Semisynthetic Approaches to Laspartomycin Analogues

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• 作者：William V. Curran ; Richard A. Leese ; Howard Jarolmen ; Donald B. Borders ; Dominique Dugourd ; Yuchen Chen ; Dale R. Cameron
• 刊名：Journal of Natural Products
• 出版年：2007
• 出版时间：March 2007
• 年：2007
• 卷：70
• 期：3
• 页码：447 - 450
• 全文大小：83K
• 年卷期：v.70,no.3(March 2007)
• ISSN：1520-6025

文摘

Laspartomycin C (1), a lipopeptide antibiotic related to amphomycin, consists of a cyclic peptide core and an asparticacid unit external to the core and linking this to a C₁₅-2,3-unsaturated fatty acid. This was reported initially to be activeagainst Staphylococcus aureus, and more recent studies have shown that it is active against VRE, VISA, and MRSAisolates. The enzymatic cleavage of the fatty acid tail was accomplished with a deacylase produced by Actinoplanesutahensis and resulted in two peptides, designated Peptide 1 and Peptide 2. Semisynthetic derivatives of both peptideshave been made, and the principal requirement for biological activity appears to be the presence of an acylaspartic acid.