Page last updated: 2024-12-06

diminazene aceturate

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

Description

diminazene diaceturate : An N-acetylglycinate salt resulting from the reaction of diminazene with 2 mol eq. of N-acetylglycine. [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 CID5284544
CHEMBL ID380216
CHEBI ID82615
SCHEMBL ID11311441
MeSH IDM0045045
PubMed CID65060
CHEMBL ID124025
SCHEMBL ID120718
MeSH IDM0045045

Synonyms (80)

Synonym
n-acetylglycine - 4-[(1e)-3-{4-[amino(imino)methyl]phenyl}triaz-1-en-1-yl]benzenecarboximidamide (2:1)
diminazene diaceturate
908-54-3
diminazene aceturate
CHEMBL380216
chebi:82615 ,
HMS3264M22
SCHEMBL11311441
S4104
FT-0624974
AKOS025310610
CCG-213828
diminazene aceturate [mi]
diminazene aceturate [mart.]
(triaz-1-ene-1,3-diyldi-4,1-phenylene)bis(iminomethanaminium) bis(acetamidoacetate)
diminazene bis(n-acetylglycinate)
W-100324
DTXSID4022945
diminazene aceturate, analytical standard
AKOS030243015
HMS3652K14
mfcd00058386
4,4'-(triaz-1-ene-1,3-diyl)dibenzimidamide bis(acetylglycinate)
SW219273-1
(e)-4,4'-(triaz-1-ene-1,3-diyl)dibenzimidamide bis(2-acetamidoacetate)
diminazene (aceturate)
CS-0011255
HY-12404
Q27156132
AS-14290
diminazene (diaceturate)
4,4'-(1-triazene-1,3-diyl)bis[benzenecarboximidamide] bis(n-acetylglycinate)
4,4'-(triaz-1-ene-1,3-diyl)dibenzimidamide bis(2-acetamidoacetate)
4-[2-(4-carbamimidoylphenyl)iminohydrazinyl]benzene-carboximidamide diaceturate
A916389
diminazene aceturate is known as an anti-protozoal diamidine.
diminazene aceturate 100 microg/ml in acetonitrile:water
2-acetamidoacetic acid;4-[2-(4-carbamimidoylphenyl)iminohydrazinyl]benzenecarboximidamide
diminazene 1000 microg/ml in acetonitrile:water
einecs 212-999-2
di-(4-amidinophenyl)-triazen-(n-1,3)-diaceturat [german]
4,4'-(diamino)dibenzamide diaceturate
nsc 114835
di-(4-amidinophenyl)-triazine-(n-1,3)-diaceturate
1,3-bis(4-guanylphenyl)triazene diaceturate
n-acetylglycine, compound with 4,4'-(1-triazene-1,3-diyl)bis(benzenecarboxamidine) (2:1)
diminazenaceturate
beronal
4,4'-diamidinodiazoaminobenzene diaceturate
ganasag
berenil
diaminazene aceturate
diminazine aceturate
azidin
p,p'-diguanyldiazoaminobenzene diaceturate
nsc114835
4,4'-(diazoamino)dibenzamidine diaceturate
nsc-114835
ganaseg
1,3-bis(p-amidinophenyl)triazene bis(n-acetylglycinate)
azidine
1,3-bis[4-guanylphenyl]triazene diaceturate
bevenil
CHEMBL124025
nsc759843
pharmakon1600-01502349
nsc-759843
di-(4-amidinophenyl)-triazen-(n-1,3)-diaceturat
unii-ji8sad85no
ji8sad85no ,
smr004701261
MLS006010139
SCHEMBL120718
AKOS026750040
bis(2-acetamidoacetic acid); 4-[(2e)-3-(4-carbamimidoylphenyl)triaz-2-en-1-yl]benzene-1-carboximidamide
M011GS5PF5 ,
diminazene monoaceturate
unii-m011gs5pf5
15114-96-2
Q27281516

Research Excerpts

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
)
0.4
"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
)
0.43
" 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
)
0.51
" 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
)
0.62

Pharmacokinetics

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
)
0.29

Compound-Compound Interactions

Susceptibility patterns of sensitive and resistant parasites were evaluated against calcium antagonists of several chemical classes.

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
)
0.28
" 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
)
0.29

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
)
0.28
"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
)
0.42

Dosage Studied

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
)
0.28
" 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
)
0.29
" 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
)
0.29
" 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
" 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
)
0.38
" 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 (1)

ClassDescription
N-acetylglycinate saltAny salt prepared using N-acetylglycine as the acid component.
[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]

Bioassays (74)

Assay IDTitleYearJournalArticle
AID1435163Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 40 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435160Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 37 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1426364Anti-parasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as reduction in parasitemia at 10 mg/kg, ip bid administered on day 21 to 30 post infection measured on day 180 by microscopic method2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.
AID1689543Competitive binding affinity to Escherichia coli XL-1 pUC18 plasmid DNA at 20 uM after 30 to 120 mins by DAPI staining based spectrofluorimetric method relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1585774Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei strain 427 after 48 hrs by resazurin dye-based assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
AID1435162Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 39 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1689521Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei 427 infected in 449_Grx-roGFP2 cells assessed as cell viability after 24 hrs by propidium iodide staining based flow cytometric analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1695260Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by resazurin assay
AID1435159Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 36 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID266332Activity against Trypanosoma brucei GVR35 in infected NMRI mouse at 40 mg/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity.
AID1689550Antitrypanosomal activity against Trypanosoma brucei brucei AnTaT 1.1 infected in Balb/cJ mouse assessed as reduction in parasitemia at 40 mg/kg, ip for single dose and measured after 7 to 17 days2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1368576Antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Swiss Webster mouse assessed as mean relapse time at 10 mg/kg, ip administered as single dose on day 21 post-infection (Rvb = 31 days)2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1689538Induction of cell cycle arrest in bloodstream form Trypanosoma brucei brucei 427 assessed as accumulation at 0K+1N cells at 41 nM after 24 hrs by DAPI. staining based epifluorescence microscopic analysis relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1435157Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 34 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435161Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 38 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1689544Competitive binding affinity to Escherichia coli XL-1 pUC18 K-DNA at 20 uM after 30 to 120 mins by DAPI staining based spectrofluorimetric method relative to control2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1435165Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 43 to 45 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1689522Selectivity index, ratio of EC50 for cytotoxicity against mouse J774 cells to EC50 for antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei 4272020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID213470In vitro antitrypanosomal activity against Trypanosoma brucei rhodesiense2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Bisguanidine, bis(2-aminoimidazoline), and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation.
AID1689536Induction of cell cycle arrest in bloodstream form Trypanosoma brucei brucei 427 assessed as accumulation at G0/G1 phase at 41 nM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 49%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1689537Induction of cell cycle arrest in bloodstream form Trypanosoma brucei brucei 427 assessed as accumulation at 1K+1N cells at 41 nM after 24 hrs by DAPI. staining based epifluorescence microscopic analysis (Rvb = 80%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1689535Induction of cell cycle arrest in bloodstream form Trypanosoma brucei brucei 427 assessed as accumulation at G2/M phase at 41 nM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 20%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
AID1435164Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 41 to 42 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1695263Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 infected in human HEK293 cells assessed as parasite growth inhibition measured after 48 hrs by alamar blue assay
AID1368580Antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Swiss Webster mouse assessed as infection cure rate at 10 mg/kg, ip administered as single dose on day 4 post-infection (Rvb = 0%)2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1435180Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasite levels in brain at 10 mg/kg, ip administered as single dose on day 21 post infection by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1368581Antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Swiss Webster mouse assessed as infection cure rate at 10 mg/kg, ip administered as single dose on day 21 post-infection (Rvb = 0%)2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.
AID1435179Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasite levels in peripheries at 10 mg/kg, ip administered as single dose on day 21 post infection by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435166Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 50 to 51 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID1435158Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 10 mg/kg, ip administered as single dose on day 21 post infection measured on day 35 by microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.
AID576019Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2238-encoded QacBIV gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID110827Compound was tested for Trypanocidal Activity in mice at 0.4 mg/kg; 24/451984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID110963Compound was tested for Trypanocidal Activity in mice at 100 mg/kg; 5/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID111001Compound was tested for Trypanocidal Activity in mice at 25 mg/kg; 3/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID110993Compound was tested for Trypanocidal Activity in mice at 2.5 mg/kg; 9/101984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID576021Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2238-encoded QacBIV S151I mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID576022Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2238-encoded QacBIV A184V mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID111145Compound was tested for Trypanocidal Activity in mice at 6 mg/kg; 10/101984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID110975Compound was tested for Trypanocidal Activity in mice at 150 mg/kg; 3/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID46169Inhibitory concentration against ethidium:Calf thymus DNA(0.1:1) binding at pH 51997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
1-[(omega-aminoalkyl)amino]-4-[N-(omega-aminoalkyl)carbamoyl]-9-oxo-9, 10-dihydroacridines as intercalating cytotoxic agents: synthesis, DNA binding, and biological evaluation.
AID608617Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Synthesis and biological evaluation of 4-nitro-substituted 1,3-diaryltriazenes as a novel class of potent antitumor agents.
AID660873Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei 427 (BS221) after 72 hrs by alamar blue assay2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity.
AID576014Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZN10 containing cat and bla genes by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID110820Compound was tested for Trypanocidal Activity in mice at 0.06 mg/kg; 0/101984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID576016Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2182-encoded QacBII gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID111138Compound was tested for Trypanocidal Activity in mice at 60 mg/kg; 5/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID110983Compound was tested for Trypanocidal Activity in mice at 15 mg/kg; 3/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID608831Cytotoxicity against mouse L1210 cells at 32 uM2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Synthesis and biological evaluation of 4-nitro-substituted 1,3-diaryltriazenes as a novel class of potent antitumor agents.
AID111122Compound was tested for Trypanocidal Activity in mice at 40 mg/kg; 5/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID660874Antitrypanosomal activity against TbAt1-deficient bloodstraem form of Trypanosoma brucei brucei 427 (BS221) after 72 hrs by alamar blue assay2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity.
AID311567Antibabesial activity against Babesia gibsoni2007Journal of natural products, Oct, Volume: 70, Issue:10
Screening of Indonesian medicinal plant extracts for antibabesial activity and isolation of new quassinoids from Brucea javanica.
AID55499Concentration required to give 50% fluorescence quenching of bound ethidium for [ethidium]: [(poly dG-dC)]2 DNA in ratio of 0.1:1 at pH 51997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
1-[(omega-aminoalkyl)amino]-4-[N-(omega-aminoalkyl)carbamoyl]-9-oxo-9, 10-dihydroacridines as intercalating cytotoxic agents: synthesis, DNA binding, and biological evaluation.
AID110957Compound was tested for Trypanocidal Activity in mice at 1.5 mg/kg; 19/201984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID111127Compound was tested for Trypanocidal Activity in mice at 4 mg/kg; 10/101984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID463400Selectivity ratio of EC50 for Trypanosoma brucei brucei 427 to EC50 for Trypanosoma brucei brucei deltaTbat1-KO2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species.
AID110949Compound was tested for Trypanocidal Activity in mice at 0.6 mg/kg; 23/251984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID110825Compound was tested for Trypanocidal Activity in mice at 0.25 mg/kg; 28/401984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID662819Antileishmanial activity against amastigotes of Leishmania mexicana MNYC/BZ/62/M379 after 72 hrs by alamar blue assay2011ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12
Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity.
AID576015Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2396-encoded QacA gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID576017Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2162-encoded QacBIII gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID377793Antibabesial activity against Babesia gibsoni in dog erythrocytes after 72 hrs2005Journal of natural products, Apr, Volume: 68, Issue:4
Anti-babesial and anti-plasmodial compounds from Phyllanthus niruri.
AID98563Cytotoxic potency required to inhibit L1210 cell growth by 50% after cell drug contact for 48 hrs1997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
1-[(omega-aminoalkyl)amino]-4-[N-(omega-aminoalkyl)carbamoyl]-9-oxo-9, 10-dihydroacridines as intercalating cytotoxic agents: synthesis, DNA binding, and biological evaluation.
AID110972Compound was tested for Trypanocidal Activity in mice at 10 mg/kg; 5/51984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID110952Compound was tested for Trypanocidal Activity in mice at 1.0 mg/kg; 9/101984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID55500Concentration required to give 50% fluorescence quenching of bound ethidium for [ethidium]: [poly(dA-dT)]2 DNA in ratio of 0.1:1 at pH 51997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
1-[(omega-aminoalkyl)amino]-4-[N-(omega-aminoalkyl)carbamoyl]-9-oxo-9, 10-dihydroacridines as intercalating cytotoxic agents: synthesis, DNA binding, and biological evaluation.
AID110822Compound was tested for Trypanocidal Activity in mice at 0.15 mg/kg; 6/201984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID576018Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2162-encoded QacBIII E320A mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID46135Inhibitory concentration against ethidium:Calf thymus DNA (1.26:1) binding at pH 71997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
1-[(omega-aminoalkyl)amino]-4-[N-(omega-aminoalkyl)carbamoyl]-9-oxo-9, 10-dihydroacridines as intercalating cytotoxic agents: synthesis, DNA binding, and biological evaluation.
AID1812896Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei measured after 3 to 4 days by Z2 coulter counter based analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.
AID113850Effective dose against Trypanosoma brucei infection in mice1984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID46133Inhibitory concentration against ethidium:calf thymus DNA (1.26:1) binding at pH 51997Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23
1-[(omega-aminoalkyl)amino]-4-[N-(omega-aminoalkyl)carbamoyl]-9-oxo-9, 10-dihydroacridines as intercalating cytotoxic agents: synthesis, DNA binding, and biological evaluation.
AID576023Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2238-encoded QacBIV E377G mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
AID110823Compound was tested for Trypanocidal Activity in mice at 0.1 mg/kg; 1/101984Journal of medicinal chemistry, Jan, Volume: 27, Issue:1
Trypanocidal 1,3-arylene diketone bis(guanylhydrazone)s. Structure-activity relationships among substituted and heterocyclic analogues.
AID576020Antimicrobial activity against Staphylococcus aureus RDN1 harboring cloned pTZ2238-encoded QacBIV A19T mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Fluoroquinolone efflux by the plasmid-mediated multidrug efflux pump QacB variant QacBIII in Staphylococcus aureus.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (557)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990130 (23.34)18.7374
1990's145 (26.03)18.2507
2000's74 (13.29)29.6817
2010's154 (27.65)24.3611
2020's54 (9.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 51.47

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 Index51.47 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.95 (4.65)
Search Engine Demand Index75.75 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (51.47)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (2.85%)5.53%
Trials0 (0.00%)5.53%
Reviews14 (2.49%)6.00%
Reviews0 (0.00%)6.00%
Case Studies6 (1.07%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other526 (93.59%)84.16%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Safety of Trypan Blue Capsule Staining to Corneal Endothelium in Patients With Diabetic Retinopathy [NCT03755752]65 participants (Actual)Interventional2018-01-01Completed
Membranepeeling With Trypan Blue Versus Membranpeeling With Brillant Blue for Patients With Idiopathic Epiretinal Membranes [NCT00757380]60 participants (Actual)Interventional2008-07-31Completed
A Descriptive Study to Evaluate the Efficacy of the Dye Compound of the Combination of Lutein, Zeaxanthin and Trypan Blue to Stain the Anterior Lens Capsule During Cataract Phacoemulsification. [NCT01621789]Phase 325 participants (Actual)Interventional2012-06-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]