Design at the atomic level: Generation of novel hybrid biaryloxazolidinones as promising new antibiotics

被引：35

作者：

Zhou, Jiacheng ^{[2
]}

Bhattacharjee, Ashoke ^{[2
]}

Chen, Shili ^{[2
]}

Chen, Yi ^{[2
]}

Duffy, Erin ^{[1
]}

Farmer, Jay ^{[2
]}

Goldberg, Joel ^{[2
]}

Hanselmann, Roger ^{[2
]}

Ippolito, Joseph A. ^{[1
]}

Lou, Rongliang ^{[2
]}

Orbin, Alia ^{[2
]}

Oyelere, Ayomi ^{[2
]}

Salvino, Joe ^{[2
]}

Springer, Dane ^{[2
]}

Tran, Jennifer ^{[2
]}

Wang, Deping ^{[1
]}

Wu, Yusheng ^{[2
]}

Johnson, Graham ^{[1
,2
]}

机构：

[1] Rib X Pharmaceut Inc, Dept Struct Based Drug Design, New Haven, CT 06511 USA

[2] Rib X Pharmaceut Inc, Dept Med Chem, New Haven, CT 06511 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

Oxazolidinone; Biaryloxazolidinone; Structure-based drug design; Linezolid; Sparsomycin; Gram-negative bacteria; X-ray crystal structure; Ribosome; Oral antibiotics; Hybrid antibiotics;

D O I：

10.1016/j.bmcl.2008.10.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

From the X-ray crystal structures of linezolid and the non-selective antibiotic sparsomycin, we have derived a new family of hybrid oxazolidinones. From this initial compound set we have developed a new biaryloxazolidinone scaffold that shows both potent antimicrobial activity as well as selective inhibition of ribosomal translation. The synthesis of these compounds is outlined. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6179 / 6183

页数：5

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