Tehran University of Medical Sciences
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Abbas Shafiee

Synthesis and in vitro leishmanicidal activity of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles.


Authors: Foroumadi A , Pournourmohammadi S , Soltani F , Asgharian-Rezaee M , Dabiri S , Kharazmi A , Shafiee A ,
Bioorganic & medicinal chemistry letters , Vol., No. 0960-894X (Print) , 20050405 ,Page:0
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).