diminazene profile

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]

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

Excerpt	Reference
"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."	( Gründer, S; Joussen, S; Rossetti, G; Schmidt, A, 2017)
"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."	( Birkenheuer, AJ; Cohn, LA; Lewis, KM; Marr, HS, 2014)
"Diminazene aceturate is a commonly used antibabesial agent. "	( Joubert, KE; Kettner, F; Lobetti, RG; Miller, DM, 2003)

Excerpt	Reference
"Diminazene aceturate has remained a very important therapeutic drug for trypanosomosis in cattle, sheep and goats since its introduction into the market in 1955. "	( Karanja, WM; Mdachi, RE; Murilla, GA, 2002)

Excerpt	Reference
"Diminazene aceturate treatment did not induce arrhythmic events in normal, as well as in hyperglycaemic animals."	( Coutinho, DC; Ferreira, AJ; Medei, E; Monnerat-Cahli, G, 2014)
"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."	( 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)
"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."	( 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)
"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."	( 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)
"Treatment with diminazene significantly inhibited the expression of casein kinase and lactate dehydrogenase, and reduced infarct size in AMI rats."	( Chen, J; Cui, L; Liu, Q; Ma, R; Sang, H; Shan, L; Yuan, J; Zhang, S, 2017)
"Treatment with diminazene aceturate reversed the reproductive abnormalities caused by the parasite."	( Ezeh, IO; Ezeokonkwo, RC; Idika, IK; Iheagwam, CN; Obi, CF; Obidike, RI; Omoja, VU, 2013)
"The treatment with diminazene aceturate had an efficacy of 85.7%."	( Costa, MM; Da Silva, AS; Garcia, HA; Lopes, ST; Monteiro, SG; Santurio, JM; Teixeira, MM; Wolkmer, P; Zanette, RA, 2009)

Role	Description
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
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]

Process	via Protein(s)	Taxonomy
proteolysis	Cathepsin B	Homo sapiens (human)
thyroid hormone generation	Cathepsin B	Homo sapiens (human)
collagen catabolic process	Cathepsin B	Homo sapiens (human)
epithelial cell differentiation	Cathepsin B	Homo sapiens (human)
regulation of apoptotic process	Cathepsin B	Homo sapiens (human)
decidualization	Cathepsin B	Homo sapiens (human)
symbiont entry into host cell	Cathepsin B	Homo sapiens (human)
proteolysis involved in protein catabolic process	Cathepsin B	Homo sapiens (human)
cellular response to thyroid hormone stimulus	Cathepsin B	Homo sapiens (human)
negative regulation of nerve growth factor production	Furin	Homo sapiens (human)
viral translation	Furin	Homo sapiens (human)
protein processing	Furin	Homo sapiens (human)
blastocyst formation	Furin	Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulus	Furin	Homo sapiens (human)
signal peptide processing	Furin	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Furin	Homo sapiens (human)
regulation of signal transduction	Furin	Homo sapiens (human)
protein processing	Furin	Homo sapiens (human)
peptide hormone processing	Furin	Homo sapiens (human)
viral life cycle	Furin	Homo sapiens (human)
viral protein processing	Furin	Homo sapiens (human)
extracellular matrix disassembly	Furin	Homo sapiens (human)
extracellular matrix organization	Furin	Homo sapiens (human)
collagen catabolic process	Furin	Homo sapiens (human)
zymogen activation	Furin	Homo sapiens (human)
regulation of cholesterol transport	Furin	Homo sapiens (human)
negative regulation of low-density lipoprotein particle receptor catabolic process	Furin	Homo sapiens (human)
nerve growth factor production	Furin	Homo sapiens (human)
negative regulation of transforming growth factor beta1 production	Furin	Homo sapiens (human)
secretion by cell	Furin	Homo sapiens (human)
plasma lipoprotein particle remodeling	Furin	Homo sapiens (human)
regulation of protein catabolic process	Furin	Homo sapiens (human)
peptide biosynthetic process	Furin	Homo sapiens (human)
positive regulation of viral entry into host cell	Furin	Homo sapiens (human)
positive regulation of membrane protein ectodomain proteolysis	Furin	Homo sapiens (human)
protein maturation	Furin	Homo sapiens (human)
regulation of endopeptidase activity	Furin	Homo sapiens (human)
dibasic protein processing	Furin	Homo sapiens (human)
cytokine precursor processing	Furin	Homo sapiens (human)
amyloid fibril formation	Furin	Homo sapiens (human)
putrescine metabolic process	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
response to antibiotic	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
amine metabolic process	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
angiogenesis	Diamine acetyltransferase 1	Homo sapiens (human)
polyamine biosynthetic process	Diamine acetyltransferase 1	Homo sapiens (human)
putrescine catabolic process	Diamine acetyltransferase 1	Homo sapiens (human)
spermidine acetylation	Diamine acetyltransferase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cysteine-type endopeptidase activity	Cathepsin B	Homo sapiens (human)
protein binding	Cathepsin B	Homo sapiens (human)
collagen binding	Cathepsin B	Homo sapiens (human)
peptidase activity	Cathepsin B	Homo sapiens (human)
cysteine-type peptidase activity	Cathepsin B	Homo sapiens (human)
proteoglycan binding	Cathepsin B	Homo sapiens (human)
protease binding	Furin	Homo sapiens (human)
endopeptidase activity	Furin	Homo sapiens (human)
serine-type endopeptidase activity	Furin	Homo sapiens (human)
serine-type endopeptidase inhibitor activity	Furin	Homo sapiens (human)
protein binding	Furin	Homo sapiens (human)
heparin binding	Furin	Homo sapiens (human)
peptidase activity	Furin	Homo sapiens (human)
serine-type peptidase activity	Furin	Homo sapiens (human)
peptide binding	Furin	Homo sapiens (human)
metal ion binding	Furin	Homo sapiens (human)
nerve growth factor binding	Furin	Homo sapiens (human)
heparan sulfate binding	Furin	Homo sapiens (human)
copper ion binding	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
calcium ion binding	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
protein binding	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
primary amine oxidase activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
heparin binding	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
protein homodimerization activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
quinone binding	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
putrescine oxidase activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
diamine oxidase activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
histamine oxidase activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
methylputrescine oxidase activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
propane-1,3-diamine oxidase activity	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
diamine N-acetyltransferase activity	Diamine acetyltransferase 1	Homo sapiens (human)
protein binding	Diamine acetyltransferase 1	Homo sapiens (human)
N-acetyltransferase activity	Diamine acetyltransferase 1	Homo sapiens (human)
identical protein binding	Diamine acetyltransferase 1	Homo sapiens (human)
spermidine binding	Diamine acetyltransferase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
collagen-containing extracellular matrix	Cathepsin B	Homo sapiens (human)
extracellular region	Cathepsin B	Homo sapiens (human)
extracellular space	Cathepsin B	Homo sapiens (human)
lysosome	Cathepsin B	Homo sapiens (human)
external side of plasma membrane	Cathepsin B	Homo sapiens (human)
apical plasma membrane	Cathepsin B	Homo sapiens (human)
endolysosome lumen	Cathepsin B	Homo sapiens (human)
melanosome	Cathepsin B	Homo sapiens (human)
perinuclear region of cytoplasm	Cathepsin B	Homo sapiens (human)
collagen-containing extracellular matrix	Cathepsin B	Homo sapiens (human)
extracellular exosome	Cathepsin B	Homo sapiens (human)
peptidase inhibitor complex	Cathepsin B	Homo sapiens (human)
ficolin-1-rich granule lumen	Cathepsin B	Homo sapiens (human)
extracellular space	Cathepsin B	Homo sapiens (human)
lysosome	Cathepsin B	Homo sapiens (human)
extracellular space	Furin	Homo sapiens (human)
Golgi membrane	Furin	Homo sapiens (human)
extracellular region	Furin	Homo sapiens (human)
endoplasmic reticulum	Furin	Homo sapiens (human)
Golgi lumen	Furin	Homo sapiens (human)
trans-Golgi network	Furin	Homo sapiens (human)
plasma membrane	Furin	Homo sapiens (human)
cell surface	Furin	Homo sapiens (human)
endosome membrane	Furin	Homo sapiens (human)
membrane	Furin	Homo sapiens (human)
trans-Golgi network transport vesicle	Furin	Homo sapiens (human)
membrane raft	Furin	Homo sapiens (human)
extracellular exosome	Furin	Homo sapiens (human)
Golgi membrane	Furin	Homo sapiens (human)
trans-Golgi network	Furin	Homo sapiens (human)
extracellular space	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
extracellular region	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
extracellular space	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
peroxisome	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
plasma membrane	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
bicellular tight junction	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
specific granule lumen	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
extracellular exosome	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
plasma membrane	Amiloride-sensitive amine oxidase [copper-containing]	Homo sapiens (human)
cytosol	Diamine acetyltransferase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (144)

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]

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]

Article	Year
Cytotoxicity and anti-inflammatory effect of a novel diminazene aceturate derivative in bovine mammary epithelial cells. Research in veterinary science, Volume: 137	2021
Safety and efficacy of hydroxyurea and eflornithine against most blood parasites Babesia and Theileria. PloS one, Volume: 15, Issue: 2	2020
Safety and efficacy of three trypanocides in confirmed field cases of trypanosomiasis in working equines in The Gambia: a prospective, randomised, non-inferiority trial. PLoS neglected tropical diseases, Volume: 13, Issue: 3	2019
Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity. European journal of medicinal chemistry, Feb-15, Volume: 164	2019
Nerolidol nanospheres increases its trypanocidal efficacy against Trypanosoma evansi: New approach against diminazene aceturate resistance and toxicity. Experimental parasitology, Volume: 166	2016
Failure of efficacy and adverse events associated with dose-intense diminazene diaceturate treatment of chronic Cytauxzoon felis infection in five cats. Journal of feline medicine and surgery, Volume: 16, Issue: 2	2014
In vitro activity and preliminary toxicity of various diamidine compounds against Trypanosoma evansi. Veterinary parasitology, May-11, Volume: 169, Issue: 3-4	2010
Leishmania donovani: differential activities of classical topoisomerase inhibitors and antileishmanials against parasite and host cells at the level of DNA topoisomerase I and in cytotoxicity assays. Experimental parasitology, Volume: 112, Issue: 1	2006
Drug cytotoxicity assay for African trypanosomes and Leishmania species. The Journal of infectious diseases, Volume: 172, Issue: 4	1995
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Article	Year
The intravenous pharmacokinetics of diminazene in healthy dogs. Journal of the South African Veterinary Association, Volume: 80, Issue: 4	2009
The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs. Journal of the South African Veterinary Association, Volume: 76, Issue: 3	2005
Pharmacokinetics, urinary excretion and dosage regimen of diminazene in crossbred calves. Acta veterinaria Hungarica, Volume: 48, Issue: 2	2000
Comparative pharmacokinetics of diminazene in lactating goats and sheep. Zentralblatt fur Veterinarmedizin. Reihe A, Volume: 46, Issue: 1	1999
Pharmacokinetics of diminazene in plasma and lymph of goats. American journal of veterinary research, Volume: 57, Issue: 5	1996
Pharmacokinetics of diminazene in female Boran (Bos indicus) cattle. Journal of veterinary pharmacology and therapeutics, Volume: 16, Issue: 3	1993
Comparative pharmacokinetics of diminazene in noninfected Boran (Bos indicus) cattle and Boran cattle infected with Trypanosoma congolense. Antimicrobial agents and chemotherapy, Volume: 37, Issue: 5	1993
Pharmacokinetics of diminazene in plasma and cerebrospinal fluid of goats. Research in veterinary science, Volume: 57, Issue: 2	1994
Variations in packed red cell volume and trypanosome prevalence and relationships with reproductive traits in east African Zebu cows exposed to drug-resistant trypanosomes. Acta tropica, Volume: 59, Issue: 2	1995
A bioequivalence and pharmacokinetic evaluation of two commercial diminazene aceturate formulations administered intramuscularly to cattle. The Onderstepoort journal of veterinary research, Volume: 61, Issue: 4	1994
Pharmacokinetics of diminazene in sheep. Journal of pharmacokinetics and biopharmaceutics, Volume: 13, Issue: 2	1985
Effects of trypanosomal infection on the pharmacokinetics of diminazene aceturate in dogs. Tropical medicine and parasitology : official organ of Deutsche Tropenmedizinische Gesellschaft and of Deutsche Gesellschaft fur Technische Zusammenarbeit (GTZ), Volume: 40, Issue: 4	1989
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Article	Year
New antiglaucomatous agent for the treatment of open angle glaucoma: Polymeric inserts for drug release and in vitro and in vivo study. Journal of biomedical materials research. Part A, Volume: 109, Issue: 3	2021
Upregulation of Angiotensin (1-7)-Mediated Signaling Preserves Endothelial Function Through Reducing Oxidative Stress in Diabetes. Antioxidants & redox signaling, Oct-10, Volume: 23, Issue: 11	2015
Diminazene protects corpus cavernosum against hypercholesterolemia-induced injury. The journal of sexual medicine, Volume: 12, Issue: 2	2015
Enzymatic response of the eucalypt defoliator Thyrinteina arnobia (Stoll) (Lepidoptera: Geometridae) to a bis-benzamidine proteinase Inhibitor. i. Neotropical entomology, Volume: 41, Issue: 5	2012
Pharmacokinetics, urinary excretion and dosage regimen of diminazene in crossbred calves. Acta veterinaria Hungarica, Volume: 48, Issue: 2	2000
Pharmacokinetics of diminazene in female Boran (Bos indicus) cattle. Journal of veterinary pharmacology and therapeutics, Volume: 16, Issue: 3	1993
Studies in cattle on the disposition of the anti-trypanosomal drug diminazene diaceturate (Berenil). Tropical medicine and parasitology : official organ of Deutsche Tropenmedizinische Gesellschaft and of Deutsche Gesellschaft fur Technische Zusammenarbeit (GTZ), Volume: 36, Issue: 4	1985
In vivo and in vitro sensitivity of Trypanosoma evansi and T. equiperdum to diminazene, suramin, MelCy, quinapyramine and isometamidium. Acta tropica, Volume: 50, Issue: 2	1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

diminazene

Description

Cross-References

Synonyms (53)

Research Excerpts

Overview

Effects

Treatment

Roles (2)

Drug Classes (2)

Protein Targets (6)

Inhibition Measurements

Biological Processes (45)

Molecular Functions (30)

Ceullar Components (26)

Bioassays (144)

Research

Studies (740)

Study Types

Research Highlights

Safety/Toxicity (11)

Long-term Use (1)

Pharmacokinetics (12)

Bioavailability (8)

Dosage (22)

Interactions (3)

Article	Year
Short-term treatment with diminazene aceturate ameliorates the reduction in kidney ACE2 activity in rats with subtotal nephrectomy. PloS one, Volume: 10, Issue: 3	2015
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Article	Year
Variation of sensitivity of Trypanosoma evansi isolates from Isiolo and Marsabit counties of Kenya to locally available trypanocidal drugs. PloS one, Volume: 18, Issue: 2	2023
Diminazene aceturate liposomes: morphometric and biochemical liver, kidney, and spleen of rats infected with Trypanosoma evansi. Pathology, research and practice, Volume: 210, Issue: 12	2014
Kenyan purple tea anthocyanins and coenzyme-Q10 ameliorate post treatment reactive encephalopathy associated with cerebral human African trypanosomiasis in murine model. Parasitology international, Volume: 63, Issue: 2	2014
Validation of an HPLC method for the simultaneous determination of diminazene diaceturate and phenazone in injectable veterinary granules and bulk powders. Pakistan journal of pharmaceutical sciences, Volume: 25, Issue: 1	2012
Effects of melarsamine hydrochloride (Cymelarsan) and diminazene aceturate (Berenil) on the pathology of experimental Trypanosoma brucei infection in red fronted gazelles (Gazella rufifrons). Veterinary parasitology, Jul-07, Volume: 163, Issue: 1-2	2009
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. Tropical animal health and production, Volume: 36, Issue: 1	2004
Pharmacokinetics, urinary excretion and dosage regimen of diminazene in crossbred calves. Acta veterinaria Hungarica, Volume: 48, Issue: 2	2000
The use of trypanocides and antibiotics by Maasai pastoralists. Tropical animal health and production, Volume: 32, Issue: 6	2000
Variation in sensitivity of Trypanosoma congolense to diminazene during the early phase of tsetse-transmitted infection in goats. Veterinary parasitology, Volume: 50, Issue: 1-2	1993
Putrescine uptake inhibition by aromatic diamidines in Leishmania infantum promastigotes. Biochemical pharmacology, May-18, Volume: 47, Issue: 10	1994
Time-dose-response of Trypanosoma brucei brucei to diminazene aceturate (Berenil) and in vitro simulation of drug-concentration-time profiles in cattle plasma. Acta tropica, Volume: 54, Issue: 1	1993
Apparent rarity of diminazene-resistant trypanosomes in goats infected with a diminazene-resistant population of Trypanosoma congolense. Research in veterinary science, Volume: 58, Issue: 2	1995
Frequency of diminazene-resistant trypanosomes in populations of Trypanosoma congolense arising in infected animals following treatment with diminazene aceturate. Antimicrobial agents and chemotherapy, Volume: 39, Issue: 5	1995
Pharmacotherapeutics of drugs used in treatment of anaplasmosis and babesiosis. Journal of the American Veterinary Medical Association, May-15, Volume: 176, Issue: 10 Spec No	1980
Studies in rabbits on the disposition and trypanocidal activity of the anti-trypanosomal drug, diminazene aceturate (Berenil). British journal of pharmacology, Volume: 80, Issue: 1	1983
Observation on drug resistance of Trypanosoma (Nannomonas) congolense and Trypanosoma (Duttonella) vivax in cattle at a feedlot in the Northern Ivory Coast. Tropenmedizin und Parasitologie, Volume: 34, Issue: 3	1983
Comparative studies of the effects of quinuronium sulfate and diminazene diaceturate in sheep. Veterinary and human toxicology, Volume: 27, Issue: 6	1985
Extravascular foci of Trypanosoma vivax in goats: the central nervous system and aqueous humor of the eye as potential sources of relapse infections after chemotherapy. Parasitology, Volume: 97 ( Pt 1)	1988
Combination therapy of trypanosomiasis using diminazene and non-steroidal anti-inflammatory drugs. Journal of chemotherapy (Florence, Italy), Volume: 3, Issue: 4	1991
In vivo and in vitro sensitivity of Trypanosoma evansi and T. equiperdum to diminazene, suramin, MelCy, quinapyramine and isometamidium. Acta tropica, Volume: 50, Issue: 2	1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Article	Year
Use of a doxycycline-enrofloxacin-metronidazole combination with/without diminazene diaceturate to treat naturally occurring canine babesiosis caused by Babesia gibsoni. Acta veterinaria Scandinavica, Apr-24, Volume: 52	2010
Trypanocidal resistance in Trypanosoma evansi in vitro: effects of verapamil, cyproheptidine, desipramine and chlorpromazine alone and in combination with trypanocides. Veterinary parasitology, Volume: 62, Issue: 1-2	1996
The effect of verapamil alone and in combination with trypanocides on multidrug-resistant Trypanosoma brucei brucei. Acta tropica, Volume: 49, Issue: 3	1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Description	Relationhip Strength	Studies	Classes	Roles
hoe 33342	[no description available]	medium	2	bibenzimidazole; N-methylpiperazine	fluorochrome
stallimycin	[no description available]	medium	12
daunorubicin	[no description available]	medium	2	aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones	antineoplastic agent; bacterial metabolite
cc 1065	[no description available]	medium	2
dapi	[no description available]	medium	19	indoles	fluorochrome
pentamidine	[no description available]	high	73	aromatic ether; carboxamidine; diether	anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic
ethidium bromide	[no description available]	medium	2	organic bromide salt	geroprotector; intercalator; trypanocidal drug
4',6-bis(2'imidazolinyl-4',5'-h)-2-phenylindole	[no description available]	medium	1
1,2-di(5-amidino-2-benzofuranyl)ethane	[no description available]	medium	1
furamidine	[no description available]	medium	7
2-(4-amidinophenyl)-1-benzofuran-5-carboxamidine	[no description available]	medium	1
stilbamidine	[no description available]	medium	7
acriflavine chloride	[no description available]	medium	1	organic chloride salt	antibacterial agent; antiseptic drug; carcinogenic agent; histological dye; intercalator
proflavine	[no description available]	medium	3	aminoacridines	antibacterial agent; antiseptic drug; carcinogenic agent; chromophore; intercalator
nitracrine	[no description available]	medium	1	acridines
4-(9-acridinylamino)aniline	[no description available]	medium	1
1-nitro-9-aminoacridine	[no description available]	medium	1
amsacrine	[no description available]	medium	1	acridines; aromatic ether; sulfonamide	antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
acridines	[no description available]	medium	3	acridines; mancude organic heterotricyclic parent; polycyclic heteroarene	genotoxin
adenine	[no description available]	medium	7	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
n-butylamine	[no description available]	medium	1	primary aliphatic amine
mitoguazone	[no description available]	medium	9	guanidines; hydrazone	antineoplastic agent; apoptosis inducer; EC 4.1.1.50 (adenosylmethionine decarboxylase) inhibitor
mdl 73811	[no description available]	medium	1
chloroquine	[no description available]	medium	5	aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug
mefloquine hydrochloride	[no description available]	medium	1	organofluorine compound; piperidines; quinolines; secondary alcohol
oxophenylarsine	[no description available]	medium	8	arsine oxides	antineoplastic agent; apoptosis inducer; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor
melarsoprol	[no description available]	medium	26	triazines
2'-deoxyadenosine	[no description available]	medium	1	purine 2'-deoxyribonucleoside; purines 2'-deoxy-D-ribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
suramin	[no description available]	high	37	naphthalenesulfonic acid; phenylureas; secondary carboxamide	angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug
quinacrine	[no description available]	medium	1	acridines; aromatic ether; organochlorine compound; tertiary amino compound	antimalarial; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor
propamidine	[no description available]	medium	4	aromatic ether; guanidines; polyether	antimicrobial agent; antiseptic drug
tebuquine	[no description available]	medium	1
n,n-dideethylchloroquine	[no description available]	medium	1
3,6-diamino-9-(4-(methylsulfonyl)aminophenyl)aminoacridine	[no description available]	medium	1
cryptolepine monohydrochloride	[no description available]	medium	1
quinidine	[no description available]	medium	1	cinchona alkaloid	alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker
quinine	[no description available]	medium	3	cinchona alkaloid	antimalarial; muscle relaxant; non-narcotic analgesic
bisbenzimidazole	[no description available]	medium	15	bibenzimidazole; N-methylpiperazine	anthelminthic drug; fluorochrome
mitoxantrone	[no description available]	medium	1	dihydroxyanthraquinone	analgesic; antineoplastic agent
netropsin	[no description available]	medium	19

diminazene

Description

Cross-References

Synonyms (53)

Research Excerpts

Overview

Effects

Treatment

Roles (2)

Drug Classes (2)

Protein Targets (6)

Inhibition Measurements

Biological Processes (45)

Molecular Functions (30)

Ceullar Components (26)

Bioassays (144)

Research

Studies (740)

Study Types

Related Drugs (419)

Related Conditions (858)

Research Highlights

Safety/Toxicity (11)

Long-term Use (1)

Pharmacokinetics (12)

Bioavailability (8)

Dosage (22)

Interactions (3)