Design and synthesis of bridged γ-lactams as analogues of β-lactam antibiotics

被引：34

作者：

Aszodi, J

Rowlands, DA

Mauvais, P

Collette, P

Bonnefoy, A

Lampilas, M

机构：

[1] Aventis Pharma, Med Chem, F-93235 Romainville, France

[2] Aventis Pharma, Mol Modelisat, F-93235 Romainville, France

[3] Aventis Pharma, Infect Dis Grp, F-93235 Romainville, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 10期

关键词：

bridged gamma-lactam; carbenoid; penicillin binding proteins; antibiotic;

D O I：

10.1016/j.bmcl.2004.03.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Anti-Bredt bridged bicyclo[3.2.1] gamma-lactams were designed as inhibitors of penicillin binding proteins (PBPs). The compounds were prepared by a carbenoid insertion into a lactam N-H bond. Their weak antibacterial activity could either be explained by a poor chemical stability or by unfavorable steric interactions of the methylene bridge of the gamma-lactam with the targeted enzymes. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2489 / 2492

页数：4

共 25 条

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