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苯乙烯基/吡咯基/吡唑基磺酰甲基-1,3,4-恶二唑基胺与苯乙烯基/吡咯基/吡唑基磺酰甲基-1,3,4-噻二唑基胺的合成及其抗菌活性

Synthesis and antimicrobial activity of styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl amines and styryl/pyrrolyl/pyrazolyl sulfonylmethyl-1,3,4-thiadiazolyl amines.

作者信息

Sravya G, Yamini G, Padmavathi V, Padmaja A

机构信息

Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India.

Department of Chemistry, Sri Venkateswara University, Tirupati 517 502, Andhra Pradesh, India.

出版信息

Eur J Med Chem. 2016 Oct 21;122:647-655. doi: 10.1016/j.ejmech.2016.06.014. Epub 2016 Jul 4.

Abstract

A new class of mono and bis heterocycles - styryl sulfonylmethyl-1,3,4-oxadiazolyl/1,3,4-thiadiazolyl amines, pyrrolyl sulfonylmethyl-1,3,4-oxadiazolyl/1,3,4-thiadiazolyl amines and pyrazolyl sulfonylmethyl-1,3,4-oxadiazolyl/1,3,4-thiadiazolyl amines were prepared from the synthetic intermediate Z-styrylsulfonylacetic acid adopting simple and well versed synthetic methodologies and studied their antimicrobial activity. Amongst all the tested compounds styryl thiadiazole 5c exhibited promising antimicrobial activity against Pseudomonas aeruginosa and Penicillium chrysogenum.

摘要

一类新型的单杂环和双杂环化合物——苯乙烯基磺酰甲基-1,3,4-恶二唑基/1,3,4-噻二唑基胺、吡咯基磺酰甲基-1,3,4-恶二唑基/1,3,4-噻二唑基胺和吡唑基磺酰甲基-1,3,4-恶二唑基/1,3,4-噻二唑基胺,采用简单且成熟的合成方法,由合成中间体Z-苯乙烯基磺酰乙酸制备而成,并对其抗菌活性进行了研究。在所有测试化合物中,苯乙烯基噻二唑5c对铜绿假单胞菌和产黄青霉表现出有前景的抗菌活性。

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