Pulvinones as bacterial cell wall biosynthesis inhibitors

被引：56

作者：

Antane, S ^{[1
]}

Caufield, CE

Hu, W

Keeney, D

Labthavikul, P

Morris, K

Naughton, SM

Petersen, PJ

Rasmussen, BA

Singh, G

Yang, YJ

机构：

[1] Wyeth Res, Med Chem Chem & Screening Sci, Princeton, NJ 08543 USA

[2] Wyeth Res, Infect Dis, Pearl River, NY 10965 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 01期

关键词：

pulvinones; murein enzyme inhibitors; antibacterial; microwave demethylation;

D O I：

10.1016/j.bmcl.2005.09.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pulvin ones were synthesized (> 180) in arrays and evaluated as inhibitors of early stage cell wall biosynthesis enzymes MurA-MurD. Several pulvinones inhibited Mur enzymes with IC50's in the 1-10 mu g/mL range and demonstrated antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphyloccus aureus, vancomycin-resistant Enterococcus faecalis, and penicillin-resistant Streptococcus pneumoniae. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：176 / 180

页数：5

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