Assay ID | Title | Year | Journal | Article |
AID322579 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected mouse model assessed as survival at 5 mg/kg, ip after 4 days | 2008 | Bioorganic & 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. |
AID372440 | Resistance factor, ratio of IC50 for tbat1 knock out Trypanosoma cruzi BS221 to IC50 for wild type Trypanosoma cruzi BS221 | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| 2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. |
AID228684 | In vitro DNA binding affinity to oligo [d(CGCGAATTCGCG)2]. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents. |
AID478754 | Binding affinity to d(CGCGAATTCGCG)2 dodecamer assessed as change in melting temperature | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5
| Theoretical models of pentamidine analogs activity based on their DNA minor groove complexes. |
AID269497 | Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as average days of survival at 20 mg/kg, ip | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID562487 | Antitrypanosomal activity against Trypanosoma brucei gambiense K03048 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID191632 | Toxicity is evaluated according to a five-level scale ranging from 0 to 5+ at the specified iv dose of 13.3 (umol/kg/day) | 1999 | Journal 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. |
AID779102 | Antitrypanosomal 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 days | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. |
AID1235077 | Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in presence of 30 uM spermine | 2015 | Bioorganic & 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. |
AID1767951 | Antiplasmodial 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 | | | |
AID551686 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID173671 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 13.3 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID1128530 | Uncompetitive 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 analysis | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID53470 | Inhibitory dose against oncornaviral DNA polymerase activity of moloney murine leukemia virus | 1980 | Journal of medicinal chemistry, Jul, Volume: 23, Issue:7
| Diaryl amidine derivatives as oncornaviral DNA polymerase inhibitors. |
AID1146855 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 10 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID249233 | In 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 4 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs. |
AID1426421 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense after 70 hrs by Alamar blue assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID124114 | In 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. administration | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Synthesis and antiprotozoal activity of aza-analogues of furamidine. |
AID1146852 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 2.5 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID249181 | Apparent permeability determined across the Caco-2 cell monolayers in both basolateral (BL) to apical (AP) directions | 2004 | Journal 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. |
AID173669 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 0.03 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID1128531 | Inhibition 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID372439 | Antitrypanosomal activity against tbat1 knockout Trypanosoma cruzi BS221 infected in mouse macrophage by reporter dye assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| 2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. |
AID1873842 | Binding affinity to biotin labeled hairpin DNA 5'-GAATTC-3' (unknown origin) assessed as equilibrium dissociation constant by sensor chip immobilization based surface plasmon resonance analysis | 2022 | Bioorganic & medicinal chemistry, 08-15, Volume: 68 | Drug design and DNA structural research inspired by the Neidle laboratory: DNA minor groove binding and transcription factor inhibition by thiophene diamidines. |
AID249190 | In vitro cytotoxicity evaluated using cultured L6 rat myoblast cells | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs. |
AID779103 | Antitrypanosomal 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 days | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. |
AID174181 | The cysts/g of lung (% of control ) is calculated at a dose of 0.3 umol/kg /day against Pneumocystis carinii in rats | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents. |
AID593435 | Binding affinity to poly(dA-dT)2DNA assessed as change in melting temperature | 2011 | Bioorganic & 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. |
AID1128532 | Inhibition of PRMT1 in human 293T cells assessed as reduction of GFP-ALY methylation by Western blot analysis | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID286672 | Cytotoxic index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1426412 | Antiparasitic activity against asexual intraerythrocytic stage of Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID562495 | Ratio of IC50 for Trypanosoma brucei gambiense ITMAP141267 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB903 | 2009 | Antimicrobial 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. |
AID562488 | Antitrypanosomal activity against Trypanosoma brucei gambiense ITMAP141267 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID562485 | Antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID42672 | In vitro minimum fungicidal concentration against Candida albicans. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents. |
AID1506653 | Inhibition 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 assay | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. |
AID382524 | Toxicity against immunosuppressed rat pneumocystis model at 39.8 umol/kg/day, po | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
| Carbamate prodrugs of N-alkylfuramidines. |
AID212860 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 0.3 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID290096 | Antiparasitic activity against Trypanosoma cruzi Tulahuen LacZ C4 | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID598107 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
| Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. |
AID243248 | Ratio of maximum concentration bound and specificity sum for triplex nucleic acids | 2004 | Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
| Structural selectivity of aromatic diamidines. |
AID213471 | In vitro inhibitory activity against Trypanosoma brucei rhodesiense | 2004 | Journal 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. |
AID290098 | Antitrypanosomal activity in Trypanosoma brucei rhodesiense STIB900 infected mouse at 20 mg/kg, ip administered for 4 days | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID551685 | Binding affinity to Poly d(A-T)n DNA assessed as change in melting temperature | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID562514 | Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as cure from infection at 20 mg/kg, ip for 5 days | 2009 | Antimicrobial 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. |
AID1506646 | Inhibition 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 a | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. |
AID564073 | Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi YuYu after 24 hrs by light microscopy in presence of 50% mouse blood | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment. |
AID756894 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID228683 | In vitro binding affinity to poly dA.dT. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents. |
AID454674 | Selectivity ratio of IC50 for Trypanosoma brucei rhodesiense STIB900 to IC50 for Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID593440 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2011 | Bioorganic & 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. |
AID454672 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID756883 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as host mean survival days at 5 mg/kg, ip qd for 4 days | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID322577 | Antiprotozoal activity against Plasmodium falciparum K1 | 2008 | Bioorganic & 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. |
AID756893 | Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID251284 | In vivo antitrypanosomal activity (20 mg/kg for 4 days, i.p.) measured as survival days of mice infected with Trypanosoma brucei rhodesiense strain STIB900 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs. |
AID340909 | Binding affinity to Clostridium perfringens genomic DNA assessed as decrease in fluorescence intensity at 1 uM by fluorescence spectral method relative to control | 2007 | Antimicrobial 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. |
AID151198 | In vitro inhibitory activity against Plasmodium falciparum | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Synthesis and antiprotozoal activity of aza-analogues of furamidine. |
AID290094 | Antiparasitic activity against Plasmodium falciparum K1 | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID161946 | The compound was tested in vivo against Pneumocystis carinii pneumonia (PCP) in the immunosuppressed rat model at iv dose of 13.3 (umol/kg/day) | 1999 | Journal 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. |
AID521059 | Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity 10 uM after 10 mins | 2008 | Antimicrobial 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. |
AID551689 | Antiplasmodial activity against Plasmodium falciparum K1 infected in human RBC after 48 hrs by [3H]-hypoxanthine incorporation assay | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID598109 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
| Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. |
AID598105 | Binding affinity to poly(dA-dT)n DNA assessed as change in melting temperature at 0.3:1 molar compound/DNA ratio by spectrophotometry | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
| Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. |
AID432049 | Cytotoxicity against rat L6 cells | 2009 | European 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. |
AID118270 | Number 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/kg | 2004 | Journal 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. |
AID562493 | Ratio of IC50 for melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB901 | 2009 | Antimicrobial 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. |
AID100421 | Inhibitory activity against Leishmania donovani (amastigote) | 2003 | Bioorganic & 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. |
AID252577 | In vivo effect on average days of survival was measured upon intraperitoneal dose at 40 mg/kg in STIB900 mouse model | 2004 | Journal 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. |
AID1146860 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 320 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID1128526 | Inhibition 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID481848 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 in infected mouse model assessed as host survival time at 5 mg/kg, ip for 4 days | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles. |
AID756892 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma cruzi Tulahuen C2C4 | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID1391153 | Inhibition of recombinant human NQO2 assessed as change in rate of decolouration of DCPIP measured over 1 min by spectrophotometric method | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| Evaluation of analogues of furan-amidines as inhibitors of NQO2. |
AID521062 | Drug uptake in Trypanosoma brucei brucei 427 bloodstream form nucleus at 1 uM after 5 mins by fluorescence microscopy | 2008 | Antimicrobial 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. |
AID269493 | Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as survival upto 60 days at 20 mg/kg, ip | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID117932 | In 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/kg | 2004 | Journal 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. |
AID286669 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID562517 | Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 20 mg/kg, ip for 5 days | 2009 | Antimicrobial 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. |
AID454675 | Cytotoxicity against rat L6 cells | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID521055 | Antimicrobial 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 test | 2008 | Antimicrobial 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. |
AID1506648 | Inhibition 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 assay | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. |
AID290099 | Survival of Trypanosoma brucei rhodesiense STIB900 infected mouse at 20 mg/kg, ip administered for 4 days | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID481844 | Antiplasmodial activity against Plasmodium falciparum K1 | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles. |
AID454679 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival days at 5 mg/kg, ip | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID756891 | Antiprotozoal activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by [3H]-hypoxanthine incorporation assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID521056 | Antimicrobial 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 test | 2008 | Antimicrobial 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. |
AID1128536 | Antiproliferative activity against human MOLM13 cells with MLL-AF9 translocation assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID565605 | Antimicrobial 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 days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID551688 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID1146859 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 160 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID269498 | Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as average days of survival at 5 mg/kg, ip | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID212722 | Toxicity at a dose of 2.7 umol/kg/day against Pneumocystis carinii in rats | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents. |
AID1426427 | Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID246017 | In 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 model | 2004 | Journal 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. |
AID340906 | Drug level in Trypanosoma brucei brucei S427 at 7.5 uM after 8 hrs | 2007 | Antimicrobial 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. |
AID1426415 | Oral bioavailability in Swiss Webster mouse at 30 mg/kg | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID382517 | Antimicrobial activity against Pneumocystis carinii in immunosuppressed rat assessed as number of cysts/g of lung at 13.3 umol/kg/day, iv relative to control | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
| Carbamate prodrugs of N-alkylfuramidines. |
AID1235079 | Displacement of [3H]-ifenprodil from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine | 2015 | Bioorganic & 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. |
AID1755260 | Inhibition 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 | 2019 | Journal 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. |
AID55635 | DNA binding affinity measured as an increase in thermal melting of poly(dA.dT)2 | 2003 | Bioorganic & 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. |
AID756886 | Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID1146856 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 20 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID322576 | Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB900 | 2008 | Bioorganic & 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. |
AID1297654 | Binding affinity to AT rich 5'-Biotin-DNA (unknown origin) by surface plasmon resonance analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics. |
AID1128525 | 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 after 8 mins by P81 filter binding assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID269490 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID1767954 | Antitrypanosomal 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) | | | |
AID1128528 | Inhibition 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID564075 | Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi CL after 24 hrs by light microscopy in presence of 50% mouse blood | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment. |
AID340907 | Drug level in Trypanosoma brucei brucei S427 at 7.5 uM after 24 hrs | 2007 | Antimicrobial 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. |
AID248592 | In vitro inhibitory activity against Trypanosoma brucei rhodesiense evaluated in acute mouse model of trypanosomiasis | 2004 | Journal 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. |
AID562491 | Antitrypanosomal activity against Trypanosoma brucei brucei AT1KO by Alamar blue assay | 2009 | Antimicrobial 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. |
AID454680 | Binding affinity to DNA assessed as change in melting temperature | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID765723 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID756890 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID1128524 | Inhibition 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID286674 | Cytotoxic index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1128527 | Inhibition 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID286671 | Cytotoxicity against rat L6 cells | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1062629 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as growth inhibition after 70 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID286673 | Ratio of cytotoxic index (ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense) of drug to cytotoxic index of furamidine | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1146857 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 40 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID562718 | Toxicity in NMRI mouse CNS model at 25 mg/kg, ip for 10 days | 2009 | Antimicrobial 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. |
AID269492 | Cytotoxicity against rat L6 cells | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID1146858 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 80 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID1767949 | Binding affinity to poly (dA-dT) (unknown origin) assessed as thermal stability by measuring change in melting temperature | | | |
AID564072 | Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi Y after 24 hrs by light microscopy in presence of 50% mouse blood | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment. |
AID1532278 | Inhibition of recombinant human full-length N-terminal His-tagged Tdp1 expressed in Escherichia coli BL21 | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models. |
AID158689 | In vitro inhibitory activity for Plasmodium falciparum | 2004 | Journal 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. |
AID55634 | DNA binding affinity measured as an increase in thermal melting of d(CGCGAATTCGCG)2 | 2003 | Bioorganic & 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. |
AID1128537 | Antiproliferative activity against human Jurkat cells assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID598106 | Cytotoxicity against rat L6 cells | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
| Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. |
AID372438 | Antitrypanosomal activity against wild type Trypanosoma cruzi BS221 infected in mouse macrophage by reporter dye assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| 2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities. |
AID521060 | Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity at 100 uM after 10 mins | 2008 | Antimicrobial 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. |
AID54997 | In vitro binding affinity towards calf thymus (CT DNA) | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Synthesis and antiprotozoal activity of aza-analogues of furamidine. |
AID779107 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition after 70 hrs by Alamar blue assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. |
AID340903 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs | 2007 | Antimicrobial 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. |
AID1391154 | Antimalarial activity against Plasmodium falciparum 3D7 asexual cultures grown under 5% haematocrit assessed as decrease in parasite DNA level by flow cytometry | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
| Evaluation of analogues of furan-amidines as inhibitors of NQO2. |
AID703983 | Inhibition 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 analysis | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
| 5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl-DNA phosphodiesterase I. |
AID562490 | Antitrypanosomal activity against Trypanosoma brucei brucei BS221 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID237614 | poly(d(A-T)2) binding affinity is measured as change in DNA melting temperature | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs. |
AID212867 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 2.7 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID673458 | Inhibition of Tdp1 | 2012 | Journal 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. |
AID765725 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar blue assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID1128523 | 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 at 20 uM after 8 mins by P81 filter binding assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID286676 | Selectivity for chloroquine-resistant Plasmodium falciparum K1 over Trypanosoma brucei rhodesiense | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1767952 | Selectivity index, ratio of IC50 for cytotoxicity against rat L6 cells to IC50 for antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | | | |
AID1426414 | Half life in Swiss Webster mouse at 30 mg/kg, po | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID565606 | Antimicrobial 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 days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID481842 | Binding affinity to poly(dA.dT) assessed as change in melting temperature by spectrophotometry | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles. |
AID1426428 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID340905 | Binding affinity at d(CGCGAATTCGCG) synthetic oligomer duplex assessed as increase in melting temperature | 2007 | Antimicrobial 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. |
AID226666 | Cell toxicity was evaluated | 2003 | Bioorganic & 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. |
AID521047 | Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of glucose-dependent cellular respiration at 300 uM | 2008 | Antimicrobial 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. |
AID521046 | Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of glucose-dependent cellular respiration | 2008 | Antimicrobial 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. |
AID562504 | Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival of mouse at 5 mg/kg, ip for 4 days | 2009 | Antimicrobial 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. |
AID1851332 | Cytotoxicity against human HeLa cells | 2022 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 73 | Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking. |
AID1235078 | Ratio 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 spermine | 2015 | Bioorganic & 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. |
AID1128535 | Antiproliferative 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID1506651 | Inhibition 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 spectrometry | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. |
AID551687 | Cytotoxicity against rat L6 cells by alamar blue assay | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID290093 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID756895 | Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
| Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives. |
AID598108 | Antiparasitic activity against Plasmodium falciparum K1 | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
| Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. |
AID432047 | Antileishmanial activity against Leishmania donovani MHOM/SD/62/1S-CL2D amastigotes | 2009 | European 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. |
AID779106 | Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. |
AID598110 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
| Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines. |
AID1146861 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 640 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID1426429 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID290095 | Antiparasitic activity against Leishmania donovani | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID1235076 | Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta counting analysis in absence of spermine | 2015 | Bioorganic & 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. |
AID269494 | Antiprotozoal activity in mouse infected with Trypanosoma brucei rhodesiense STIB900 measured as survival upto 60 days at 5 mg/kg, ip | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID593437 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 | 2011 | Bioorganic & 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. |
AID212865 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 13.3 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID779108 | Binding affinity to poly(dA-dT)2 DNA (unknown origin) assessed as change in melting temperature by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. |
AID1426413 | Cmax in Swiss Webster mouse at 30 mg/kg, po | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID562502 | Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival of mouse at 20 mg/kg, ip for 4 days | 2009 | Antimicrobial 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. |
AID174194 | The cysts/g of lung (% of control ) is calculated at a dose of 2.7 umol/kg/day against Pneumocystis carinii in rats | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents. |
AID521064 | Drug uptake in Trypanosoma brucei brucei 427 bloodstream form mitochondria at 100 uM after 5 mins by fluorescence microscopy | 2008 | Antimicrobial 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. |
AID521063 | Drug uptake in Trypanosoma brucei brucei 427 bloodstream form kinetoplast at 1 uM after 5 mins by fluorescence microscopy | 2008 | Antimicrobial 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. |
AID593436 | Cytotoxicity against rat L6 cells | 2011 | Bioorganic & 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. |
AID1426423 | Antiparasitic activity against Giardia lamblia | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID765719 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 5 mg/kg, ip administered for 4 days | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID593471 | Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 infected in mouse assessed as mean relapse day of parasitemia at 5 mg/kg, ip for 4 days | 2011 | Bioorganic & 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. |
AID562519 | Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse CNS model assessed as survival of mouse at 10 mg/kg, ip for 10 days | 2009 | Antimicrobial 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. |
AID562486 | Antitrypanosomal activity against melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID565604 | Antimicrobial 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 days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID286675 | Ratio of cytotoxic index (ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1) of drug to cytotoxic index of furamidine | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1506654 | Inhibition 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 assay | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. |
AID1398692 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
| Synthesis and evaluation of aryliden- and hetarylidenfuranone derivatives of usnic acid as highly potent Tdp1 inhibitors. |
AID340904 | Binding affinity to poly(dA).poly(dT) assessed as increase in melting temperature | 2007 | Antimicrobial 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. |
AID213672 | Inhibitory activity against Trypanosoma cruzi | 2003 | Bioorganic & 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. |
AID562498 | Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for Trypanosoma brucei gambiense STIB930 | 2009 | Antimicrobial 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. |
AID565597 | Antimicrobial 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 days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID1755301 | Drug localization in nucleus of mouse MigA9 cells at 20 uM incubated for 2 hrs by TO-PRO-3/propidium iodide staining based by fluorescence microscopy | 2019 | Journal 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. |
AID521061 | Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity pretreated with oligomycin for 10 mins | 2008 | Antimicrobial 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. |
AID1426425 | Antiparasitic activity against drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID1146854 | Antitrypanosomal activity against Trypanosoma rhodesiense infected in mouse assessed as increase in survival time by 30 days at 5 mg/kg relative to control | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
| Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)thiophenes and -pyrroles. |
AID1062627 | Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID454678 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival days at 20 mg/kg, ip | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID1426426 | Antiparasitic activity against drug-sensitive Plasmodium falciparum 3D7 infected in erythrocytes assessed as growth inhibition after 48 hrs by SYBR green 1 dye-based flow cytometry | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID212704 | Toxicity at a dose of 0.03 umol/kg/day against Pneumocystis carinii in rats | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents. |
AID551690 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K1 | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID1062626 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID173670 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 0.3 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID454673 | Antiplasmodial activity against Plasmodium falciparum K1 | 2009 | Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
| Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum. |
AID212707 | Toxicity at a dose of 0.3 umol/kg/day against Pneumocystis carinii in rats | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents. |
AID243249 | Ratio of maximum concentration bound and specificity sum for triplex DNA and quadruplex nucleic acids | 2004 | Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
| Structural selectivity of aromatic diamidines. |
AID551691 | Antitrypanosomal 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 days | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID593438 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2011 | Bioorganic & 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. |
AID432043 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2009 | European 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. |
AID42676 | In vitro minimum inhibitory concentration against Candida albicans. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents. |
AID562494 | Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB902 | 2009 | Antimicrobial 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. |
AID382523 | Toxicity against immunosuppressed rat pneumocystis model at 13.3 umol/kg/day, iv | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
| Carbamate prodrugs of N-alkylfuramidines. |
AID162071 | The compound was tested in vivo against Pneumocystis carinii pneumonia (PCP) in the immunosuppressed rat model at oral dose of 39.8(umol/kg/day) | 1999 | Journal 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. |
AID562496 | Ratio of IC50 for Trypanosoma brucei gambiense STIB930 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB904 | 2009 | Antimicrobial 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. |
AID481843 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles. |
AID1767953 | Selectivity 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 | | | |
AID174177 | The cysts/g of lung (% of control ) is calculated at a dose of 0.03 umol/kg /day against Pneumocystis carinii in rats | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| 2,5-bis[4-(N-alkylamidino)phenyl]furans as anti-Pneumocystis carinii agents. |
AID1128538 | Antiproliferative 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 assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID322578 | Cytotoxicity against rat L6 cells | 2008 | Bioorganic & 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. |
AID551692 | Antitrypanosomal 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 days | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents. |
AID1426424 | Antiparasitic activity against Leishmania spp. | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID1851333 | Cytotoxicity against human HEK293-A cells | 2022 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 73 | Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking. |
AID1062628 | Antiplasmodial 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 li | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID1506647 | Inhibition 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 as | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. |
AID765724 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID1851331 | Inhibition of recombinant human TDP1 measured by real-time oligonucleotide biosensor assay | 2022 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 73 | Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking. |
AID765718 | Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID432046 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2009 | European 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. |
AID1532281 | Binding affinity to recombinant human Tdp1 (149 to 608 residues) expressed in Escherichia coli BL21 (DE3) by tryptophan fluorescence quenching assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models. |
AID38040 | Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Distribution of furamidine analogues in tumor cells: influence of the number of positive charges. |
AID593439 | Antiparasitic activity against Plasmodium falciparum K1 | 2011 | Bioorganic & 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. |
AID765722 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives. |
AID322575 | Binding affinity to poly(dA-dT) DNA | 2008 | Bioorganic & 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. |
AID248239 | In vitro antiprotozoal activity against Trypanosoma brucei rhodesiense strain STIB900 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs. |
AID562484 | Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID1767950 | Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 measured after 72 hrs by alamar blue dye based fluorimetry analysis | | | |
AID269491 | Antiprotozoal activity against Plasmodium falciparum K1 | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues. |
AID562489 | Antitrypanosomal activity against Trypanosoma brucei gambiense STIB930 by Alamar blue assay | 2009 | Antimicrobial 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. |
AID1426422 | Antitrypanosomal activity against Trypanosoma cruzi after 70 hrs by Alamar blue assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. |
AID340902 | Antitrypanosomal activity against Trypanosoma brucei brucei S427 after 72 hrs | 2007 | Antimicrobial 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. |
AID1685557 | Inhibition 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 assay | 2021 | RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1
| Pharmacophore-based screening of diamidine small molecule inhibitors for protein arginine methyltransferases. |
AID1062617 | Trypanocidal 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 days | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID1767948 | Cytotoxicity against rat L6 cells by Alamar blue assay | | | |
AID290097 | Cytotoxicity against rat L6 cells by alamar blue assay | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes. |
AID124386 | No. 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 tested | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Synthesis and antiprotozoal activity of aza-analogues of furamidine. |
AID212858 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in rats measured 0.03 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID565599 | Antimicrobial 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 days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID562492 | Ratio of IC50 for pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB900 | 2009 | Antimicrobial 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. |
AID162419 | In vitro binding affinity towards Poly (dA-dT)2 | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Synthesis and antiprotozoal activity of aza-analogues of furamidine. |
AID564074 | Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi Columbian after 24 hrs by light microscopy in presence of 50% mouse blood | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment. |
AID521058 | Antimicrobial activity against Trypanosoma brucei brucei 427 bloodstream form assessed as inhibition of mitochondrial ATPase activity at 50 uM after 10 mins | 2008 | Antimicrobial 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. |
AID432045 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 | 2009 | European 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. |
AID521049 | Inhibition of respiration in Trypanosoma brucei brucei 427 bloodstream form mitochondria using glycerol-3-phosphate as substrate at 600 uM | 2008 | Antimicrobial 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. |
AID1128533 | Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID565603 | Antimicrobial 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 days | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model. |
AID779109 | Antiplasmodial activity against Plasmodium falciparum K1 assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues. |
AID247973 | In vitro antiprotozoal activity for Plasmodium falciparum K1 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs. |
AID1128529 | Competitive 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 analysis | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID208055 | In vitro inhibitory activity against T. b. rhodesiense | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Synthesis and antiprotozoal activity of aza-analogues of furamidine. |
AID1128534 | Antiproliferative activity against human CMY cells harboring trisomy 21 assessed as cell viability at 20 uM measured everyday for 3 days by CellTiter-Glo assay | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
| Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. |
AID191637 | Toxicity is evaluated according to a five-level scale ranging from 0 to 5+ at the specified oral dose of 39.8 (umol/kg/day) | 1999 | Journal 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. |
AID173672 | In vivo evaluation of iv dosage of the Dicationic furans against Pneumocystis carinii in lung tissue of rats at 2.7 umol/kg/day | 1998 | Journal of medicinal chemistry, Sep-24, Volume: 41, Issue:20
| Extended aromatic furan amidino derivatives as anti-Pneumocystis carinii agents. |
AID382518 | Antimicrobial activity against Pneumocystis carinii in immunosuppressed rat assessed as number of cysts/g of lung at 39.8 umol/kg/day, po relative to control | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
| Carbamate prodrugs of N-alkylfuramidines. |
AID562497 | Ratio of IC50 for Trypanosoma brucei brucei AT1KO to IC50 for Trypanosoma brucei brucei BS221 | 2009 | Antimicrobial 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. |
AID100423 | Inhibitory activity against Leishmania donovani (macrophage); Not determined | 2003 | Bioorganic & 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. |
AID481845 | Cytotoxicity against rat L6 cells | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles. |
AID432044 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 | 2009 | European 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. |
AID249180 | Apparent permeability determined across the Caco-2 cell monolayers in both apical (AP) to basolateral (BL) directions | 2004 | Journal 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. |
AID286670 | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
| Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles. |
AID1062625 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 infected in human red blood cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues. |
AID1532280 | Inhibition 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 method | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Novel 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] |