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新型脱氧呋喃基吲哚类抗菌剂的鉴定。

Identification of novel deoxyribofuranosyl indole antimicrobial agents.

机构信息

Laboratory of Microbiology, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 2012 Feb;65(2):53-7. doi: 10.1038/ja.2011.110. Epub 2011 Dec 14.

Abstract

Three novel deoxyribofuranosyl indole derivatives, FG050227 (1), FG050223 (2) and FG050204 (3), were identified as antimicrobial agents effective against Gram-positive bacterial strains and some fungi. The MIC values of (1), (2) and (3) against methicillin-resistant Staphylococcus aureus were 3.0, 6.0 and 13 μg ml⁻¹, respectively. Compounds 1 and 3 had bactericidal activity against exponentially growing S. aureus and inhibited biosynthesis of peptidoglycan, protein, RNA and DNA. Compound 2 was bacteriostatic and inhibited the biosynthesis of protein and RNA. The results indicated that deoxyribofuranosyl indole derivatives could be potential lead compounds for the development of antimicrobial agents.

摘要

三种新型脱氧呋喃基吲哚衍生物 FG050227(1)、FG050223(2)和 FG050204(3)被鉴定为对抗革兰氏阳性菌菌株和一些真菌有效的抗菌剂。(1)、(2)和(3)对耐甲氧西林金黄色葡萄球菌的 MIC 值分别为 3.0、6.0 和 13μg/ml。化合物 1 和 3 对指数生长期金黄色葡萄球菌具有杀菌活性,并抑制肽聚糖、蛋白质、RNA 和 DNA 的生物合成。化合物 2 具有抑菌活性,抑制蛋白质和 RNA 的生物合成。结果表明,脱氧呋喃基吲哚衍生物可能是开发抗菌剂的潜在先导化合物。

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