Synthesis and in vitro leishmanicidal activity of 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-substituted-1,3,4-thiadiazole derivatives.
A series of 2-(1-methyl-5-nitroimidazol-2-yl)-5-(1-piperazinyl, 1-piperidinyl and 1-morpholinyl)-1,3,4-thiadiazoles (3a-g) were synthesized and evaluated for in vitro leishmanicidal activity against Leishmania major promastigotes. The leishmanicidal data revealed that compounds 3a-g had strong and much better leishmanicidal activity than the reference drug pentostam. Compound 3c (piperazine analog) was the most active compound (IC50=0.19 microM).
Foroumadi
Alireza
A
Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Tehran University of Medical Science, Tehran 14174, Iran. aforoumadi@yahoo.com
Emami
Saeed
S
Pournourmohammadi
Shirin
S
Kharazmi
Arsalan
A
Shafiee
Abbas
A
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D018320:Leishmania major / Q000187:drug effects* / Q000378:metabolism*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000981:Antiprotozoal Agents; D013830:Thiadiazoles