Exploration of in vitro time point quantitative evaluation of newly synthesized benzimidazole and benzothiazole derivatives as potential antibacterial agents

被引：82

作者：

Bandyopadhyay, Prabal ^{[1
]}

Sathe, Manisha ^{[1
]}

Ponmariappan, S. ^{[1
]}

Sharma, Arti ^{[1
]}

Sharma, Pratibha ^{[2
]}

Srivastava, A. K. ^{[1
]}

Kaushik, M. P. ^{[1
]}

机构：

[1] Def Res & Dev Estab, Proc Technol Dev Div, Discovery Ctr, Gwalior 474002, MP, India

[2] Devi Ahilya Univ, Sch Chem Sci, Indore 452001, Madhya Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 24期

关键词：

Antibacterial activity; Quantitative assay; Benzimidazole; Benzothiazole; In vitro; 2-SUBSTITUTED BENZOTHIAZOLES; ANTITUMOR BENZOTHIAZOLES; ANTIMALARIAL EVALUATION; 2-ARYLBENZOTHIAZOLES; 2-ARYLBENZIMIDAZOLES; EFFICIENT;

D O I：

10.1016/j.bmcl.2011.10.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Present communication deals with the in vitro time point quantitative antibacterial evaluation of newly synthesized 1,2-disubstituted benzimidazoles (3a-p) and 2-substituted benzothiazoles (5a-h) against Gram-positive bacteria Staphylococcus aureus, Bacillus cereus, and Gram-negative bacteria Vibrio cholerae, Shigella dysenteriae and Escherichia coli. These compounds were synthesized under mild reaction conditions using Al(2)O(3)-Fe(2)O(3) nanocrystals as heterogeneous catalyst. Bio-evaluation studies revealed that, compounds 3a, 5a and 5d exhibited moderate to good antibacterial activity against all the tested bacterial stains. The compounds 3a, 3f and 5a have shown enhanced inhibitory activity compared with standard antibacterial drug ciprofloxacin against V. cholerae, B. cereus, and S. dysenteriae, respectively. Additionally, the compounds 3a, 3e, 3f, 3h and 5b displayed complete bactericidal activity within 24 h, whereas ciprofloxacin took 48 h to kill those bacteria completely. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7306 / 7309

页数：4

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