Page last updated: 2024-11-07

furamidine

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

Description

furamidine: RN given refers to parent cpd; WR 199385 refers to di-HCl; pafuramidine is a prodrug of this [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID126437
CHEMBL ID24057
SCHEMBL ID549198
MeSH IDM0103342

Synonyms (44)

Synonym
NCI60_002601
4,4'-(2,5-furandiyl)bis(benzenecarboximidamide)
2,5-bis(4-amidinophenyl)furan
brn 1435532
db 75
benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-, dihydrochloride
nsc305831 ,
nsc-305831
2,5-bis(4-amidinophenyl)-furan
db75
furamidine
furandiamidine
benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-
NCGC00014688
BGF ,
NCI305831
NCISTRUC1_001694
NCISTRUC2_001468
NCGC00097791-01
NCGC00097791-02
CHEMBL24057
4-[5-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide
73819-26-8
bdbm50388602
CCG-37385
NCGC00014688-03
NCGC00014688-02
unii-08gh1yf0ra
08gh1yf0ra ,
5-18-07-00177 (beilstein handbook reference)
furamidine-d8
furamidine dihydrochloride
SCHEMBL549198
DTXSID00224264
AKOS030254780
HY-110137A
336786-81-3
db75;nsc 305831
db-75
4,4'-(2,5-furandiyl)bis [benzenecarboximidamide]
NCGC00014688-06
CS-0058706
4,4'-(furan-2,5-diyl)dibenzimidamide
73819-26-8 (free base)

Research Excerpts

Overview

Furamidine is an effective antimicrobial agent; however, oral potency of furamidine was poor. Pafuramidine is a novel orally active antimalarial.

ExcerptReferenceRelevance
"Furamidine is an effective antimicrobial agent; however, oral potency of furamidine is poor. "( Unusual dehydroxylation of antimicrobial amidoxime prodrugs by cytochrome b5 and NADH cytochrome b5 reductase.
Anbazhagan, M; Boykin, DW; Bridges, AS; Hall, JE; Kurian, JR; Saulter, JY; Stephens, CE; Tidwell, RR; Trepanier, LA, 2005
)
1.77
"Pafuramidine is a novel orally active antimalarial. "( Interactions of DB75, a novel antimalarial agent, with other antimalarial drugs in vitro.
Meshnick, SR; Purfield, AE; Tidwell, RR, 2008
)
1.07

Pharmacokinetics

ExcerptReferenceRelevance
" In this study, we aimed to determine the mechanisms underlying the differential efficacies of these diamidines against HAT by conducting a comprehensive pharmacokinetic characterization."( Pharmacokinetic comparison to determine the mechanisms underlying the differential efficacies of cationic diamidines against first- and second-stage human African trypanosomiasis.
Boykin, DW; Brun, R; Miller, PN; Wang, MZ; Wenzler, T; Wu, H; Yang, S, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
" However, DB75 does not exhibit significant oral bioavailability and has proved to be ineffective against mouse models of late-stage sleeping sickness regardless of administration route."( Distribution and quantitation of the anti-trypanosomal diamidine 2,5-bis(4-amidinophenyl)furan (DB75) and its N-methoxy prodrug DB289 in murine brain tissue.
Bagnell, CR; Brock, JL; Hall, JE; Sturk, LM; Tidwell, RR, 2004
)
0.32
" Oral doses were well absorbed (approximately 50-70%) and effectively converted to DB75 in both species but subject to first-pass metabolism and hepatic retention, limiting its systemic bioavailability to 10 to 20%."( Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride).
Boykin, DW; Cybulski, ZR; Fitzpatrick, K; Henderson, SJ; Houchen, TL; John, BA; McBurney, A; Midgley, I; Taylor, LM; Trendler, KL; Wright, SJ, 2007
)
0.34
" An orally bioavailable prodrug of CPD-0801, DB868, is metabolized primarily in the liver to the active form."( Application of monoclonal antibodies to measure metabolism of an anti-trypanosomal compound in vitro and in vivo.
Generaux, CN; Goldsmith, RB; Gray, DR; Reisner, HM; Tidwell, RR; Yan, Z, 2010
)
0.36

Dosage Studied

ExcerptRelevanceReference
"1% of control when administered at a dosage of 10 mumol/kg."( 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
Bender, BC; Boykin, DW; Hall, JE; Kumar, A; McCurdy, DR; Tidwell, RR; Wilson, WD; Xiao, G, 1998
)
0.3
"1% of control when administered at a dosage of 10 micromol/kg."( Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
Bajic, M; Bender, BC; Boykin, DW; Hall, JE; Hopkins, KT; Kumar, A; McCurdy, DR; Tidwell, RR; Wilson, WD, 1998
)
0.3
" The in vivo results show that the 4-fluorophenyl carbamate 8 and the 4-methoxyphenyl carbamate 9 in this series had the best anti-PCP activity by both intravenous and oral administration at a dosage level of 22 mol and 33 micromol/kg/day, respectively."( Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan.
Bender, BC; Boykin, DW; Hall, JE; McCurdy, DR; Rahmathullah, SM; Tidwell, RR, 1999
)
0.3
" Compound 6a produced cures at an oral dosage of 5 mg/kg."( Synthesis and antiprotozoal activity of aza-analogues of furamidine.
Boykin, DW; Brun, R; Easterbrook, JD; Ismail, MA; Tanious, FA; Wilson, WD, 2003
)
0.56
" Although effective treatments for early-stage sleeping sickness exist, these drugs usually require extended dosing schedules and intravenous administration."( Distribution and quantitation of the anti-trypanosomal diamidine 2,5-bis(4-amidinophenyl)furan (DB75) and its N-methoxy prodrug DB289 in murine brain tissue.
Bagnell, CR; Brock, JL; Hall, JE; Sturk, LM; Tidwell, RR, 2004
)
0.32
" Complete cures were achieved with oral dosing of the prodrug DB289 in all three models without any overt toxicity."( Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis.
Brun, R; Kagira, JM; Karanja, SM; Mdachi, RE; Ngotho, JM; Thuita, JK; Tidwell, R; Wenzler, T, 2008
)
0.35
" Sixteen healthy volunteers were dosed and challenged in a single cohort."( Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoites.
Bakshi, RP; Hendrix, CW; Kumar, N; Nyunt, MM; Shapiro, TA, 2009
)
0.59
" rhodesiense in vivo, curing three of four infected mice dosed intraperitoneally at 5 mg/kg x 4 days."( Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
Bakunov, SA; Bakunova, SM; Barzcz, T; Brun, R; Chen, H; Jones, SK; Kumar, EV; Patrick, DA; Tidwell, RR; Wenzler, T; Werbovetz, KA, 2009
)
0.35
" The amidoxime and N-methoxyamidine of 5a were the only produgs to provide cures (1/4 cures) in the same mouse model on oral dosage at 4x25mg/kg."( Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
Boykin, DW; Branowska, D; Brun, R; Farahat, AA; Kumar, A; Liu, Y; Wenzler, T; Wilson, WD, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (25)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency5.14530.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency5.14530.025120.237639.8107AID886; AID893
thioredoxin reductaseRattus norvegicus (Norway rat)Potency57.45710.100020.879379.4328AID588453; AID588456
TDP1 proteinHomo sapiens (human)Potency7.12640.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency4.46680.011212.4002100.0000AID1030
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency5.01190.28189.721235.4813AID2326
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency3.54810.001815.663839.8107AID894
flap endonuclease 1Homo sapiens (human)Potency39.81070.133725.412989.1251AID588795
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency10.00000.050127.073689.1251AID588590
DNA polymerase kappa isoform 1Homo sapiens (human)Potency12.58930.031622.3146100.0000AID588579
caspase-1 isoform alpha precursorHomo sapiens (human)Potency3.98110.000311.448431.6228AID900
Caspase-7Homo sapiens (human)Potency3.98113.981118.585631.6228AID889
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protein arginine N-methyltransferase 5Homo sapiens (human)IC50 (µMol)211.00000.00900.69158.6000AID1128526; AID1506648
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC50 (µMol)0.03500.00271.62879.9000AID1391153
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)5.85500.00071.600310.0000AID1235076; AID1235077
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)5.85500.00071.630610.0000AID1235076; AID1235077
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)5.85500.00061.525710.0000AID1235076; AID1235077
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)5.85500.00071.747210.0000AID1235076; AID1235077
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)5.85500.00071.741110.0000AID1235076; AID1235077
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)5.85500.00071.741110.0000AID1235076; AID1235077
Protein arginine N-methyltransferase 1Homo sapiens (human)IC50 (µMol)13.43330.25003.61679.4000AID1128525; AID1506647; AID1685557
Tyrosyl-DNA phosphodiesterase 1Homo sapiens (human)IC50 (µMol)10.94500.01203.32138.4300AID1398692; AID1532278; AID1532280; AID1851331; AID673458; AID703983
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)5.85500.00071.741110.0000AID1235076; AID1235077
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protein arginine N-methyltransferase 1Homo sapiens (human)Kis2.60002.60002.60002.6000AID1128529
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (76)

Processvia Protein(s)Taxonomy
peptidyl-arginine N-methylationProtein arginine N-methyltransferase 5Homo sapiens (human)
spliceosomal snRNP assemblyProtein arginine N-methyltransferase 5Homo sapiens (human)
chromatin remodelingProtein arginine N-methyltransferase 5Homo sapiens (human)
DNA-templated transcription terminationProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of mitotic nuclear divisionProtein arginine N-methyltransferase 5Homo sapiens (human)
peptidyl-arginine methylationProtein arginine N-methyltransferase 5Homo sapiens (human)
circadian regulation of gene expressionProtein arginine N-methyltransferase 5Homo sapiens (human)
endothelial cell activationProtein arginine N-methyltransferase 5Homo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationProtein arginine N-methyltransferase 5Homo sapiens (human)
negative regulation of cell differentiationProtein arginine N-methyltransferase 5Homo sapiens (human)
negative regulation of DNA-templated transcriptionProtein arginine N-methyltransferase 5Homo sapiens (human)
positive regulation of mRNA splicing, via spliceosomeProtein arginine N-methyltransferase 5Homo sapiens (human)
positive regulation of oligodendrocyte differentiationProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of ERK1 and ERK2 cascadeProtein arginine N-methyltransferase 5Homo sapiens (human)
Golgi ribbon formationProtein arginine N-methyltransferase 5Homo sapiens (human)
liver regenerationProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of signal transduction by p53 class mediatorProtein arginine N-methyltransferase 5Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting dopamine receptor signaling pathwayProtein arginine N-methyltransferase 5Homo sapiens (human)
regulation of DNA-templated transcriptionProtein arginine N-methyltransferase 5Homo sapiens (human)
quinone catabolic processRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
proteolysisCaspase-7Homo sapiens (human)
apoptotic processCaspase-7Homo sapiens (human)
heart developmentCaspase-7Homo sapiens (human)
response to UVCaspase-7Homo sapiens (human)
protein processingCaspase-7Homo sapiens (human)
protein catabolic processCaspase-7Homo sapiens (human)
defense response to bacteriumCaspase-7Homo sapiens (human)
fibroblast apoptotic processCaspase-7Homo sapiens (human)
striated muscle cell differentiationCaspase-7Homo sapiens (human)
neuron apoptotic processCaspase-7Homo sapiens (human)
protein maturationCaspase-7Homo sapiens (human)
lymphocyte apoptotic processCaspase-7Homo sapiens (human)
cellular response to lipopolysaccharideCaspase-7Homo sapiens (human)
cellular response to staurosporineCaspase-7Homo sapiens (human)
execution phase of apoptosisCaspase-7Homo sapiens (human)
positive regulation of plasma membrane repairCaspase-7Homo sapiens (human)
positive regulation of neuron apoptotic processCaspase-7Homo sapiens (human)
regulation of DNA-templated transcriptionHistone-arginine methyltransferase CARM1Homo sapiens (human)
positive regulation of cell population proliferationHistone-arginine methyltransferase CARM1Homo sapiens (human)
methylationHistone-arginine methyltransferase CARM1Homo sapiens (human)
regulation of intracellular estrogen receptor signaling pathwayHistone-arginine methyltransferase CARM1Homo sapiens (human)
positive regulation of fat cell differentiationHistone-arginine methyltransferase CARM1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IHistone-arginine methyltransferase CARM1Homo sapiens (human)
response to cAMPHistone-arginine methyltransferase CARM1Homo sapiens (human)
replication fork reversalHistone-arginine methyltransferase CARM1Homo sapiens (human)
positive regulation of epithelial cell apoptotic processHistone-arginine methyltransferase CARM1Homo sapiens (human)
negative regulation of dendrite developmentHistone-arginine methyltransferase CARM1Homo sapiens (human)
peptidyl-arginine methylation, to asymmetrical-dimethyl arginineHistone-arginine methyltransferase CARM1Homo sapiens (human)
chromatin remodelingHistone-arginine methyltransferase CARM1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIProtein arginine N-methyltransferase 6Homo sapiens (human)
base-excision repairProtein arginine N-methyltransferase 6Homo sapiens (human)
regulation of mitochondrion organizationProtein arginine N-methyltransferase 6Homo sapiens (human)
methylationProtein arginine N-methyltransferase 6Homo sapiens (human)
protein modification processProtein arginine N-methyltransferase 6Homo sapiens (human)
regulation of megakaryocyte differentiationProtein arginine N-methyltransferase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionProtein arginine N-methyltransferase 6Homo sapiens (human)
cellular senescenceProtein arginine N-methyltransferase 6Homo sapiens (human)
regulation of signal transduction by p53 class mediatorProtein arginine N-methyltransferase 6Homo sapiens (human)
negative regulation of ubiquitin-dependent protein catabolic processProtein arginine N-methyltransferase 6Homo sapiens (human)
peptidyl-arginine methylation, to asymmetrical-dimethyl arginineProtein arginine N-methyltransferase 6Homo sapiens (human)
chromatin remodelingProtein arginine N-methyltransferase 6Homo sapiens (human)
in utero embryonic developmentProtein arginine N-methyltransferase 1Homo sapiens (human)
protein methylationProtein arginine N-methyltransferase 1Homo sapiens (human)
DNA damage responseProtein arginine N-methyltransferase 1Homo sapiens (human)
cell surface receptor signaling pathwayProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of cell population proliferationProtein arginine N-methyltransferase 1Homo sapiens (human)
RNA splicingProtein arginine N-methyltransferase 1Homo sapiens (human)
peptidyl-arginine methylationProtein arginine N-methyltransferase 1Homo sapiens (human)
viral protein processingProtein arginine N-methyltransferase 1Homo sapiens (human)
regulation of BMP signaling pathwayProtein arginine N-methyltransferase 1Homo sapiens (human)
neuron projection developmentProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of erythrocyte differentiationProtein arginine N-methyltransferase 1Homo sapiens (human)
regulation of megakaryocyte differentiationProtein arginine N-methyltransferase 1Homo sapiens (human)
negative regulation of megakaryocyte differentiationProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of translationProtein arginine N-methyltransferase 1Homo sapiens (human)
negative regulation of JNK cascadeProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of hemoglobin biosynthetic processProtein arginine N-methyltransferase 1Homo sapiens (human)
cardiac muscle tissue developmentProtein arginine N-methyltransferase 1Homo sapiens (human)
protein homooligomerizationProtein arginine N-methyltransferase 1Homo sapiens (human)
cellular response to methionineProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of p38MAPK cascadeProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of TORC1 signalingProtein arginine N-methyltransferase 1Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationProtein arginine N-methyltransferase 1Homo sapiens (human)
chromatin remodelingProtein arginine N-methyltransferase 1Homo sapiens (human)
peptidyl-arginine methylation, to asymmetrical-dimethyl arginineProtein arginine N-methyltransferase 1Homo sapiens (human)
single strand break repairTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
DNA repairTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
double-strand break repairTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (56)

Processvia Protein(s)Taxonomy
p53 bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
transcription corepressor activityProtein arginine N-methyltransferase 5Homo sapiens (human)
protein bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
methyl-CpG bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
protein-arginine N-methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
protein-arginine omega-N symmetric methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
histone methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
identical protein bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
ribonucleoprotein complex bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
histone H4R3 methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
protein heterodimerization activityProtein arginine N-methyltransferase 5Homo sapiens (human)
E-box bindingProtein arginine N-methyltransferase 5Homo sapiens (human)
histone H3 methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
histone arginine N-methyltransferase activityProtein arginine N-methyltransferase 5Homo sapiens (human)
dihydronicotinamide riboside quinone reductase activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
protein bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
zinc ion bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
electron transfer activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
oxidoreductase activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
oxidoreductase activity, acting on other nitrogenous compounds as donorsRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
chloride ion bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
protein homodimerization activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
FAD bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
melatonin bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
resveratrol bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
NAD(P)H dehydrogenase (quinone) activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
RNA bindingCaspase-7Homo sapiens (human)
aspartic-type endopeptidase activityCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-7Homo sapiens (human)
protein bindingCaspase-7Homo sapiens (human)
peptidase activityCaspase-7Homo sapiens (human)
cysteine-type peptidase activityCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activity involved in apoptotic processCaspase-7Homo sapiens (human)
cysteine-type endopeptidase activity involved in execution phase of apoptosisCaspase-7Homo sapiens (human)
transcription cis-regulatory region bindingHistone-arginine methyltransferase CARM1Homo sapiens (human)
transcription coactivator activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
protein bindingHistone-arginine methyltransferase CARM1Homo sapiens (human)
beta-catenin bindingHistone-arginine methyltransferase CARM1Homo sapiens (human)
protein methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
histone arginine N-methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
protein-arginine N-methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
nuclear receptor coactivator activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
protein-arginine omega-N asymmetric methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
histone H3R17 methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
histone methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
lysine-acetylated histone bindingHistone-arginine methyltransferase CARM1Homo sapiens (human)
histone H3R2 methyltransferase activityHistone-arginine methyltransferase CARM1Homo sapiens (human)
DNA-binding transcription factor bindingHistone-arginine methyltransferase CARM1Homo sapiens (human)
chromatin bindingProtein arginine N-methyltransferase 6Homo sapiens (human)
protein bindingProtein arginine N-methyltransferase 6Homo sapiens (human)
histone arginine N-methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
protein-arginine N-methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
protein-arginine omega-N monomethyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
protein-arginine omega-N asymmetric methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
histone methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
histone bindingProtein arginine N-methyltransferase 6Homo sapiens (human)
histone H4R3 methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
histone H3R2 methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
histone H2AR3 methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
histone H3 methyltransferase activityProtein arginine N-methyltransferase 6Homo sapiens (human)
RNA bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
protein bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
N-methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
protein methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
methyl-CpG bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
protein-arginine N-methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
enzyme bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
protein-arginine omega-N monomethyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
protein-arginine omega-N asymmetric methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
histone methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
identical protein bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
histone H4R3 methyltransferase activityProtein arginine N-methyltransferase 1Homo sapiens (human)
mitogen-activated protein kinase p38 bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
GATOR1 complex bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
S-adenosyl-L-methionine bindingProtein arginine N-methyltransferase 1Homo sapiens (human)
double-stranded DNA bindingTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
single-stranded DNA bindingTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
exonuclease activityTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
protein bindingTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
3'-tyrosyl-DNA phosphodiesterase activityTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleusProtein arginine N-methyltransferase 5Homo sapiens (human)
nucleoplasmProtein arginine N-methyltransferase 5Homo sapiens (human)
Golgi apparatusProtein arginine N-methyltransferase 5Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 5Homo sapiens (human)
methylosomeProtein arginine N-methyltransferase 5Homo sapiens (human)
chromatinProtein arginine N-methyltransferase 5Homo sapiens (human)
cytoplasmProtein arginine N-methyltransferase 5Homo sapiens (human)
histone methyltransferase complexProtein arginine N-methyltransferase 5Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 5Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 5Homo sapiens (human)
nucleoplasmRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
cytosolRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
extracellular exosomeRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
cytosolRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
extracellular spaceCaspase-7Homo sapiens (human)
nucleusCaspase-7Homo sapiens (human)
cytoplasmCaspase-7Homo sapiens (human)
cytosolCaspase-7Homo sapiens (human)
nucleusCaspase-7Homo sapiens (human)
nucleoplasmCaspase-7Homo sapiens (human)
cytosolCaspase-7Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
nuclear replication forkHistone-arginine methyltransferase CARM1Homo sapiens (human)
nucleusHistone-arginine methyltransferase CARM1Homo sapiens (human)
nucleoplasmHistone-arginine methyltransferase CARM1Homo sapiens (human)
cytoplasmHistone-arginine methyltransferase CARM1Homo sapiens (human)
cytosolHistone-arginine methyltransferase CARM1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
nucleusProtein arginine N-methyltransferase 6Homo sapiens (human)
nucleoplasmProtein arginine N-methyltransferase 6Homo sapiens (human)
nucleolusProtein arginine N-methyltransferase 6Homo sapiens (human)
lysosomal membraneProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleoplasmProtein arginine N-methyltransferase 1Homo sapiens (human)
cytoplasmProtein arginine N-methyltransferase 1Homo sapiens (human)
cytosolProtein arginine N-methyltransferase 1Homo sapiens (human)
methylosomeProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleusProtein arginine N-methyltransferase 1Homo sapiens (human)
nucleoplasmTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
cytoplasmTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
plasma membraneTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
intracellular membrane-bounded organelleTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
nucleusTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (274)

Assay IDTitleYearJournalArticle
AID322579Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected mouse model assessed as survival at 5 mg/kg, ip after 4 days2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.
AID372440Resistance factor, ratio of IC50 for tbat1 knock out Trypanosoma cruzi BS221 to IC50 for wild type Trypanosoma cruzi BS2212007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID228684In vitro DNA binding affinity to oligo [d(CGCGAATTCGCG)2].2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents.
AID478754Binding affinity to d(CGCGAATTCGCG)2 dodecamer assessed as change in melting temperature2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Theoretical models of pentamidine analogs activity based on their DNA minor groove complexes.
AID269497Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as average days of survival at 20 mg/kg, ip2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID562487Antitrypanosomal activity against Trypanosoma brucei gambiense K03048 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID191632Toxicity is evaluated according to a five-level scale ranging from 0 to 5+ at the specified iv dose of 13.3 (umol/kg/day)1999Journal of medicinal chemistry, Sep-23, Volume: 42, Issue:19
Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan.
AID779102Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mouse survival at 5 mg/kg, ip administered on day 3 post infection for 4 days measured up to 60 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID1235077Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in presence of 30 uM spermine2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.
AID1767951Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation measured after 24 hrs by liquid scintillation counting method
AID551686Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID173671In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 13.3 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID1128530Uncompetitive inhibition of His6x-tagged recombinant PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]SAM and histone H4 (1 to 20) as substrate by double reciprocal plot analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID53470Inhibitory dose against oncornaviral DNA polymerase activity of moloney murine leukemia virus1980Journal of medicinal chemistry, Jul, Volume: 23, Issue:7
Diaryl amidine derivatives as oncornaviral DNA polymerase inhibitors.
AID1146855Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 10 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID249233In vivo antitrypanosomal activity (20 mg/kg for 4 days, i.p.) measured as cured mice infected with Trypanosoma brucei rhodesiense strain STIB900; 0 cured out of 42005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
AID1426421Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense after 70 hrs by Alamar blue assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID124114In vivo average survival rate of mouse infected by T.b. rhodesiense was determined for a period of 60 days at dose of 20 mg/kg by i.p. administration2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID1146852Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 2.5 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID249181Apparent permeability determined across the Caco-2 cell monolayers in both basolateral (BL) to apical (AP) directions2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID173669In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 0.03 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID1128531Inhibition of His6x-tagged recombinant PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) using fluorescein-labeled histone H4 (1 to 20) as substrate at 10 to 50 uM after 8 mins by competitive fluorescence anisotropy binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID372439Antitrypanosomal activity against tbat1 knockout Trypanosoma cruzi BS221 infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID1873842Binding affinity to biotin labeled hairpin DNA 5'-GAATTC-3' (unknown origin) assessed as equilibrium dissociation constant by sensor chip immobilization based surface plasmon resonance analysis2022Bioorganic & medicinal chemistry, 08-15, Volume: 68Drug design and DNA structural research inspired by the Neidle laboratory: DNA minor groove binding and transcription factor inhibition by thiophene diamidines.
AID249190In vitro cytotoxicity evaluated using cultured L6 rat myoblast cells2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
AID779103Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mouse survival at 20 mg/kg, ip administered on day 3 post infection for 4 days measured up to 60 days2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID174181The cysts/g of lung (% of control ) is calculated at a dose of 0.3 umol/kg /day against Pneumocystis carinii in rats1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
AID593435Binding affinity to poly(dA-dT)2DNA assessed as change in melting temperature2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID1128532Inhibition of PRMT1 in human 293T cells assessed as reduction of GFP-ALY methylation by Western blot analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID286672Cytotoxic index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1426412Antiparasitic activity against asexual intraerythrocytic stage of Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID562495Ratio of IC50 for Trypanosoma brucei gambiense ITMAP141267 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9032009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID562488Antitrypanosomal activity against Trypanosoma brucei gambiense ITMAP141267 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID562485Antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID42672In vitro minimum fungicidal concentration against Candida albicans.2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents.
AID1506653Inhibition of PRMT1 (unknown origin) assessed as reduction in methyl transfer from [14C]SAM to biotinylated histone H4 peptide H4-20-Biotin at 0.2 mM incubated for 30 mins by radiometric gel assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
AID382524Toxicity against immunosuppressed rat pneumocystis model at 39.8 umol/kg/day, po2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID212860In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 0.3 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID290096Antiparasitic activity against Trypanosoma cruzi Tulahuen LacZ C42007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID598107Antiparasitic activity against Trypanosoma brucei rhodesiense STIB9002010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
AID243248Ratio of maximum concentration bound and specificity sum for triplex nucleic acids2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Structural selectivity of aromatic diamidines.
AID213471In vitro inhibitory activity against Trypanosoma brucei rhodesiense2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID290098Antitrypanosomal activity in Trypanosoma brucei rhodesiense STIB900 infected mouse at 20 mg/kg, ip administered for 4 days2007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID551685Binding affinity to Poly d(A-T)n DNA assessed as change in melting temperature2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID562514Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as cure from infection at 20 mg/kg, ip for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1506646Inhibition of PRMT5 (unknown origin) assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histone H4 peptide H4-20-Biotin at 100 uM pre-incubated for 3 mins before [3H]-SAM addition and measured after 45 mins by scintillation proximity a2017MedChemComm, Feb-01, Volume: 8, Issue:2
Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
AID564073Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi YuYu after 24 hrs by light microscopy in presence of 50% mouse blood2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID756894Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID228683In vitro binding affinity to poly dA.dT.2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents.
AID454674Selectivity ratio of IC50 for Trypanosoma brucei rhodesiense STIB900 to IC50 for Plasmodium falciparum K12009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID593440Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K12011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID454672Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID756883Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as host mean survival days at 5 mg/kg, ip qd for 4 days2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID322577Antiprotozoal activity against Plasmodium falciparum K1 2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.
AID756893Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID251284In vivo antitrypanosomal activity (20 mg/kg for 4 days, i.p.) measured as survival days of mice infected with Trypanosoma brucei rhodesiense strain STIB9002005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
AID340909Binding affinity to Clostridium perfringens genomic DNA assessed as decrease in fluorescence intensity at 1 uM by fluorescence spectral method relative to control2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID151198In vitro inhibitory activity against Plasmodium falciparum2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID290094Antiparasitic activity against Plasmodium falciparum K12007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID161946The compound was tested in vivo against Pneumocystis carinii pneumonia (PCP) in the immunosuppressed rat model at iv dose of 13.3 (umol/kg/day)1999Journal of medicinal chemistry, Sep-23, Volume: 42, Issue:19
Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan.
AID521059Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity 10 uM after 10 mins2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID551689Antiplasmodial activity against Plasmodium falciparum K1 infected in human RBC after 48 hrs by [3H]-hypoxanthine incorporation assay2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID598109Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
AID598105Binding affinity to poly(dA-dT)n DNA assessed as change in melting temperature at 0.3:1 molar compound/DNA ratio by spectrophotometry2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
AID432049Cytotoxicity against rat L6 cells2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID118270Number of mice (out of 4) cured from Trypanosoma brucei rhodesiense infection which are parasite free for 60 days was determined at i.p. dose of 20 mg/kg2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID562493Ratio of IC50 for melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9012009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID100421Inhibitory activity against Leishmania donovani (amastigote)2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID252577In vivo effect on average days of survival was measured upon intraperitoneal dose at 40 mg/kg in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID1146860Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 320 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID1128526Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID481848Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 in infected mouse model assessed as host survival time at 5 mg/kg, ip for 4 days2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID756892Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma cruzi Tulahuen C2C42013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID1391153Inhibition of recombinant human NQO2 assessed as change in rate of decolouration of DCPIP measured over 1 min by spectrophotometric method2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
Evaluation of analogues of furan-amidines as inhibitors of NQO2.
AID521062Drug uptake in Trypanosoma brucei brucei 427 bloodstream form nucleus at 1 uM after 5 mins by fluorescence microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID269493Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as survival upto 60 days at 20 mg/kg, ip2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID117932In vivo average survival days of mice infected by Trypanosoma brucei rhodesiense was determined for a period of 60 days at i.p. dose of 20 mg/kg2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID286669Antitrypanosomal activity against Trypanosoma brucei rhodesiense2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID562517Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 20 mg/kg, ip for 5 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID454675Cytotoxicity against rat L6 cells2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID521055Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as reduction in mitochondrial membrane potential at 1 uM after 1 min using rhodamine 123 exclusion test2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID1506648Inhibition of PRMT5 (unknown origin) assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histone H4 peptide H4-20-Biotin pre-incubated for 3 mins before [3H]-SAM addition and measured after 45 mins by scintillation proximity assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
AID290099Survival of Trypanosoma brucei rhodesiense STIB900 infected mouse at 20 mg/kg, ip administered for 4 days2007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID481844Antiplasmodial activity against Plasmodium falciparum K12010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID454679Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival days at 5 mg/kg, ip2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID756891Antiprotozoal activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID521056Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as reduction in mitochondrial membrane potential at 10 uM after 1 min using rhodamine 123 exclusion test2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID1128536Antiproliferative activity against human MOLM13 cells with MLL-AF9 translocation assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID565605Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as complete cure from microbial infection at 0.20 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID551688Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID1146859Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 160 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID269498Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as average days of survival at 5 mg/kg, ip2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID212722Toxicity at a dose of 2.7 umol/kg/day against Pneumocystis carinii in rats1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
AID1426427Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID246017In vivo effect (cures) determined by number of mice that survived (0) and are parasite free (8) for 60 days upon intraperitoneal dose, observed in STIB900 mouse model2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID340906Drug level in Trypanosoma brucei brucei S427 at 7.5 uM after 8 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID1426415Oral bioavailability in Swiss Webster mouse at 30 mg/kg2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID382517Antimicrobial activity against Pneumocystis carinii in immunosuppressed rat assessed as number of cysts/g of lung at 13.3 umol/kg/day, iv relative to control2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID1235079Displacement of [3H]-ifenprodil from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.
AID1755260Inhibition of HOXA9 (unknown origin) expressed in reticulocyte lysate system binding to DNA Hoxa9-binding site (5'-biotin-cctctcctctcctGCGATGATTTACGACCGC) (unknown origin) assessed as Hoxa9/DNA remaining complexes at 5 to 10 uM incubated for 20 mins with 2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Heterocyclic Diamidine DNA Ligands as HOXA9 Transcription Factor Inhibitors: Design, Molecular Evaluation, and Cellular Consequences in a HOXA9-Dependant Leukemia Cell Model.
AID55635DNA binding affinity measured as an increase in thermal melting of poly(dA.dT)22003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID756886Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID1146856Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 20 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID322576Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB9002008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.
AID1297654Binding affinity to AT rich 5'-Biotin-DNA (unknown origin) by surface plasmon resonance analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics.
AID1128525Inhibition of His6x-tagged recombinant PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID269490Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB9002006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID1767954Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in mouse assessed as reduction in parasitemia by measuring time taken to cure at 5 mg/kg, ip measured up to 60 days (Rvb = 11 days)
AID1128528Inhibition of His6x-tagged PRMT6 (unknown origin) using [3H]SAM and histone H3.1 as substrate at 20 uM after 1 hr by P81 filter binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID564075Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi CL after 24 hrs by light microscopy in presence of 50% mouse blood2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID340907Drug level in Trypanosoma brucei brucei S427 at 7.5 uM after 24 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID248592In vitro inhibitory activity against Trypanosoma brucei rhodesiense evaluated in acute mouse model of trypanosomiasis2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID562491Antitrypanosomal activity against Trypanosoma brucei brucei AT1KO by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID454680Binding affinity to DNA assessed as change in melting temperature2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID765723Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K12013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID756890Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K12013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID1128524Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate at 20 uM after 8 mins by P81 filter binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID286674Cytotoxic index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K12007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1128527Inhibition of GST-tagged CARM1 (unknown origin) using [3H]SAM and histone H3.1 as substrate at 20 uM after 1 hr by P81 filter binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID286671Cytotoxicity against rat L6 cells2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1062629Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as growth inhibition after 70 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID286673Ratio of cytotoxic index (ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense) of drug to cytotoxic index of furamidine2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1146857Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 40 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID562718Toxicity in NMRI mouse CNS model at 25 mg/kg, ip for 10 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID269492Cytotoxicity against rat L6 cells2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID1146858Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 80 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID1767949Binding affinity to poly (dA-dT) (unknown origin) assessed as thermal stability by measuring change in melting temperature
AID564072Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi Y after 24 hrs by light microscopy in presence of 50% mouse blood2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1532278Inhibition of recombinant human full-length N-terminal His-tagged Tdp1 expressed in Escherichia coli BL212019European journal of medicinal chemistry, Jan-01, Volume: 161Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
AID158689In vitro inhibitory activity for Plasmodium falciparum2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines as antiprotozoal agents.
AID55634DNA binding affinity measured as an increase in thermal melting of d(CGCGAATTCGCG)22003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID1128537Antiproliferative activity against human Jurkat cells assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID598106Cytotoxicity against rat L6 cells2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
AID372438Antitrypanosomal activity against wild type Trypanosoma cruzi BS221 infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID521060Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity at 100 uM after 10 mins2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID54997In vitro binding affinity towards calf thymus (CT DNA)2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID779107Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition after 70 hrs by Alamar blue assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID340903Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID1391154Antimalarial activity against Plasmodium falciparum 3D7 asexual cultures grown under 5% haematocrit assessed as decrease in parasite DNA level by flow cytometry2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
Evaluation of analogues of furan-amidines as inhibitors of NQO2.
AID703983Inhibition of human recombinant Tdp1 assessed as conversion of 14-mer 5'-32P-labeled 3'-phosphotyrosyl DNA substrate N14Y to 14-mer 5'-32P-labeled 3'-phosphate DNA product N14P after 15 mins by PAGE analysis2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl-DNA phosphodiesterase I.
AID562490Antitrypanosomal activity against Trypanosoma brucei brucei BS221 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID237614poly(d(A-T)2) binding affinity is measured as change in DNA melting temperature2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
AID212867In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 2.7 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID673458Inhibition of Tdp12012Journal of medicinal chemistry, 05-10, Volume: 55, Issue:9
Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase I (Tdp1)-topoisomerase I (Top1) inhibitors.
AID765725Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar blue assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID1128523Inhibition of His6x-tagged recombinant PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]SAM and histone H4 (1 to 20) as substrate at 20 uM after 8 mins by P81 filter binding assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID286676Selectivity for chloroquine-resistant Plasmodium falciparum K1 over Trypanosoma brucei rhodesiense2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1767952Selectivity index, ratio of IC50 for cytotoxicity against rat L6 cells to IC50 for antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900
AID1426414Half life in Swiss Webster mouse at 30 mg/kg, po2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID565606Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.20 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID481842Binding affinity to poly(dA.dT) assessed as change in melting temperature by spectrophotometry2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID1426428Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID340905Binding affinity at d(CGCGAATTCGCG) synthetic oligomer duplex assessed as increase in melting temperature2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID226666Cell toxicity was evaluated2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID521047Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of glucose-dependent cellular respiration at 300 uM2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID521046Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of glucose-dependent cellular respiration2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID562504Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival of mouse at 5 mg/kg, ip for 4 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1851332Cytotoxicity against human HeLa cells2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking.
AID1235078Ratio of IC50 for displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor in presence of 30 uM spermine to IC50 for displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor in absence of 30 spermine2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.
AID1128535Antiproliferative activity against human CHRF-288-11 cells harboring trisomy 21 assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID1506651Inhibition of PRMT1 (unknown origin) assessed as reduction in methyl transfer from SAM to biotinylated histone H4 peptide H4-20-Biotin at 0.2 mM incubated for 3.5 hrs by mass spectrometry2017MedChemComm, Feb-01, Volume: 8, Issue:2
Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
AID551687Cytotoxicity against rat L6 cells by alamar blue assay2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID290093Antiparasitic activity against Trypanosoma brucei rhodesiense STIB9002007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID756895Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID598108Antiparasitic activity against Plasmodium falciparum K12010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
AID432047Antileishmanial activity against Leishmania donovani MHOM/SD/62/1S-CL2D amastigotes2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID779106Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID598110Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K12010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.
AID1146861Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 640 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID1426429Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID290095Antiparasitic activity against Leishmania donovani2007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID1235076Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.
AID269494Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as survival upto 60 days at 5 mg/kg, ip2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID593437Antiparasitic activity against Trypanosoma brucei rhodesiense STIB9002011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID212865In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 13.3 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID779108Binding affinity to poly(dA-dT)2 DNA (unknown origin) assessed as change in melting temperature by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID1426413Cmax in Swiss Webster mouse at 30 mg/kg, po2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID562502Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival of mouse at 20 mg/kg, ip for 4 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID174194The cysts/g of lung (% of control ) is calculated at a dose of 2.7 umol/kg/day against Pneumocystis carinii in rats1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
AID521064Drug uptake in Trypanosoma brucei brucei 427 bloodstream form mitochondria at 100 uM after 5 mins by fluorescence microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID521063Drug uptake in Trypanosoma brucei brucei 427 bloodstream form kinetoplast at 1 uM after 5 mins by fluorescence microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID593436Cytotoxicity against rat L6 cells2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID1426423Antiparasitic activity against Giardia lamblia2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID765719Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 5 mg/kg, ip administered for 4 days2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID593471Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 infected in mouse assessed as mean relapse day of parasitemia at 5 mg/kg, ip for 4 days2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID562519Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 10 mg/kg, ip for 10 days2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID562486Antitrypanosomal activity against melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID565604Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as complete cure from microbial infection at 0.25 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID286675Ratio of cytotoxic index (ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1) of drug to cytotoxic index of furamidine2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1506654Inhibition of PRMT1 (unknown origin) assessed as reduction in methyl transfer from [14C]SAM to biotinylated histone H4 peptide H4-20-Biotin at 0.1 mM incubated for 30 mins by radiometric gel assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
AID1398692Inhibition of recombinant Tdp1 (unknown origin) using 5'-(5,6 FAM-aac gtc agg gtc ttc c-BHQ1)-3' as substrate measured every 55 secs for 8 mins by fluorimetric assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Synthesis and evaluation of aryliden- and hetarylidenfuranone derivatives of usnic acid as highly potent Tdp1 inhibitors.
AID340904Binding affinity to poly(dA).poly(dT) assessed as increase in melting temperature2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID213672Inhibitory activity against Trypanosoma cruzi2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID562498Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for Trypanosoma brucei gambiense STIB9302009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID565597Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.125 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID1755301Drug localization in nucleus of mouse MigA9 cells at 20 uM incubated for 2 hrs by TO-PRO-3/propidium iodide staining based by fluorescence microscopy2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Heterocyclic Diamidine DNA Ligands as HOXA9 Transcription Factor Inhibitors: Design, Molecular Evaluation, and Cellular Consequences in a HOXA9-Dependant Leukemia Cell Model.
AID521061Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity pretreated with oligomycin for 10 mins2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID1426425Antiparasitic activity against drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID1146854Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 5 mg/kg relative to control1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles.
AID1062627Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID454678Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival days at 20 mg/kg, ip2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID1426426Antiparasitic activity against drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as growth inhibition after 48 hrs by SYBR green 1 dye-based flow cytometry2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID212704Toxicity at a dose of 0.03 umol/kg/day against Pneumocystis carinii in rats1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
AID551690Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K12011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID1062626Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID173670In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 0.3 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID454673Antiplasmodial activity against Plasmodium falciparum K12009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
AID212707Toxicity at a dose of 0.3 umol/kg/day against Pneumocystis carinii in rats1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
AID243249Ratio of maximum concentration bound and specificity sum for triplex DNA and quadruplex nucleic acids2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Structural selectivity of aromatic diamidines.
AID551691Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as parasitemia free host at 5 mg/kg, ip administered 2 days after post infection for 4 consecutive days measured up to 60 days2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID593438Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID432043Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID42676In vitro minimum inhibitory concentration against Candida albicans.2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents.
AID562494Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9022009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID382523Toxicity against immunosuppressed rat pneumocystis model at 13.3 umol/kg/day, iv2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID162071The compound was tested in vivo against Pneumocystis carinii pneumonia (PCP) in the immunosuppressed rat model at oral dose of 39.8(umol/kg/day)1999Journal of medicinal chemistry, Sep-23, Volume: 42, Issue:19
Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan.
AID562496Ratio of IC50 for Trypanosoma brucei gambiense STIB930 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9042009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID481843Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID1767953Selectivity index, ratio of IC50 for cytotoxicity against rat L6 cells to IC50 for antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 infected in human red blood cells
AID174177The cysts/g of lung (% of control ) is calculated at a dose of 0.03 umol/kg /day against Pneumocystis carinii in rats1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents.
AID1128538Antiproliferative activity against human HL60 cells with PML-RAR alpha translocation assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID322578Cytotoxicity against rat L6 cells2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.
AID551692Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as effect on survival days at 5 mg/kg, ip administered 2 days after post infection for 4 consecutive days measured up to 60 days2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.
AID1426424Antiparasitic activity against Leishmania spp.2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID1851333Cytotoxicity against human HEK293-A cells2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking.
AID1062628Antiplasmodial activity against chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells assessed as [3H]-hypoxanthine incorporation incubated for 48 hrs prior to [3H]-hypoxanthine addition measured after 24 hrs by li2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID1506647Inhibition of PRMT1 (unknown origin) assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histone H4 peptide H4-20-Biotin at 10 uM pre-incubated for 3 mins before [3H]-SAM addition and measured after 15 mins by scintillation proximity as2017MedChemComm, Feb-01, Volume: 8, Issue:2
Discovery of Decamidine as a New and Potent PRMT1 Inhibitor.
AID765724Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID1851331Inhibition of recombinant human TDP1 measured by real-time oligonucleotide biosensor assay2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking.
AID765718Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID432046Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K12009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID1532281Binding affinity to recombinant human Tdp1 (149 to 608 residues) expressed in Escherichia coli BL21 (DE3) by tryptophan fluorescence quenching assay2019European journal of medicinal chemistry, Jan-01, Volume: 161Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
AID38040Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation2002Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
Distribution of furamidine analogues in tumor cells: influence of the number of positive charges.
AID593439Antiparasitic activity against Plasmodium falciparum K12011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.
AID765722Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K12013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID322575Binding affinity to poly(dA-dT) DNA2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.
AID248239In vitro antiprotozoal activity against Trypanosoma brucei rhodesiense strain STIB9002005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
AID562484Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1767950Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 measured after 72 hrs by alamar blue dye based fluorimetry analysis
AID269491Antiprotozoal activity against Plasmodium falciparum K12006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.
AID562489Antitrypanosomal activity against Trypanosoma brucei gambiense STIB930 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1426422Antitrypanosomal activity against Trypanosoma cruzi after 70 hrs by Alamar blue assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum.
AID340902Antitrypanosomal activity against Trypanosoma brucei brucei S427 after 72 hrs2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
AID1685557Inhibition of recombinant human His-tagged PRMT1 expressed in Escherichia coli BL21 (DE3) using biotin-labeled histone H4-20 as substrate incubated for 8 mins in presence of [3H]-SAM cofactor by scintillation proximity assay2021RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
Pharmacophore-based screening of diamidine small molecule inhibitors for protein arginine methyltransferases.
AID1062617Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 5 mg/kg, ip qd administered for 4 days2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID1767948Cytotoxicity against rat L6 cells by Alamar blue assay
AID290097Cytotoxicity against rat L6 cells by alamar blue assay2007European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
AID124386No. of mice that survived T.b. rhodesiense infection and are parasite free for 60 days was determined at dose of 20 mg/kg by i.p. administration; 4 animals tested2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID212858In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 0.03 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID565599Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.0625 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID562492Ratio of IC50 for pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9002009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID162419In vitro binding affinity towards Poly (dA-dT)22003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID564074Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi Columbian after 24 hrs by light microscopy in presence of 50% mouse blood2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID521058Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity at 50 uM after 10 mins2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID432045Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID521049Inhibition of respiration in Trypanosoma brucei brucei 427 bloodstream form mitochondria using glycerol-3-phosphate as substrate at 600 uM2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
The mitochondrion is a site of trypanocidal action of the aromatic diamidine DB75 in bloodstream forms of Trypanosoma brucei.
AID1128533Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID565603Antimicrobial activity against Trypanosoma evansi STIB 806K infected in NMRI mouse assessed as host survival days at 0.25 mg/kg, ip administered 3 to 6 days after infection for 4 consecutive days2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.
AID779109Antiplasmodial activity against Plasmodium falciparum K1 assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
AID247973In vitro antiprotozoal activity for Plasmodium falciparum K12005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
AID1128529Competitive inhibition of His6x-tagged recombinant PRMT1 (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]SAM and histone H4 (1 to 20) as substrate by double reciprocal plot analysis2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID208055In vitro inhibitory activity against T. b. rhodesiense2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Synthesis and antiprotozoal activity of aza-analogues of furamidine.
AID1128534Antiproliferative activity against human CMY cells harboring trisomy 21 assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
AID191637Toxicity is evaluated according to a five-level scale ranging from 0 to 5+ at the specified oral dose of 39.8 (umol/kg/day)1999Journal of medicinal chemistry, Sep-23, Volume: 42, Issue:19
Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan.
AID173672In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 2.7 umol/kg/day1998Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents.
AID382518Antimicrobial activity against Pneumocystis carinii in immunosuppressed rat assessed as number of cysts/g of lung at 39.8 umol/kg/day, po relative to control2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Carbamate prodrugs of N-alkylfuramidines.
AID562497Ratio of IC50 for Trypanosoma brucei brucei AT1KO to IC50 for Trypanosoma brucei brucei BS2212009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID100423Inhibitory activity against Leishmania donovani (macrophage); Not determined2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID481845Cytotoxicity against rat L6 cells2010Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.
AID432044Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID249180Apparent permeability determined across the Caco-2 cell monolayers in both apical (AP) to basolateral (BL) directions2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
O-alkoxyamidine prodrugs of furamidine: in vitro transport and microsomal metabolism as indicators of in vivo efficacy in a mouse model of Trypanosoma brucei rhodesiense infection.
AID286670Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K12007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID1062625Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID1532280Inhibition of recombinant human full-length N-terminal His-tagged Tdp1 expressed in Escherichia coli BL21 (DE3) using 5'-(5,6 FAM-aac gtc agg gtc ttc c-BHQ1)-3' as substrate measured every 1 min for 7 mins by fluorimetric method2019European journal of medicinal chemistry, Jan-01, Volume: 161Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (108)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (3.70)18.7374
1990's10 (9.26)18.2507
2000's56 (51.85)29.6817
2010's31 (28.70)24.3611
2020's7 (6.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.79

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.79 (24.57)
Research Supply Index4.70 (2.92)
Research Growth Index5.17 (4.65)
Search Engine Demand Index32.40 (26.88)
Search Engine Supply Index1.83 (0.95)

This Compound (29.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.93%)5.53%
Reviews3 (2.78%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other104 (96.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]