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：64

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

页码：1346 / 1350

页数：5

共 25 条

[21]

MODABBER F, 1993, TROPICAL DIS RES PRO, P77

[22] Treatment of visceral leishmaniasis in 2004 [J].