Synthesis and in vitro leishmanicidal activity of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles.
A series of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles (5a-d and 6a-j) were synthesized and evaluated against Leishmania major promastigotes using (3)H-thymidine incorporation. Most of the compounds showed activity better than the reference drug sodium stibogluconate (Pentostam). The most active compound was 6c (IC(50)=0.1 microM).
Foroumadi
Alireza
A
Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman 76351, Iran.
Pournourmohammadi
Shirin
S
Soltani
Fatemeh
F
Asgharian-Rezaee
Mitra
M
Dabiri
Shahriar
S
Kharazmi
Arsalan
A
Shafiee
Abbas
A
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D018320:Leishmania major / Q000187:drug effects* / Q000254:growth & development*; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000981:Antiprotozoal Agents; D013830:Thiadiazoles