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具有嘌呤环的截短侧耳素衍生物。第2部分：中心间隔基对革兰氏阳性病原体抗菌活性的影响。

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

作者信息

Hirokawa Yoshimi, Kinoshita Hironori, Tanaka Tomoyuki, Nakamura Takanori, Fujimoto Koichi, Kashimoto Shigeki, Kojima Tsuyoshi, Kato Shiro

机构信息

Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co, Ltd, Enoki, Suita, Japan.

出版信息

Bioorg Med Chem Lett. 2009 Jan 1;19(1):170-4. doi: 10.1016/j.bmcl.2008.10.123. Epub 2008 Nov 5.

DOI:10.1016/j.bmcl.2008.10.123
PMID:19028096
Abstract

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.

摘要

作为具有嘌呤环的首个截短侧耳素类似物2A和2B的间隔基团，对4-哌啶硫基部分进行结构修饰，从而发现了新型截短侧耳素衍生物14B和17B。这些化合物在水中具有良好的溶解性，对包括耐甲氧西林金黄色葡萄球菌（MRSA）、耐青霉素肺炎链球菌（PRSP）和耐万古霉素肠球菌（VRE）在内的多种革兰氏阳性菌显示出有前景的体外抗菌活性，并且具有强大的体内疗效。

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