Synthesis and in vitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against MRSA

被引：103

作者：

Tuncbilek, Meral ^{[1
]}

Kiper, Tulug ^{[2
]}

Altanlar, Nurten ^{[3
]}

机构：

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

[2] Novagenix Bioanalyt R&D Ctr, TR-06970 Ankara, Turkey

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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 03期

关键词：

Benzimidazole derivatives; Antibacterial; Antifungal; Methicillin-resistant Staphylococcus aureus; ANTIOXIDANT PROPERTIES; BIOLOGICAL-ACTIVITY; AGENTS; INHIBITORS; RESISTANCE; ANALOGS; BINDING; ALKYL;

D O I：

10.1016/j.ejmech.2008.06.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The novel benzimidazole derivatives (3, 5, 8, 9, 12-14, 18-41) were prepared in this paper and the antimicrobial activities of these compounds against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA, standard and clinical isolates), Bacillus subtilis, Escherichia coli and Candida albicans were evaluated. Compounds 24-26 which have no substitution of N-1 position displayed better antibacterial activities than those of standards (ciprofloxacin, ampicillin and sultamicillin) against both the drug-resistant bacteria (MRSA, standard and clinical isolates). These derivatives (24-26), 2,5,6-trihalogenobenzimidazole analogues (8, 12), 5,6-dichloro-2-amino derivative (13), and 5-chloro-2-(4-benzyloxyphenyl)benzimidazole (35) exhibited the most potent antibacterial activity with MIC 3.12 mu g/ml against S. aureus. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：1024 / 1033

页数：10

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