Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogens

被引：29

作者：

Hirokawa, Yoshimi ^{[1
]}

Kinoshita, Hironori ^{[1
]}

Tanaka, Tomoyuki ^{[1
]}

Nakamura, Takanori ^{[1
]}

Fujimoto, Koichi ^{[2
]}

Kashimoto, Shigeki ^{[2
]}

Kojima, Tsuyoshi ^{[2
]}

Kato, Shiro ^{[1
]}

机构：

[1] Dainippon Sumitomo Pharma Co Ltd, Chem Res Labs, Suita, Osaka 5640053, Japan

[2] Dainippon Sumitomo Pharma Co Ltd, Pharmacol Res Labs, Konohana Ku, Osaka 5540022, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 01期

关键词：

Pleuromutilin; Gram-positive bacteria; MRSA; PRSP; VRE; Purine ring; Spacer; MIC; Sulfide; Piperazine ring; ENHANCED ANTIMICROBIAL ACTIVITY;

D O I：

10.1016/j.bmcl.2008.10.123

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structural modification of the 4-piperidinethio moiety, as a spacer of the first pleuromutilin analogues 2A and 2B having a purine ring, led to discovery of the novel pleuromutilin derivatives 14B and 17B. These compounds with good solubility in water showed promising in vitro antibacterial activity against various Gram-positive bacteria including MRSA, PRSP, and VRE and have potent in vivo efficacy. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：170 / 174

页数：5

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (12) :3556-3561

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