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阿里地菌素,新型糖肽类抗生素。III. 苷元衍生物的制备、表征及生物活性

Aridicins, novel glycopeptide antibiotics. III. Preparation, characterization, and biological activities of aglycone derivatives.

作者信息

Sitrin R D, Chan G W, Chapin F, Giovenella A J, Grappel S F, Jeffs P W, Phillips L, Snader K M, Nisbet L J

出版信息

J Antibiot (Tokyo). 1986 Jan;39(1):68-75. doi: 10.7164/antibiotics.39.68.

Abstract

The aglycone and two pseudoaglycones of aridicin A were prepared by selective hydrolysis and characterized, chemically and biologically. These new analogs demonstrate improved activities in vitro over the parent antibiotics against methicillin sensitive and resistant staphylococci. The major determinant of activity is the mannose substituent, the presence of which results in less potent compounds. The analogs have potent activity against enterococci.

摘要

通过选择性水解制备了阿立地辛A的苷元及两种假苷元,并对其进行了化学和生物学表征。这些新类似物在体外对甲氧西林敏感和耐药葡萄球菌的活性比母体抗生素有所提高。活性的主要决定因素是甘露糖取代基,其存在会导致化合物活性降低。这些类似物对肠球菌具有强效活性。

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