy stilbamidine and stilbamidine, respectively, although no inhibitory effects on cell growth were found at 1 mM propamidine, phenamidine and amicarbalide." | ( Putrescine uptake inhibition by aromatic diamidines in Leishmania infantum promastigotes. Alvarez Bujidos, ML; Balaña Fouce, R; Cubria, JC; Ordoñez, D; Reguera, R, 1994) | 0.29 |
", when the same flies were allowed to feed on clean goats, the resultant infections were sensitive to treatment with the same drug dosage when administered 24 h following infection." | ( Variation in sensitivity of Trypanosoma congolense to diminazene during the early phase of tsetse-transmitted infection in goats. Katende, J; Mamman, M; Moloo, SK; Peregrine, AS, 1993) | 0.53 |
" Underdosing with trypanocides appeared to be uncommon and the indications were that farmers generally gave the drugs at dosage rates above the recommended standard dose." | ( The use of trypanocides and antibiotics by Maasai pastoralists. Mwendia, C; Okech, G; Roderick, S; Stevenson, P, 2000) | 0.31 |
"The pharmacokinetics, urinary excretion and dosage regimen of diminazene were investigated in crossbred male calves following a single intramuscular dose (3." | ( Pharmacokinetics, urinary excretion and dosage regimen of diminazene in crossbred calves. Chaudhary, RK; Kaur, G; Srivastava, AK, 2000) | 0.79 |
" Following the free of charge treatment of the adult cattle at intervals of 7 weeks and at a dosage of 15 ml/100 kg body weight, there was an increase in the average packed cell volume in the herd although the decline in the incidence of trypanosomal infections was more prolonged." | ( A large-scale trial to evaluate the efficacy of a 1% pour-on formulation of cyfluthrin (Cylence, Bayer) in controlling bovine trypanosomosis in Eastern Zambia. Jooste, R; Lumamba, D; Mubanga, J; Munsimbwe, L; Van den Bossche, P, 2004) | 0.32 |
" Method had the potential to determine these drugs simultaneously from dosage forms without any interference with each other." | ( Validation of an HPLC method for the simultaneous determination of diminazene diaceturate and phenazone in injectable veterinary granules and bulk powders. Bekhit, AA; Genete, G; Hymete, A; Kassaye, L, 2012) | 0.62 |
" Judicious treatment of confirmed trypanosomiasis cases with correct dosage would still be effective in controlling the disease since the observed resistance was at the population and not clonal level." | ( Variation of sensitivity of Trypanosoma evansi isolates from Isiolo and Marsabit counties of Kenya to locally available trypanocidal drugs. Alusi, PM; Auma, JE; Chemuliti, JK; Kurgat, RK; Mdachi, RE; Mugunieri, LG; Mukiria, PW; Ogolla, KO; Okoth, SO; Wamwiri, FN; Wanjala, KB, 2023) | 0.91 |
Role | Description |
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antiparasitic agent | A substance used to treat or prevent parasitic infections. |
trypanocidal drug | A drug used to treat or prevent infections caused by protozoal organisms belonging to the suborder Trypanosomatida. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
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triazene derivative | A nitrogen molecular entity resulting from the formal substitution of one or more of the hydrogens of triazene. |
carboxamidine | Compounds having the structure RC(=NR)NR2. The term is used as a suffix in systematic nomenclature to denote the -C(=NH)NH2 group including its carbon atom. |
[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] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Cathepsin B | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0002 | 1.8453 | 10.0000 | AID312631 |
Furin | Homo sapiens (human) | Ki | 5.4200 | 0.0042 | 1.2544 | 5.4200 | AID1895619 |
Amiloride-sensitive amine oxidase [copper-containing] | Homo sapiens (human) | Ki | 0.0130 | 0.0130 | 0.1515 | 0.2900 | AID1124814 |
Diamine acetyltransferase 1 | Homo sapiens (human) | Ki | 2.4000 | 2.0000 | 2.2000 | 2.4000 | AID1124816 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1881385 | Resistance factor, ratio of EC50 for bloodstream form of Trypanosoma brucei brucei B48 to EC50 for wild-type bloodstream form of Trypanosoma brucei brucei | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID666705 | Resistance factor, ratio of EC50 for diminazene-, pentamidine-, and melaminophenyl arsenical-resistant HAPT1-deficient Trypanosoma brucei brucei B48 to EC50 for wild type Trypanosoma brucei brucei Lister 427 | 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. |
AID1124807 | Inhibition of mouse hippocampal neurons ASIC transfected in CHO cells assessed as inhibition of acid-evoked current at -60 mV holding potential by two-electrode voltage-clamp electrophysiology assay | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Some non-conventional biomolecular targets for diamidines. A short survey. |
AID1312508 | Binding affinity to 5'-FAM/3'-TAMRA labeled c-MYC 22-mer G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 4 uM after 12 hrs by TR-FRET assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID466923 | Antitrypanosomal activity against Trypanosoma evansi ITMAV170475 after 48 hrs by alamar blue assay | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species. |
AID336011 | Displacement of ethidium bromide from calf thymus type 1 DNA after 24 hrs by microtiter assay | 1992 | Journal of natural products, Nov, Volume: 55, Issue:11 | A colorimetric microassay for the detection of agents that interact with DNA. |
AID1688798 | Resistance factor, ratio of EC50 for antitrypanosomal activity against drug resistant Trypanosoma brucei B48 to antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream form | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
AID489462 | Cytotoxicity against HEK239 cells after 72 hrs by Alamar blue assay | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | 7',8'-Dihydroobolactone, a typanocidal alpha-pyrone from the rainforest tree Cryptocarya obovata. |
AID1688794 | Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream forms assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
AID1394622 | Anti-parasitic activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 after 48 hrs in presence of 5 mM glycerol by resazurin-based assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. |
AID1312513 | Antiproliferative activity against human OVCAR3 cells after 72 hrs by WST-1 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID565591 | Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as complete cure from microbial infection at 2 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID1821420 | Trypanocidal activity against Trypanosoma evansi assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian |
AID1543056 | Inhibition of pH 6.6-stimulated mouse ASIC1a homomer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS. |
AID1624255 | Antitrypanosomal activity against Trypanosoma brucei TbAT1-KO after 48 hrs by alamar blue assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID1688795 | Antitrypanosomal activity against drug resistant Trypanosoma brucei harboring TbAT1 deficient assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
AID152454 | Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 10 ug/mL | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes. |
AID1688796 | Resistance factor, ratio of EC50 for antitrypanosomal activity against drug resistant Trypanosoma brucei harboring TbAT1 deficient to antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream form | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
AID1431830 | Anti-parasitic activity against bloodstream form of Trypanosoma congolense IL3000 after 48 hrs by alamar blue based fluorescence assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion. |
AID644198 | Antitrypanosomal activity against wild type Trypanosoma brucei after 3 days by resazurin-based fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinol derivatives as potential trypanocidal agents. |
AID279551 | Antiproliferative activity against Leishmania donovani DI700 promastigotes in presence of 100 uM spermidine | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Leishmania donovani polyamine biosynthetic enzyme overproducers as tools to investigate the mode of action of cytotoxic polyamine analogs. |
AID1431829 | Anti-parasitic activity against diminazene, pentamidine and melaminophenyl arsenical-resistant bloodstream trypomastigote stage of Trypanosoma brucei brucei B48 harboring TbAT1 deletion mutant after 48 hrs by alamar blue based fluorescence assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion. |
AID1821411 | Trypanocidal activity against Trypanosoma brucei brucei GUTat3.1 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian |
AID1679081 | Selectivity index, ratio of IC50 for human HEK293 cells to IC50 for antitrypanosomal activity against Trypanosoma brucei brucei 427 | 2020 | RSC medicinal chemistry, Dec-17, Volume: 11, Issue:12 | Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness. |
AID1881380 | Resistance factor, ratio of EC50 for bloodstream form of diminazene-resistant Trypanosoma congolense DimR to EC50 for bloodstream form of wild-type Trypanosoma congolense | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID279546 | Antiproliferative activity against Leishmania donovani DI700 promastigotes | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Leishmania donovani polyamine biosynthetic enzyme overproducers as tools to investigate the mode of action of cytotoxic polyamine analogs. |
AID1881378 | Antitrypanosomal activity against bloodstream form of diminazene-resistant Trypanosoma congolense DimR measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID279547 | Antiproliferative activity against Leishmania donovani DI700 promastigotes overproducing ODC enzyme | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Leishmania donovani polyamine biosynthetic enzyme overproducers as tools to investigate the mode of action of cytotoxic polyamine analogs. |
AID1543058 | Inhibition of pH 6.25-stimulated mouse ASIC1a/2a heterodimer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS. |
AID1124816 | Inhibition of human SSAT using spermidine as substrate | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Some non-conventional biomolecular targets for diamidines. A short survey. |
AID1394624 | Resistance factor, ratio of EC50 for bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 in presence of 5 mM glycerol to EC50 for bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. |
AID1821417 | Trypanocidal activity against Trypanosoma brucei rhodesiense IL1501 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian |
AID1182805 | Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 grown in HMI-9 medium after 48 hrs by Alamar blue assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1. |
AID666703 | Resistance factor, ratio of EC50 for diminazene aceturate-resistant TbAT1 gene-deficient Trypanosoma brucei brucei AT1-KO to EC50 for wild type Trypanosoma brucei brucei Lister 427 | 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. |
AID1808246 | Antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei brucei B48 assessed as reduction in parasite viability by resazurin-based assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure-Activity Relationship Studies. |
AID1394621 | Anti-parasitic activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 after 48 hrs by resazurin-based assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. |
AID1624257 | Antitrypanosomal activity against isometamidium resistant Trypanosoma brucei ISMR1 after 48 hrs by alamar blue assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID466918 | Antitrypanosomal activity against diminazene-resistant Trypanosoma brucei brucei deltaTbat1-KO after 48 hrs by alamar blue assay | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species. |
AID1624256 | Antitrypanosomal activity against pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 after 48 hrs by alamar blue assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID1124814 | Mixed type inhibition of recombinant human DAO expressed in drosophila S2 cells | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Some non-conventional biomolecular targets for diamidines. A short survey. |
AID478755 | Binding affinity to d(CGCGATATCGCG)2 dodecamer assessed as change in melting temperature | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Theoretical models of pentamidine analogs activity based on their DNA minor groove complexes. |
AID152455 | Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 1 ug/mL | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes. |
AID565593 | Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 1 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID312631 | Inhibition of human liver cathepsin B | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. |
AID1312517 | Antiproliferative activity against human MCR5A cells after 72 hrs by WST-1 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1202924 | Antitrypanosomal activity against AT1 knock out Trypanosoma brucei brucei assessed as cell viability after 48 hrs by alamar blue assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts. |
AID1431844 | Resistant factor, ratio of EC50 for bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 assessed as inhibition of respiration in presence of glycerol to EC50 for bloodstream trypomastigote stage of wild-type Trypanosoma bruc | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion. |
AID441755 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 795 infected in NMRI mouse African trypanosomiasis model assessed as parasite free mouse survival at 10 mg/kg, ip qd administered for 4 consecutive days from day 3 to 6 postinfection me | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives. |
AID1394629 | Anti-parasitic activity against bloodstream trypomastigote stage of pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 after 48 hrs by resazurin-based assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. |
AID336010 | Displacement of methyl green from DNA after 24 hrs by microtiter assay | 1992 | Journal of natural products, Nov, Volume: 55, Issue:11 | A colorimetric microassay for the detection of agents that interact with DNA. |
AID395133 | Binding affinity to poly(dA).poly(dT) duplex DNA assessed as ratio of KA to KB by ESI-MS analysis | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Ligand binding to nucleic acids and proteins: Does selectivity increase with strength? |
AID1312512 | Binding affinity to 5'-FAM/3'-TAMRA labeled 26-mer duplex DNA (unknown origin) assessed as change in melting temperature at 4 uM after 12 hrs by TR-FRET assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1312551 | Binding affinity to wild type Bcl2 27-mer G-quadruplex DNA (unknown origin) by isothermal titration calorimetry | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1394632 | Resistance factor, ratio of EC50 for bloodstream trypomastigote stage of pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 to EC50 for bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. |
AID1202925 | Resistance factor, ratio of EC50 for AT1 knock out Trypanosoma brucei brucei to EC50 for wild type Trypanosoma brucei brucei s427 trypomastigotes | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts. |
AID1202923 | Antitrypanosomal activity against wild type Trypanosoma brucei brucei s427 trypomastigotes assessed as cell viability after 48 hrs by alamar blue assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts. |
AID215159 | Trypanocidal activity against Trypanosoma brucei, exposure of parasites to compound prior to injection into mice at 10 e-6 M concentration in dark conditions | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Identification of an acridine photoaffinity probe for trypanocidal action. |
AID1312509 | Binding affinity to 5'-FAM/3'-TAMRA labeled F21T 21-mer G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 4 uM after 12 hrs by TR-FRET assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1881379 | Antitrypanosomal activity against bloodstream form of diminazene-resistant Trypanosoma congolense EMS MUT DimR measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID1821419 | Trypanocidal activity against Trypanosoma brucei congolense IL3000 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian |
AID1808248 | Resistance factor, ratio of EC50 for antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei brucei B48 to EC50 for antitrypanosomal activity against bloodstream form trypomastigotes of wild type Trypanosoma brucei brucei Lister 427 | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure-Activity Relationship Studies. |
AID1394623 | Anti-parasitic activity against bloodstream form of Trypanosoma congolense IL3000 after 48 hrs by resazurin-based assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense. |
AID1881392 | Antitrypanosomal activity against bloodstream form of Trypanosoma congolense measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID1312511 | Binding affinity to 5'-FAM/3'-TAMRA labeled k-RAS21R 21-mer G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 4 uM after 12 hrs by TR-FRET assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1312534 | Stabilization of c-MYC template Pu27 mutant DNA (unknown origin) assessed as inhibition of Taq polymerase-mediated polymerization/extension of Pu27 mutant and Pu27rev oligomers at 1 to 25 uM preincubated for 6 hrs followed by Taq polymerase addition by PC | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1688800 | Resistance factor, ratio of EC50 for antitrypanosomal activity against drug resistant Trypanosoma brucei ISMR1 to antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream form | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
AID489459 | Antitrypanosomal activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | 7',8'-Dihydroobolactone, a typanocidal alpha-pyrone from the rainforest tree Cryptocarya obovata. |
AID1312510 | Binding affinity to 5'-FAM/3'-TAMRA labeled c-kit2 26-mer G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 4 uM after 12 hrs by TR-FRET assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1624260 | Resistance factor, ratio of EC50 for isometamidium resistant Trypanosoma brucei B48 to EC50 for wild type Trypanosoma brucei Lister 427 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID1821416 | Trypanocidal activity against Trypanosoma brucei gambiense IL1922 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian |
AID152453 | Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 100 ug/mL | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes. |
AID225778 | Inhibitory concentration against ethidium in DNA-binding assay with [poly(dG-dC)]2 (synthetic oligonucleotide) | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID54990 | Change in DNA-melting (deltaTm) with calf thymus DNA at pH 7.0 | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID1881384 | Resistance factor, ratio of EC50 for bloodstream form of tbat1-/- deficient Trypanosoma brucei brucei to EC50 for wild-type bloodstream form of Trypanosoma brucei brucei | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID666702 | Antitrypanosomal activity against diminazene aceturate-resistant TbAT1 gene-deficient Trypanosoma brucei brucei AT1-KO after 3 days 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. |
AID396382 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Pharmacophore based discovery of potential antimalarial agent targeting haem detoxification pathway. |
AID552699 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as suppression of parasitemia level in mouse tail blood at 10 mg/kg, ip qd for 4 consecutive days measured 5 days post infection | 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. |
AID54988 | Change in DNA-melting (deltaTm) with calf thymus DNA at pH 65.0 | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID1881372 | Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei Lister 427 measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID644201 | Selectivity ratio of EC50 for P2/AT1 double knockout Trypanosoma brucei to EC50 for wild type Trypanosoma brucei | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinol derivatives as potential trypanocidal agents. |
AID1881383 | Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei B48 measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID1624259 | Resistance factor, ratio of EC50 for pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 to EC50 for wild type Trypanosoma brucei Lister 427 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID1679073 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as parasite growth inhibition incubated for 48 hrs by resazurin dye based assay | 2020 | RSC medicinal chemistry, Dec-17, Volume: 11, Issue:12 | Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness. |
AID1244568 | Resistant factor, ratio of EC50 for diminazene/pentamidine/melaminophenyl arsenicals-resistant Trypanosoma brucei brucei B48 to EC50 for wild type bloodstream form of Trypanosoma brucei brucei s427 trypomastigotes | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro. |
AID1881374 | Antitrypanosomal activity against bloodstream form of Trypanosoma congolense IL3000 measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID1312528 | Stabilization of c-MYC Pu27 G-quadruplex DNA (unknown origin) assessed as inhibition of Taq polymerase-mediated polymerization/extension of Pu27 and Pu27rev oligomers at 10 uM preincubated for 6 hrs followed by Taq polymerase addition by PCR stop assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID53471 | Compound was evaluated for 50% inhibitory dose against oncornaviral DNA polymerase activity of moloney murine leukemia virus | 1980 | Journal of medicinal chemistry, Jul, Volume: 23, Issue:7 | Diaryl amidine derivatives as oncornaviral DNA polymerase inhibitors. |
AID1312520 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability at 20 uM after 72 hrs by WST-1 assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1312553 | Selectivity ratio of Kd for 8-bp AT rich duplex DNA (unknown origin) to Kd for wild type Bcl2 27-mer G-quadruplex DNA (unknown origin) | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1543057 | Inhibition of pH 5.5-stimulated mouse ASIC2a homomer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS. |
AID1881381 | Resistance factor, ratio of EC50 for bloodstream form of diminazene-resistant Trypanosoma congolense EMS MUT DimR to EC50 for wild-type bloodstream form of Trypanosoma congolense | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID279550 | Antiproliferative activity against Leishmania donovani DI700 promastigotes in presence of 100 uM putrescine | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Leishmania donovani polyamine biosynthetic enzyme overproducers as tools to investigate the mode of action of cytotoxic polyamine analogs. |
AID372443 | Biphasic antitrypanosomal activity against Trypanosoma brucei brucei s427 by alamar blue fluorescent dye assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | 2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. |
AID55303 | Inhibitory concentration against DNA-bound ethidium for cytotoxicity | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID1624258 | Resistance factor, ratio of EC50 for Trypanosoma brucei TbAT1-KO to EC50 for wild type Trypanosoma brucei Lister 427 | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID225777 | Inhibitory concentration against ethidium in DNA-binding assay with [poly(dA-dT)]2 (synthetic oligonucleotide) | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID1124815 | Inhibition of mouse polyamine oxidase assessed as conversion of N-acetylspermine to N-acetylspermidine | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Some non-conventional biomolecular targets for diamidines. A short survey. |
AID279548 | Antiproliferative activity against Leishmania donovani DI700 promastigotes overproducing SPDSYN enzyme | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Leishmania donovani polyamine biosynthetic enzyme overproducers as tools to investigate the mode of action of cytotoxic polyamine analogs. |
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. |
AID565595 | Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.2 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID1312519 | Antiproliferative activity against human PC3 cells assessed as cell viability at 20 uM after 72 hrs by WST-1 assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1312550 | Binding affinity to wild type c-MYC 24-mer G-quadruplex DNA (unknown origin) by isothermal titration calorimetry | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID279549 | Antiproliferative activity against Leishmania donovani DI700 promastigotes overproducing ADOMETDC enzyme | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Leishmania donovani polyamine biosynthetic enzyme overproducers as tools to investigate the mode of action of cytotoxic polyamine analogs. |
AID215161 | Compound is evaluated for trypanocidal activity against Trypanosoma brucei, by exposing the parasites directly to compound prior to injection to mice at 10 e-7 M concentration in dark | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Identification of an acridine photoaffinity probe for trypanocidal action. |
AID628481 | Cytotoxicity against human HEK293 cells at 70 uM after 48 hrs by by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa. |
AID1297650 | Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms incubated for 48 hrs by alamar blue assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics. |
AID565594 | Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as complete cure from microbial infection at 0.2 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID644197 | Cytotoxicity against human MRC5 cells after 3 days by resazurin-based fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinol derivatives as potential trypanocidal agents. |
AID1688797 | Antitrypanosomal activity against drug resistant Trypanosoma brucei B48 assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
AID1881375 | Antitrypanosomal activity against Trypanosoma vivax STIB 719 by [3H]-hypoxanthine incorporation assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID1881382 | Antiparasitic activity against bloodstream form of tbat1-/- deficient Trypanosoma brucei brucei measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID466919 | Antitrypanosomal activity against multidrug-resistant Trypanosoma brucei brucei B48 after 48 hrs by alamar blue assay | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species. |
AID1312516 | Antiproliferative activity against human bone marrow cells after 72 hrs by WST-1 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID98558 | Concentration required to inhibit the cell growth by 50 % after 48 hr in L1210 leukemic cells. | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID1312552 | Selectivity ratio of Kd for 8-bp AT rich duplex DNA (unknown origin) to Kd for wild type c-MYC 24-mer G-quadruplex DNA (unknown origin) | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1244566 | Trypanocidal activity against wild type bloodstream form of Trypanosoma brucei brucei s427 trypomastigotes after 70 hrs by Alamar Blue assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro. |
AID215864 | In vitro activity against bloodstream from trypomastigotes. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7 | An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes. |
AID1182806 | Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 grown in Creek's minimal medium after 48 hrs by Alamar blue assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1. |
AID1431828 | Anti-parasitic activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 after 48 hrs by alamar blue based fluorescence assay | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion. |
AID1881391 | Antiparasitic activity against wild-type Trypanosoma brucei brucei measured after 48 hrs by alamar blue assay | 2021 | RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8 | Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype. |
AID565592 | Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 2 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12 | In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID1431843 | Trypanocidal activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 assessed as inhibition of respiration in presence of glycerol | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion. |
AID666704 | Antitrypanosomal activity against diminazene-, pentamidine-, and melaminophenyl arsenical-resistant HAPT1-deficient Trypanosoma brucei brucei B48 after 3 days 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. |
AID1624292 | Antitrypanosomal activity against Trypanosoma congolense by resazurin assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID1688799 | Antitrypanosomal activity against drug resistant Trypanosoma brucei ISMR1 assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents. |
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. |
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. |
AID1821418 | Trypanocidal activity against Trypanosoma brucei rhodesiense assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay | 2022 | Journal of natural products, 01-28, Volume: 85, Issue:1 | Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian |
AID54658 | Inhibitory concentration against ethidium in DNA-binding assay | 1995 | Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18 | Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity. |
AID1895619 | Inhibition of furin (unknown origin) using Pyr-RTKR-MCA as substrate incubated for 30 mins and measured by FRET assay | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Why All the Fury over Furin? |
AID1244567 | Trypanocidal activity against diminazene/pentamidine/melaminophenyl arsenicals-resistant bloodstream form of Trypanosoma brucei brucei B48 trypomastigotes after 70 hrs by Alamar Blue assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro. |
AID215154 | Trypanocidal activity against Trypanosoma brucei, exposure of parasites to compound prior to injection into mice at 10 e-5 M concentration in dark conditions | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | Identification of an acridine photoaffinity probe for trypanocidal action. |
AID1202926 | Antitrypanosomal activity against Trypanosoma brucei brucei B48 with nonfunctional high affinity pentamidine transporter assessed as cell viability after 48 hrs by alamar blue assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts. |
AID1312533 | Stabilization of c-MYC template Pu27-13,14 mutant DNA (unknown origin) assessed as inhibition of Taq polymerase-mediated polymerization/extension of Pu27-13,14 mutant and Pu27rev oligomers at 25 uM preincubated for 6 hrs followed by Taq polymerase additio | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID312629 | Antitrypanosomal activity against Trypanosoma brucei | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. |
AID628473 | Antitrypanosomal activity against Trypanosoma brucei brucei after 48 hrs by by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa. |
AID1312554 | Binding affinity to 8-bp AT rich duplex DNA (unknown origin) by isothermal titration calorimetry | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities. |
AID1808247 | Antitrypanosomal activity against bloodstream form trypomastigotes of wild type Trypanosoma brucei brucei Lister 427 assessed as reduction in parasite viability by resazurin-based assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure-Activity Relationship Studies. |
AID1624254 | Antitrypanosomal activity against wild type Trypanosoma brucei Lister 427 after 48 hrs by alamar blue assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. |
AID466917 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 48 hrs by alamar blue assay | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species. |
AID666701 | Antitrypanosomal activity against wild type Trypanosoma brucei brucei Lister 427 after 3 days 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. |
AID644199 | Antitrypanosomal activity against P2/AT1 double knockout Trypanosoma brucei after 3 days by resazurin-based fluorescence assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Quinol derivatives as potential trypanocidal agents. |
AID1202927 | Resistance factor, ratio of EC50 for Trypanosoma brucei brucei B48 to EC50 for wild type Trypanosoma brucei brucei s427 trypomastigotes | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2 | SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 195 (26.35) | 18.7374 |
1990's | 187 (25.27) | 18.2507 |
2000's | 99 (13.38) | 29.6817 |
2010's | 197 (26.62) | 24.3611 |
2020's | 62 (8.38) | 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 (55.63) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 24 (3.17%) | 5.53% |
Reviews | 22 (2.90%) | 6.00% |
Case Studies | 11 (1.45%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 701 (92.48%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |