Synthesis and Structure-Activity Relationship Studies of Highly Potent Novel Oxazolidinone Antibacterials

被引：61

作者：

Komine, Takashi ^{[1
]}

Kojima, Akihiko ^{[1
]}

Asahina, Yoshikazu ^{[1
]}

Saito, Tatsuhiro ^{[1
]}

Takano, Hisashi ^{[1
]}

Shibue, Taku ^{[1
]}

Fukuda, Yasumichi ^{[1
]}

机构：

[1] Kyorin Pharmaceut Co Ltd, Discovery Res Labs, Nogi, Tochigi 3290114, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 20期

关键词：

D O I：

10.1021/jm800800c

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel antibacterial biaryl oxazolidinones bearing an aza-, an oxa-, or a thiabicyclo[3.1.0]hex-6-yl ring system were synthesized, and their in vitro antibacterial activity and structure-activity relationships (SAR) were evaluated. Most of the synthesized biaryl bicyclo[3.1.0]hex-6-yl oxazolidinones showed good antibacterial activity against the Gram-positive and -negative bacteria tested. Regarding SAR trends among the C-ring subtypes, the pyridyl ring was preferable to the phenyl ring. The results showed that the structural variety of the C-ring has a greater impact on antibacterial activity than that of the B-ring. A cyano group at the D-ring C-6 position plays an important role in the highly potent antibacterial activity.

引用

页码：6558 / 6562

页数：5

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