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顶孢菌素,由顶孢霉属LL-Cyan 416产生的新型聚酮类抗生素。

Acremonidins, new polyketide-derived antibiotics produced by Acremonium sp., LL-Cyan 416.

作者信息

He Haiyin, Bigelis Ramunas, Solum Eric H, Greenstein Michael, Carter Guy T

机构信息

Natural Products Research, Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA.

出版信息

J Antibiot (Tokyo). 2003 Nov;56(11):923-30. doi: 10.7164/antibiotics.56.923.

Abstract

Acremonidins A to approximately E (1 to approximately 5) were produced by fermentation of Acremonium sp., LL-Cyan 416, in heterogeneous phases. The structures of these compounds, containing a bridging keto group, were determined by spectroscopic analysis. Acremonidins A and B showed moderate activity against Gram-positive bacteria, including the methicillin-resistant staphylococci and vancomycin-resistant enterococci. Selective acylations of acremonidin B afforded ester derivatives 6 to approximately 9 that exhibited improved antibacterial activity.

摘要

顶头孢菌素A至约E(1至约5)是由顶孢霉属LL-Cyan 416在非均相体系中发酵产生的。这些含有桥连酮基的化合物的结构通过光谱分析确定。顶头孢菌素A和B对革兰氏阳性菌表现出中等活性,包括耐甲氧西林葡萄球菌和耐万古霉素肠球菌。对顶头孢菌素B进行选择性酰化得到酯衍生物6至约9,其抗菌活性有所提高。

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