Design, synthesis and biological evaluation of some novel isoniazid cyclocondensed azetidinones

Drug Invention Today Pub Date : 2013-06-01 DOI:10.1016/j.dit.2013.05.007

Karthikeyan Elumalai , Mohammed Ashraf Ali , Manogaran Elumalai , Kalpana Eluri , Sivaneswari Srinivasan , Sujit Kumar Mohanti , Anil Thota

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引用次数: 7

Abstract

Background

In the present study, a series of novel azetidinone derivatives synthesized because of its potent antimicrobial and antimycobacterial activity.

Method

Compounds (10a–10j) were synthesized by reacting Schiff's base of isoniazid reacted with, chloro acetyl chloride in presence of triethyl amine and 1, 4-dioxane as an efficient catalyst, analyzed for their structures. in vitro antimicrobial and antimycobacterial activity were carried out.

Results

Among the synthesized compounds, compound 10b and 10i was found to be the most potent against gram-positive bacteria Bacillus subtilis, gram-negative bacteria Escherichia coli, Mycobacterium tuberculosis CIP and M. tuberculosis H37Rv.

Conclusion

A series of novel azetidinone derivatives of biological interest were synthesized and analyzed, suggests that it an interesting compound compared to the current therapeutic agents and are considered to investigate further for the same.

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几种新型异烟肼环缩合氮杂二酮的设计、合成及生物学评价

本研究合成了一系列新的氮杂啶酮衍生物，因为其具有很强的抗菌和抑菌活性。方法以异烟肼希夫碱与氯乙酰氯在三乙胺和1,4 -二恶烷的催化下反应合成化合物(10a-10j)，并对其结构进行分析。体外抗菌和抑菌活性测定。结果化合物10b和10i对革兰氏阳性菌枯草芽孢杆菌、革兰氏阴性菌大肠杆菌、结核分枝杆菌CIP和结核分枝杆菌H37Rv的抑制作用最强。结论合成并分析了一系列具有生物学意义的新型氮杂啶酮衍生物，与现有的治疗药物相比，它是一种令人感兴趣的化合物，值得进一步研究。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Drug Invention Today

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