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新型查尔酮恶唑烷酮杂化物的合成、构效关系及抗菌研究

Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.

作者信息

Selvakumar N, Kumar G Sunil, Azhagan A Malar, Rajulu G Govinda, Sharma Shikha, Kumar M Sitaram, Das Jagattaran, Iqbal Javed, Trehan Sanjay

机构信息

Anti-infectives Discovery Group, Discovery Research, Dr. Reddy's Laboratories Ltd., Miyapur, Hyderabad 500 049, India.

出版信息

Eur J Med Chem. 2007 Apr;42(4):538-43. doi: 10.1016/j.ejmech.2006.10.013. Epub 2006 Dec 5.

DOI:10.1016/j.ejmech.2006.10.013
PMID:17150281
Abstract

With an intention to synergise the antibacterial activity of chalcones and oxazolidinones, several hybrid compounds possessing both chalcone and oxazolidinone moieties were synthesized and tested for antibacterial activity. The hybrid molecules containing heterocycles instead of aromatic ring were found to be active. A SAR study with various heterocycles resulted in a lead molecule 20, which was converted to one of the potent antibacterial compounds 27.

摘要

为了增强查耳酮和恶唑烷酮的抗菌活性,合成了几种同时含有查耳酮和恶唑烷酮部分的杂化化合物,并对其抗菌活性进行了测试。发现含有杂环而非芳环的杂化分子具有活性。对各种杂环进行的构效关系研究产生了先导分子20,其被转化为强效抗菌化合物27之一。

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