4.5 Article

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

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 8, 页码 1983-1985

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.02.073

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1,3,4-thiadiazole; nitrofuran; nitrothiophene; leishmanicidal activity

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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 H-3-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 mu M). (c) 2005 Elsevier Ltd. All rights reserved.

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