Synthesis and potent antibacterial activity against MRSA of some novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidines

被引：152

作者：

Göker, H

Özden, S

Yildiz, S

Boykin, DW

机构：

[1] Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey

[2] Ankara Univ, Fac Pharm, Dept Microbiol, TR-06100 Ankara, Turkey

[3] Georgia State Univ, Dept Chem, Atlanta, GA 30303 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 40卷 / 10期

关键词：

1H-benzimidazole-carboxamidines; methicilline resistant S. aureus; antibacterial activity;

D O I：

10.1016/j.ejmech.2005.05.002

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A series of 28 novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidine derivatives were synthesized and evaluated for in vitro antibacterial activities against Staphylococcus aureus and methicillin resistant S. aureus (MRSA) by the tube dilution method. The results showed that compounds 45-46 and 55-57, having 3,4-dichloro substituted phenyl at the position C-2, of N-bulky alkyl substituted benzimidazolecarboxamidines exhibited the greatest activity with MIC values of 1.56-0.39 mu g/ml. (c) 2005 Elsevier SAS. All rights reserved.

引用

页码：1062 / 1069

页数：8

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