Synthesis, characterization, antiamoebic activity and cytotoxicity of novel 2-(quinolin-8-yloxy) acetohydrazones and their cyclized products (1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives)

被引：47

作者：

Hayat, Faisal ^{[1
]}

Salahuddin, Attar ^{[1
]}

Zargan, Jamil ^{[2
]}

Azam, Amir ^{[1
]}

机构：

[1] Jamia Millia Islamia, Dept Chem, New Delhi 110025, India

[2] Jamia Hamdard, Dept Toxicol, New Delhi 110062, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 12期

关键词：

2-(Quinolin-8-yloxy)acetohydrazones; 1,2,3-Thiadiazoles; 1,2,3-Selenadiazoles; Entamoeba histolytica; MTT assay; ENTAMOEBA-HISTOLYTICA; VITRO; ANTIBACTERIAL;

D O I：

10.1016/j.ejmech.2010.09.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives were synthesized by the cyclization of novel 2-(quinolin-8-yloxy) acetohydrazones. In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica. The results showed that all the 2-(quinolin-8-yloxy) acetohydrazones were more active than their cyclized products (1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives). SAR showed that the compounds having quinoline ring and hydrazone linkage with free N-H group are responsible for higher antiamoebic activity. The cytotoxic studies of these compounds on human breast cancer MCF-7 cell line showed that all the compounds were nontoxic at the concentration range of 1.56-50 mu M. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：6127 / 6134

页数：8

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