Side chain SAR of bicyclic β-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem

被引：26

作者：

Blizzard, Timothy A. ^{[1
]}

Chen, Helen ^{[1
]}

Kim, Seongkon ^{[1
]}

Wu, Jane ^{[1
]}

Young, Katherine ^{[2
]}

Park, Young-Whan ^{[2
]}

Ogawa, Amy ^{[2
]}

Raghoobar, Susan ^{[2
]}

Painter, Ronald E. ^{[2
]}

Hairston, Nichelle ^{[2
]}

Lee, Sang Ho ^{[2
]}

Misura, Andrew ^{[2
]}

Felcetto, Tom ^{[2
]}

Fitzgerald, Paula ^{[1
]}

Sharma, Nandini ^{[1
]}

Lu, Jun ^{[1
]}

Ha, Sookhee ^{[1
]}

Hickey, Emily ^{[2
]}

Hermes, Jeff ^{[2
]}

Hammonda, Milton L. ^{[1
,2
]}

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Infect Dis, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

beta-Lactamase; Inhibitor; Carbapenem; Imipenem; STRUCTURE-BASED DESIGN; IN-VITRO ACTIVITY; CLINICAL-PRACTICE;

D O I：

10.1016/j.bmcl.2009.12.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Bridged monobactam beta-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C beta-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：918 / 921

页数：4

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