Assay ID | Title | Year | Journal | Article |
AID1368578 | Antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Swiss Webster mouse assessed as infection cure rate at 25 mg/kg, po qd for 7 days starting 21 days post-infection (Rvb = 0%) | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides. |
AID1774613 | Antileishmanial activity against promastigote form of Leishmania donovani overexpressing Asn232His-mutant of CPSF3 | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
AID1435177 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 50 to 51 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1774614 | Antileishmanial activity against promastigote form of Leishmania donovani overexpressing wild-type CPSF3 | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
AID1435176 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 43 to 45 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID739090 | Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei Lister 427 after 48 hrs by hemocytometer | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis. |
AID1850422 | AUC (0 to 24 hrs) in rat at 25 mg/kg, po | 2022 | Bioorganic & medicinal chemistry, 06-01, Volume: 63 | Boron-Containing heterocycles as promising pharmacological agents. |
AID1368443 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream forms | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides. |
AID1435172 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 40 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1435171 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 41 to 42 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1454780 | Antitrypanosomal activity against Trypanosoma brucei brucei after 72 hrs by resazurin-based fluorescence assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
| Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry. |
AID1435175 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 39 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1435168 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 35 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1575040 | Trypanocidal activity against Trypanosoma brucei brucei 427 assessed as 50% bacterial killing at 7.2 uM preincubated for 6 hrs followed by compound washout and measured after 48 hrs by hemocytometric method | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development. |
AID1774520 | Antileishmanial activity against amastigote stage of Leishmania donovani MHOM/ET/67/L82 infected in mouse peritoneal macrophage assessed as reduction in parasite burden incubated for 5 days by Giemsa staining based microscopic analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
AID1435169 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 36 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1435170 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 46 to 49 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1435173 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 37 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1774519 | Antileishmanial activity against amastigote stage of Leishmania infantum MHOM/MA(BE)/67/ITMAP263 infected in mouse peritoneal macrophage assessed as reduction in parasite burden incubated for 5 days by Giemsa staining based microscopic analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
AID1368588 | Time duration during which drug level in brain stays at or above MIC for antitrypanosomal activity against Trypanosoma brucei brucei TREU 667 infected in Webster mouse at 25 mg/kg, po bid | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
| Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides. |
AID1575028 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 after 48 hrs by PrestoBlue dye based fluorescence assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
| Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development. |
AID1774612 | Antileishmanial activity against promastigote form of wild-type Leishmania donovani | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
AID1435174 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 38 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1435178 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 52 to 180 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1850421 | Cmax in rat at 25 mg/kg, po | 2022 | Bioorganic & medicinal chemistry, 06-01, Volume: 63 | Boron-Containing heterocycles as promising pharmacological agents. |
AID1435167 | Antiparasitic activity against Trypanosoma brucei brucei TREU667 infected in mouse assessed as decrease in parasitemia at 50 mg/kg, bid administered via oral gavage on day 21 to 34 post infection measured on day 34 by microscopic method | 2017 | Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
| Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. |
AID1774518 | Cytotoxicity against mouse primary peritoneal macrophages measured after 3 days by resazurin staining based fluorometric analysis | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
AID1774615 | Antitrypanosomal activity against bloodstream form of trypanosoma brucei brucei 427 assessed as reduction in parasitic growth after 72 hrs by resazurin staining based fluorescence assay | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |