Page last updated: 2024-11-04

diminazene

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Diminazene: An effective trypanocidal agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

diminazene : A triazene derivative that is triazene in which each of the terminal nitrogens is substituted by a 4-carbamimidoylphenyl group. [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]

Cross-References

ID SourceID
PubMed CID2354
CHEMBL ID35241
CHEBI ID81724
SCHEMBL ID120719
MeSH IDM0006470

Synonyms (53)

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

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"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

Effects

ExcerptReferenceRelevance
"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

Treatment

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.

ExcerptReferenceRelevance
"Diminazene aceturate treatment did not induce arrhythmic events in normal, as well as in hyperglycaemic animals."( Activation of angiotensin-converting enzyme 2 improves cardiac electrical changes in ventricular repolarization in streptozotocin-induced hyperglycaemic rats.
Coutinho, DC; Ferreira, AJ; Medei, E; Monnerat-Cahli, G, 2014
)
1.12
"Diminazene aceturate treatment (15 mg/kg/day) activated ACE2, increased the circulating Ang (1-7) level, and augmented EDR and FMD in db/db mouse arteries."( 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
)
1.14
"Diminazene treatment did not change the lesion size, but ameliorated the composition of aortic root and low SS-induced carotid plaques by increasing collagen content and decreasing both MMP-9 expression and macrophage infiltration."( Diminazene enhances stability of atherosclerotic plaques in ApoE-deficient mice.
Bragina, ME; Caffa, I; Costa-Fraga, FP; da Silva, RF; Fraga-Silva, RA; Mach, F; Montecucco, F; Nencioni, A; Raizada, MK; Santos, RAS; Stergiopulos, N, 2015
)
2.58
"Pretreatment with diminazene aceturate, a small molecule with ability to inhibit acid detection through blockade of the acid-sensing ion channel (ASIC) at the doses provided, did not prevent acid-induced pathologic mucus or transport defects but did mitigate airway obstruction."( Acid exposure disrupts mucus secretion and impairs mucociliary transport in neonatal piglet airways.
Atanasova, KR; Bravo, L; Collins, EN; Dadural, JS; Eken, E; Guevara, MV; Kuan, SP; Liao, YSJ; Reznikov, LR; Schurmann, V; Sponchiado, M; Vogt, K, 2020
)
0.88
"Treatment with diminazene significantly inhibited the expression of casein kinase and lactate dehydrogenase, and reduced infarct size in AMI rats."( Protective effect of diminazene attenuates myocardial infarction in rats via increased inflammation and ACE2 activity.
Chen, J; Cui, L; Liu, Q; Ma, R; Sang, H; Shan, L; Yuan, J; Zhang, S, 2017
)
1.11
"Treatment with diminazene aceturate reversed the reproductive abnormalities caused by the parasite."( Effects of Trypanosoma brucei infection and diminazene aceturate therapy on testicular morphology and function of Nigerian local dogs.
Ezeh, IO; Ezeokonkwo, RC; Idika, IK; Iheagwam, CN; Obi, CF; Obidike, RI; Omoja, VU, 2013
)
0.99
"The treatment with diminazene aceturate had an efficacy of 85.7%."( Diminazene aceturate in the control of Trypanosoma evansi infection in cats.
Costa, MM; Da Silva, AS; Garcia, HA; Lopes, ST; Monteiro, SG; Santurio, JM; Teixeira, MM; Wolkmer, P; Zanette, RA, 2009
)
2.11

Toxicity

ExcerptReferenceRelevance
" Additionally, cats were monitored for adverse drug reactions by daily observation and examination."( 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
)
0.64
"The aims of this study were to develop nerolidol-loaded nanospheres, and to evaluate their efficacy in vitro and in vivo against Trypanosoma evansi, as well as to determine their physicochemical properties, morphology, and any possible side effect in vitro against peripheral blood mononuclear cell (PBMC)."( Nerolidol nanospheres increases its trypanocidal efficacy against Trypanosoma evansi: New approach against diminazene aceturate resistance and toxicity.
Baldissera, MD; Cossetin, LF; da Silva, AP; Da Silva, AS; Dalla Lana, DF; Grando, TH; Monteiro, SG; Nascimento, K; Sagrillo, MR; Souza, CF; Stefani, LM, 2016
)
0.65
"The nucleoside antibiotic tubercidin displays strong activity against different target organisms, but it is notoriously toxic to mammalian cells."( Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
Caljon, G; Campagnaro, GD; de Koning, HP; Hulpia, F; Maes, L; Scortichini, M; Van Calenbergh, S; Van Hecke, K, 2019
)
0.51
" Following randomised trypanocidal treatment (diminazene diaceturate, melarsomine dihydrochloride or isometamidium chloride), animals were observed for immediate adverse drug reactions and follow-up assessment was performed at 1 and 2 weeks."( Safety and efficacy of three trypanocides in confirmed field cases of trypanosomiasis in working equines in The Gambia: a prospective, randomised, non-inferiority trial.
Jallow, S; Raftery, AG; Rodgers, J; Sutton, DGM, 2019
)
0.77
" However, DA has been reported to have toxic side effects that limit its application."( Cytotoxicity and anti-inflammatory effect of a novel diminazene aceturate derivative in bovine mammary epithelial cells.
Jia, F; Li, X; Ma, W; Zhang, X; Zhou, X, 2021
)
0.87

Pharmacokinetics

The pharmacokinetic aspects of diminazene aceturate were studied in lactating goats and sheep after single intravenous and intramuscular administrations.

ExcerptReferenceRelevance
" 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

Compound-Compound Interactions

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.

ExcerptReferenceRelevance
"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

Bioavailability

ExcerptReferenceRelevance
" 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

Dosage Studied

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.

ExcerptRelevanceReference
" 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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antiparasitic agentA substance used to treat or prevent parasitic infections.
trypanocidal drugA 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]

Drug Classes (2)

ClassDescription
triazene derivativeA nitrogen molecular entity resulting from the formal substitution of one or more of the hydrogens of triazene.
carboxamidineCompounds 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 Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin BHomo sapiens (human)IC50 (µMol)30.00000.00021.845310.0000AID312631
FurinHomo sapiens (human)Ki5.42000.00421.25445.4200AID1895619
Amiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)Ki0.01300.01300.15150.2900AID1124814
Diamine acetyltransferase 1Homo sapiens (human)Ki2.40002.00002.20002.4000AID1124816
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
proteolysisCathepsin BHomo sapiens (human)
thyroid hormone generationCathepsin BHomo sapiens (human)
collagen catabolic processCathepsin BHomo sapiens (human)
epithelial cell differentiationCathepsin BHomo sapiens (human)
regulation of apoptotic processCathepsin BHomo sapiens (human)
decidualizationCathepsin BHomo sapiens (human)
symbiont entry into host cellCathepsin BHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin BHomo sapiens (human)
cellular response to thyroid hormone stimulusCathepsin BHomo sapiens (human)
negative regulation of nerve growth factor productionFurinHomo sapiens (human)
viral translationFurinHomo sapiens (human)
protein processingFurinHomo sapiens (human)
blastocyst formationFurinHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusFurinHomo sapiens (human)
signal peptide processingFurinHomo sapiens (human)
transforming growth factor beta receptor signaling pathwayFurinHomo sapiens (human)
regulation of signal transductionFurinHomo sapiens (human)
protein processingFurinHomo sapiens (human)
peptide hormone processingFurinHomo sapiens (human)
viral life cycleFurinHomo sapiens (human)
viral protein processingFurinHomo sapiens (human)
extracellular matrix disassemblyFurinHomo sapiens (human)
extracellular matrix organizationFurinHomo sapiens (human)
collagen catabolic processFurinHomo sapiens (human)
zymogen activationFurinHomo sapiens (human)
regulation of cholesterol transportFurinHomo sapiens (human)
negative regulation of low-density lipoprotein particle receptor catabolic processFurinHomo sapiens (human)
nerve growth factor productionFurinHomo sapiens (human)
negative regulation of transforming growth factor beta1 productionFurinHomo sapiens (human)
secretion by cellFurinHomo sapiens (human)
plasma lipoprotein particle remodelingFurinHomo sapiens (human)
regulation of protein catabolic processFurinHomo sapiens (human)
peptide biosynthetic processFurinHomo sapiens (human)
positive regulation of viral entry into host cellFurinHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisFurinHomo sapiens (human)
protein maturationFurinHomo sapiens (human)
regulation of endopeptidase activityFurinHomo sapiens (human)
dibasic protein processingFurinHomo sapiens (human)
cytokine precursor processingFurinHomo sapiens (human)
amyloid fibril formationFurinHomo sapiens (human)
putrescine metabolic processAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
response to antibioticAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
amine metabolic processAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
angiogenesisDiamine acetyltransferase 1Homo sapiens (human)
polyamine biosynthetic processDiamine acetyltransferase 1Homo sapiens (human)
putrescine catabolic processDiamine acetyltransferase 1Homo sapiens (human)
spermidine acetylationDiamine acetyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin BHomo sapiens (human)
protein bindingCathepsin BHomo sapiens (human)
collagen bindingCathepsin BHomo sapiens (human)
peptidase activityCathepsin BHomo sapiens (human)
cysteine-type peptidase activityCathepsin BHomo sapiens (human)
proteoglycan bindingCathepsin BHomo sapiens (human)
protease bindingFurinHomo sapiens (human)
endopeptidase activityFurinHomo sapiens (human)
serine-type endopeptidase activityFurinHomo sapiens (human)
serine-type endopeptidase inhibitor activityFurinHomo sapiens (human)
protein bindingFurinHomo sapiens (human)
heparin bindingFurinHomo sapiens (human)
peptidase activityFurinHomo sapiens (human)
serine-type peptidase activityFurinHomo sapiens (human)
peptide bindingFurinHomo sapiens (human)
metal ion bindingFurinHomo sapiens (human)
nerve growth factor bindingFurinHomo sapiens (human)
heparan sulfate bindingFurinHomo sapiens (human)
copper ion bindingAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
calcium ion bindingAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
protein bindingAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
primary amine oxidase activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
heparin bindingAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
protein homodimerization activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
quinone bindingAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
putrescine oxidase activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
diamine oxidase activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
histamine oxidase activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
methylputrescine oxidase activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
propane-1,3-diamine oxidase activityAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
diamine N-acetyltransferase activityDiamine acetyltransferase 1Homo sapiens (human)
protein bindingDiamine acetyltransferase 1Homo sapiens (human)
N-acetyltransferase activityDiamine acetyltransferase 1Homo sapiens (human)
identical protein bindingDiamine acetyltransferase 1Homo sapiens (human)
spermidine bindingDiamine acetyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular regionCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
external side of plasma membraneCathepsin BHomo sapiens (human)
apical plasma membraneCathepsin BHomo sapiens (human)
endolysosome lumenCathepsin BHomo sapiens (human)
melanosomeCathepsin BHomo sapiens (human)
perinuclear region of cytoplasmCathepsin BHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular exosomeCathepsin BHomo sapiens (human)
peptidase inhibitor complexCathepsin BHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
extracellular spaceFurinHomo sapiens (human)
Golgi membraneFurinHomo sapiens (human)
extracellular regionFurinHomo sapiens (human)
endoplasmic reticulumFurinHomo sapiens (human)
Golgi lumenFurinHomo sapiens (human)
trans-Golgi networkFurinHomo sapiens (human)
plasma membraneFurinHomo sapiens (human)
cell surfaceFurinHomo sapiens (human)
endosome membraneFurinHomo sapiens (human)
membraneFurinHomo sapiens (human)
trans-Golgi network transport vesicleFurinHomo sapiens (human)
membrane raftFurinHomo sapiens (human)
extracellular exosomeFurinHomo sapiens (human)
Golgi membraneFurinHomo sapiens (human)
trans-Golgi networkFurinHomo sapiens (human)
extracellular spaceAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
extracellular regionAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
extracellular spaceAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
peroxisomeAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
plasma membraneAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
bicellular tight junctionAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
specific granule lumenAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
extracellular exosomeAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
plasma membraneAmiloride-sensitive amine oxidase [copper-containing]Homo sapiens (human)
cytosolDiamine acetyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (144)

Assay IDTitleYearJournalArticle
AID1881385Resistance factor, ratio of EC50 for bloodstream form of Trypanosoma brucei brucei B48 to EC50 for wild-type bloodstream form of Trypanosoma brucei brucei2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID666705Resistance 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 4272012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
AID1124807Inhibition 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 assay2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Some non-conventional biomolecular targets for diamidines. A short survey.
AID1312508Binding 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 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID466923Antitrypanosomal activity against Trypanosoma evansi ITMAV170475 after 48 hrs by alamar blue assay2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species.
AID336011Displacement of ethidium bromide from calf thymus type 1 DNA after 24 hrs by microtiter assay1992Journal of natural products, Nov, Volume: 55, Issue:11
A colorimetric microassay for the detection of agents that interact with DNA.
AID1688798Resistance factor, ratio of EC50 for antitrypanosomal activity against drug resistant Trypanosoma brucei B48 to antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream form2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID489462Cytotoxicity against HEK239 cells after 72 hrs by Alamar blue assay2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
7',8'-Dihydroobolactone, a typanocidal alpha-pyrone from the rainforest tree Cryptocarya obovata.
AID1688794Antitrypanosomal 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 assay2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID1394622Anti-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 assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition 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.
AID1312513Antiproliferative activity against human OVCAR3 cells after 72 hrs by WST-1 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID565591Antimicrobial 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 days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID1821420Trypanocidal activity against Trypanosoma evansi assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay2022Journal of natural products, 01-28, Volume: 85, Issue:1
Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian
AID1543056Inhibition of pH 6.6-stimulated mouse ASIC1a homomer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay2019ACS 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.
AID1624255Antitrypanosomal activity against Trypanosoma brucei TbAT1-KO after 48 hrs by alamar blue assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1688795Antitrypanosomal activity against drug resistant Trypanosoma brucei harboring TbAT1 deficient assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID152454Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 10 ug/mL1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
AID1688796Resistance 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 form2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID1431830Anti-parasitic activity against bloodstream form of Trypanosoma congolense IL3000 after 48 hrs by alamar blue based fluorescence assay2017Journal 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.
AID644198Antitrypanosomal activity against wild type Trypanosoma brucei after 3 days by resazurin-based fluorescence assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinol derivatives as potential trypanocidal agents.
AID279551Antiproliferative activity against Leishmania donovani DI700 promastigotes in presence of 100 uM spermidine2007Antimicrobial 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.
AID1431829Anti-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 assay2017Journal 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.
AID1821411Trypanocidal activity against Trypanosoma brucei brucei GUTat3.1 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay2022Journal of natural products, 01-28, Volume: 85, Issue:1
Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian
AID1679081Selectivity index, ratio of IC50 for human HEK293 cells to IC50 for antitrypanosomal activity against Trypanosoma brucei brucei 4272020RSC medicinal chemistry, Dec-17, Volume: 11, Issue:12
Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness.
AID1881380Resistance factor, ratio of EC50 for bloodstream form of diminazene-resistant Trypanosoma congolense DimR to EC50 for bloodstream form of wild-type Trypanosoma congolense2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID279546Antiproliferative activity against Leishmania donovani DI700 promastigotes2007Antimicrobial 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.
AID1881378Antitrypanosomal activity against bloodstream form of diminazene-resistant Trypanosoma congolense DimR measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID279547Antiproliferative activity against Leishmania donovani DI700 promastigotes overproducing ODC enzyme2007Antimicrobial 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.
AID1543058Inhibition of pH 6.25-stimulated mouse ASIC1a/2a heterodimer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay2019ACS 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.
AID1124816Inhibition of human SSAT using spermidine as substrate2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Some non-conventional biomolecular targets for diamidines. A short survey.
AID1394624Resistance 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 4272018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition 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.
AID1821417Trypanocidal activity against Trypanosoma brucei rhodesiense IL1501 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay2022Journal of natural products, 01-28, Volume: 85, Issue:1
Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian
AID1182805Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 grown in HMI-9 medium after 48 hrs by Alamar blue assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1.
AID666703Resistance 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 4272012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
AID1808246Antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei brucei B48 assessed as reduction in parasite viability by resazurin-based assay2022ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure-Activity Relationship Studies.
AID1394621Anti-parasitic activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 after 48 hrs by resazurin-based assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition 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.
AID1624257Antitrypanosomal activity against isometamidium resistant Trypanosoma brucei ISMR1 after 48 hrs by alamar blue assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID466918Antitrypanosomal activity against diminazene-resistant Trypanosoma brucei brucei deltaTbat1-KO after 48 hrs by alamar blue assay2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species.
AID1624256Antitrypanosomal activity against pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 after 48 hrs by alamar blue assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1124814Mixed type inhibition of recombinant human DAO expressed in drosophila S2 cells2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Some non-conventional biomolecular targets for diamidines. A short survey.
AID478755Binding affinity to d(CGCGATATCGCG)2 dodecamer assessed as change in melting temperature2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Theoretical models of pentamidine analogs activity based on their DNA minor groove complexes.
AID152455Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 1 ug/mL1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
AID565593Antimicrobial 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 days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID312631Inhibition of human liver cathepsin B2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
AID1312517Antiproliferative activity against human MCR5A cells after 72 hrs by WST-1 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1202924Antitrypanosomal activity against AT1 knock out Trypanosoma brucei brucei assessed as cell viability after 48 hrs by alamar blue assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts.
AID1431844Resistant 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 bruc2017Journal 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.
AID441755Antitrypanosomal 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 me2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.
AID1394629Anti-parasitic activity against bloodstream trypomastigote stage of pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 after 48 hrs by resazurin-based assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition 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.
AID336010Displacement of methyl green from DNA after 24 hrs by microtiter assay1992Journal of natural products, Nov, Volume: 55, Issue:11
A colorimetric microassay for the detection of agents that interact with DNA.
AID395133Binding affinity to poly(dA).poly(dT) duplex DNA assessed as ratio of KA to KB by ESI-MS analysis2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?
AID1312512Binding 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 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1312551Binding affinity to wild type Bcl2 27-mer G-quadruplex DNA (unknown origin) by isothermal titration calorimetry2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1394632Resistance 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 4272018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition 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.
AID1202925Resistance factor, ratio of EC50 for AT1 knock out Trypanosoma brucei brucei to EC50 for wild type Trypanosoma brucei brucei s427 trypomastigotes2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts.
AID1202923Antitrypanosomal activity against wild type Trypanosoma brucei brucei s427 trypomastigotes assessed as cell viability after 48 hrs by alamar blue assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts.
AID215159Trypanocidal activity against Trypanosoma brucei, exposure of parasites to compound prior to injection into mice at 10 e-6 M concentration in dark conditions1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Identification of an acridine photoaffinity probe for trypanocidal action.
AID1312509Binding 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 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1881379Antitrypanosomal activity against bloodstream form of diminazene-resistant Trypanosoma congolense EMS MUT DimR measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID1821419Trypanocidal activity against Trypanosoma brucei congolense IL3000 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay2022Journal of natural products, 01-28, Volume: 85, Issue:1
Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian
AID1808248Resistance 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 4272022ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure-Activity Relationship Studies.
AID1394623Anti-parasitic activity against bloodstream form of Trypanosoma congolense IL3000 after 48 hrs by resazurin-based assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Inhibition 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.
AID1881392Antitrypanosomal activity against bloodstream form of Trypanosoma congolense measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID1312511Binding 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 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1312534Stabilization 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 PC2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1688800Resistance factor, ratio of EC50 for antitrypanosomal activity against drug resistant Trypanosoma brucei ISMR1 to antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream form2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID489459Antitrypanosomal activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
7',8'-Dihydroobolactone, a typanocidal alpha-pyrone from the rainforest tree Cryptocarya obovata.
AID1312510Binding 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 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1624260Resistance factor, ratio of EC50 for isometamidium resistant Trypanosoma brucei B48 to EC50 for wild type Trypanosoma brucei Lister 4272019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1821416Trypanocidal activity against Trypanosoma brucei gambiense IL1922 assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay2022Journal of natural products, 01-28, Volume: 85, Issue:1
Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian
AID152453Inhibitory activity against adenosine uptake through P2 adenosine transporter of blood stream Trypanosoma brucei trypomastigotes at the concentration 100 ug/mL1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
AID225778Inhibitory concentration against ethidium in DNA-binding assay with [poly(dG-dC)]2 (synthetic oligonucleotide)1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID54990Change in DNA-melting (deltaTm) with calf thymus DNA at pH 7.01995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID1881384Resistance factor, ratio of EC50 for bloodstream form of tbat1-/- deficient Trypanosoma brucei brucei to EC50 for wild-type bloodstream form of Trypanosoma brucei brucei2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID666702Antitrypanosomal activity against diminazene aceturate-resistant TbAT1 gene-deficient Trypanosoma brucei brucei AT1-KO after 3 days by alamar blue assay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
AID396382Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Pharmacophore based discovery of potential antimalarial agent targeting haem detoxification pathway.
AID552699Antitrypanosomal 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 infection2011Bioorganic & 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.
AID54988Change in DNA-melting (deltaTm) with calf thymus DNA at pH 65.01995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID1881372Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei Lister 427 measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID644201Selectivity ratio of EC50 for P2/AT1 double knockout Trypanosoma brucei to EC50 for wild type Trypanosoma brucei2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinol derivatives as potential trypanocidal agents.
AID1881383Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei B48 measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID1624259Resistance factor, ratio of EC50 for pentamidine/diminazene/melaminophenyl arsenical resistant Trypanosoma brucei B48 to EC50 for wild type Trypanosoma brucei Lister 4272019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1679073Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as parasite growth inhibition incubated for 48 hrs by resazurin dye based assay2020RSC medicinal chemistry, Dec-17, Volume: 11, Issue:12
Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness.
AID1244568Resistant 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 trypomastigotes2015European journal of medicinal chemistry, Aug-28, Volume: 101Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro.
AID1881374Antitrypanosomal activity against bloodstream form of Trypanosoma congolense IL3000 measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID1312528Stabilization 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 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID53471Compound was evaluated for 50% inhibitory dose against oncornaviral DNA polymerase activity of moloney murine leukemia virus1980Journal of medicinal chemistry, Jul, Volume: 23, Issue:7
Diaryl amidine derivatives as oncornaviral DNA polymerase inhibitors.
AID1312520Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability at 20 uM after 72 hrs by WST-1 assay relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1312553Selectivity 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)2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1543057Inhibition of pH 5.5-stimulated mouse ASIC2a homomer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay2019ACS 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.
AID1881381Resistance factor, ratio of EC50 for bloodstream form of diminazene-resistant Trypanosoma congolense EMS MUT DimR to EC50 for wild-type bloodstream form of Trypanosoma congolense2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID279550Antiproliferative activity against Leishmania donovani DI700 promastigotes in presence of 100 uM putrescine2007Antimicrobial 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.
AID372443Biphasic antitrypanosomal activity against Trypanosoma brucei brucei s427 by alamar blue fluorescent dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID55303Inhibitory concentration against DNA-bound ethidium for cytotoxicity1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID1624258Resistance factor, ratio of EC50 for Trypanosoma brucei TbAT1-KO to EC50 for wild type Trypanosoma brucei Lister 4272019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID225777Inhibitory concentration against ethidium in DNA-binding assay with [poly(dA-dT)]2 (synthetic oligonucleotide)1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID1124815Inhibition of mouse polyamine oxidase assessed as conversion of N-acetylspermine to N-acetylspermidine2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Some non-conventional biomolecular targets for diamidines. A short survey.
AID279548Antiproliferative activity against Leishmania donovani DI700 promastigotes overproducing SPDSYN enzyme2007Antimicrobial 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.
AID552695Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay2011Bioorganic & 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.
AID565595Antimicrobial 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 days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID1312519Antiproliferative activity against human PC3 cells assessed as cell viability at 20 uM after 72 hrs by WST-1 assay relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1312550Binding affinity to wild type c-MYC 24-mer G-quadruplex DNA (unknown origin) by isothermal titration calorimetry2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID279549Antiproliferative activity against Leishmania donovani DI700 promastigotes overproducing ADOMETDC enzyme2007Antimicrobial 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.
AID215161Compound 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 dark1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Identification of an acridine photoaffinity probe for trypanocidal action.
AID628481Cytotoxicity against human HEK293 cells at 70 uM after 48 hrs by by alamar blue assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa.
AID1297650Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms incubated for 48 hrs by alamar blue assay2016European journal of medicinal chemistry, Jun-30, Volume: 116An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics.
AID565594Antimicrobial 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 days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID644197Cytotoxicity against human MRC5 cells after 3 days by resazurin-based fluorescence assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinol derivatives as potential trypanocidal agents.
AID1688797Antitrypanosomal activity against drug resistant Trypanosoma brucei B48 assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID1881375Antitrypanosomal activity against Trypanosoma vivax STIB 719 by [3H]-hypoxanthine incorporation assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID1881382Antiparasitic activity against bloodstream form of tbat1-/- deficient Trypanosoma brucei brucei measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID466919Antitrypanosomal activity against multidrug-resistant Trypanosoma brucei brucei B48 after 48 hrs by alamar blue assay2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species.
AID1312516Antiproliferative activity against human bone marrow cells after 72 hrs by WST-1 assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID98558Concentration required to inhibit the cell growth by 50 % after 48 hr in L1210 leukemic cells.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID1312552Selectivity 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)2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1244566Trypanocidal activity against wild type bloodstream form of Trypanosoma brucei brucei s427 trypomastigotes after 70 hrs by Alamar Blue assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro.
AID215864In vitro activity against bloodstream from trypomastigotes.1998Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
An approach to use an unusual adenosine transporter to selectively deliver polyamine analogues to trypanosomes.
AID1182806Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 grown in Creek's minimal medium after 48 hrs by Alamar blue assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1.
AID1431828Anti-parasitic activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 after 48 hrs by alamar blue based fluorescence assay2017Journal 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.
AID1881391Antiparasitic activity against wild-type Trypanosoma brucei brucei measured after 48 hrs by alamar blue assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Truncated S-MGBs: towards a parasite-specific and low aggregation chemotype.
AID565592Antimicrobial 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 days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID1431843Trypanocidal activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 assessed as inhibition of respiration in presence of glycerol2017Journal 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.
AID666704Antitrypanosomal activity against diminazene-, pentamidine-, and melaminophenyl arsenical-resistant HAPT1-deficient Trypanosoma brucei brucei B48 after 3 days by alamar blue assay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
AID1624292Antitrypanosomal activity against Trypanosoma congolense by resazurin assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1688799Antitrypanosomal activity against drug resistant Trypanosoma brucei ISMR1 assessed as reduction in parasite viability incubated for 48 hrs by resazurin dye based fluorescence assay2020European journal of medicinal chemistry, Feb-15, Volume: 188C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents.
AID552696Antitrypanosomal activity against bloodstream form of Trypanosoma brucei s427 after 72 hrs by MTT assay2011Bioorganic & 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.
AID644196Antitrypanosomal activity against blood stream form of Trypanosoma brucei after 69 hrs by resazurin-based fluorescence assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinol derivatives as potential trypanocidal agents.
AID1821418Trypanocidal activity against Trypanosoma brucei rhodesiense assessed as parasite growth inhibition incubated for 3 days by Celltiter-Glo luminescence assay2022Journal of natural products, 01-28, Volume: 85, Issue:1
Benzophenone Glucosides and B-Type Proanthocyanidin Dimers from Zambian
AID54658Inhibitory concentration against ethidium in DNA-binding assay1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Novel acridine-triazenes as prototype combilexins: synthesis, DNA binding, and biological activity.
AID1895619Inhibition of furin (unknown origin) using Pyr-RTKR-MCA as substrate incubated for 30 mins and measured by FRET assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Why All the Fury over Furin?
AID1244567Trypanocidal activity against diminazene/pentamidine/melaminophenyl arsenicals-resistant bloodstream form of Trypanosoma brucei brucei B48 trypomastigotes after 70 hrs by Alamar Blue assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro.
AID215154Trypanocidal activity against Trypanosoma brucei, exposure of parasites to compound prior to injection into mice at 10 e-5 M concentration in dark conditions1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Identification of an acridine photoaffinity probe for trypanocidal action.
AID1202926Antitrypanosomal activity against Trypanosoma brucei brucei B48 with nonfunctional high affinity pentamidine transporter assessed as cell viability after 48 hrs by alamar blue assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts.
AID1312533Stabilization 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 additio2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID312629Antitrypanosomal activity against Trypanosoma brucei2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
AID628473Antitrypanosomal activity against Trypanosoma brucei brucei after 48 hrs by by alamar blue assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Convolutamines I and J, antitrypanosomal alkaloids from the bryozoan Amathia tortusa.
AID1312554Binding affinity to 8-bp AT rich duplex DNA (unknown origin) by isothermal titration calorimetry2016European journal of medicinal chemistry, Aug-08, Volume: 118Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.
AID1808247Antitrypanosomal activity against bloodstream form trypomastigotes of wild type Trypanosoma brucei brucei Lister 427 assessed as reduction in parasite viability by resazurin-based assay2022ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2
Imidazoline- and Benzamidine-Based Trypanosome Alternative Oxidase Inhibitors: Synthesis and Structure-Activity Relationship Studies.
AID1624254Antitrypanosomal activity against wild type Trypanosoma brucei Lister 427 after 48 hrs by alamar blue assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID466917Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 48 hrs by alamar blue assay2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species.
AID666701Antitrypanosomal activity against wild type Trypanosoma brucei brucei Lister 427 after 3 days by alamar blue assay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
AID644199Antitrypanosomal activity against P2/AT1 double knockout Trypanosoma brucei after 3 days by resazurin-based fluorescence assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinol derivatives as potential trypanocidal agents.
AID1202927Resistance factor, ratio of EC50 for Trypanosoma brucei brucei B48 to EC50 for wild type Trypanosoma brucei brucei s427 trypomastigotes2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts.
AID552697Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay2011Bioorganic & 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]

Research

Studies (740)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990195 (26.35)18.7374
1990's187 (25.27)18.2507
2000's99 (13.38)29.6817
2010's197 (26.62)24.3611
2020's62 (8.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 55.63

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.

MetricThis Compound (vs All)
Research Demand Index55.63 (24.57)
Research Supply Index6.66 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index93.03 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (55.63)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials24 (3.17%)5.53%
Reviews22 (2.90%)6.00%
Case Studies11 (1.45%)4.05%
Observational0 (0.00%)0.25%
Other701 (92.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]