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

被引:60
作者
Foroumadi, A
Pournourmohammadi, S
Soltani, F
Asgharian-Rezaee, M
Dabiri, S
Kharazmi, A
Shafiee, A [1 ]
机构
[1] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran
[2] LICA Pharmaceut, DK-2100 Copenhagen, Denmark
[3] Kerman Univ Med Sci, Fac Pharm, Kerman 76351, Iran
关键词
1,3,4-thiadiazole; nitrofuran; nitrothiophene; leishmanicidal activity;
D O I
10.1016/j.bmcl.2005.02.073
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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 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.
引用
收藏
页码:1983 / 1985
页数:3
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