Synthesis and in vitro leishmanicidal activity of 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-5-substituted-1,3,4-thiadiazole derivatives

被引：62
|
作者：
Foroumadi, A [1 ]
Emami, S
Pournourmohammadi, S
Kharazmi, A
Shafiee, A
机构：
[1] Univ Tehran Med Sci, Dept Med Chem, Tehran 14174, Iran
[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran 14174, Iran
[3] Kerman Univ Med Sci, Dept Med Chem, Fac Pharm, Kreman 76351, Iran
[4] Mazandaran Univ Med Sci, Fac Pharm, Dept Med Chem, Sari, Iran
[5] LICA Pharmaceut, DK-2100 Copenhagen, Denmark
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 40卷 / 12期
关键词：
5-nitro-1H-imidazole; 1,3,4-thiadiazole; Leishmania major; anti-promastigote activity;
D O I：
10.1016/j.ejmech.2005.07.002
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2-(1-methyl-5-nitroimidazol-2-yl)-5-(1-piperazinyl, 1-piperidinyl and 1-morpholinyl)-1,3,4-thiadiazoles (3a-g) were synthesized and evaluated for in vitro leishmanicidal activity against Leishmania major promastigotes. The leishmanicidal data revealed that compounds 3a-g had strong and much better leishmanicidal activity than the reference drug pentostam. Compound 3c (piperazine analog) was the most active compound (IC(50) = 0. 19 mu M). (c) 2005 Elsevier SAS. All rights reserved.
引用
收藏
页码：1346 / 1350
页数：5
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