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喹唑啉酮-赖氨酸缀合物的尿素/硫脲衍生物:一类新型抗菌剂的合成及构效关系研究。

Urea/thiourea derivatives of quinazolinone-lysine conjugates: synthesis and structure-activity relationships of a new series of antimicrobials.

机构信息

Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore 570 006, Karnataka, India.

出版信息

Eur J Med Chem. 2011 Jun;46(6):2530-40. doi: 10.1016/j.ejmech.2011.03.041. Epub 2011 Apr 8.

Abstract

Synthesis of a series of urea/thiourea/acetamide/sulphonamide derivatives of quinazolinones conjugated lysine has been reported. Structures of the products have been determined by standard spectroscopical studies. All the compounds have been screened for their antibacterial studies and structure-activity relationship has been developed. The activity profile revealed that the compounds containing urea and thiourea functionalities along with fluoro group have exerted a highly potent activity. Thus, the title compounds represent a novel class of potent antimicrobial agents.

摘要

已经报道了一系列将喹唑啉酮与赖氨酸缩合的脲/硫脲/乙酰胺/磺胺衍生物的合成。通过标准光谱研究确定了产物的结构。所有化合物都进行了抗菌研究筛选,并开发了构效关系。活性概况表明,含有脲和硫脲官能团以及氟基团的化合物表现出高度有效的活性。因此,标题化合物代表了一类新型的强效抗菌剂。

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