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

…, M Asgharian-Rezaee, S Dabiri, A Kharazmi…

文献索引：Foroumadi, Alireza; Pournourmohammadi, Shirin; Soltani, Fatemeh; Asgharian-Rezaee, Mitra; Dabiri, Shahriar; Kharazmi, Arsalan; Shafiee, Abbas Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 8 p. 1983 - 1985

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被引用次数: 64

摘要

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 3H-thymidine incorporation. Most of the compounds showed activity better than the reference drug sodium stibogluconate (Pentostam). The most active compound was 6c (IC50= 0.1 μM).