Synthesis and properties of 2-(naphthosultamyl)methylcarbapenems with potent anti-MRSA activity: Discovery of L-786,392

被引：27

作者：

Ratcliffe, RW

Wilkening, RR

Wildonger, KJ

Waddell, ST

Santorelli, GM

Parker, DL

Morgan, JD

Blizzard, TA

Hammond, ML

Heck, JV

Huber, J

Kohler, J

Dorso, KL

St Rose, E

Sundelof, JG

May, WJ

Hammond, GG

机构：

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

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

[3] Merck & Co Inc, Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(99)00071-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1 beta-methyl-2-(naphthosultamyl)methyl-carbapenems bearing dicationic groups on the naphthosultamyl moiety was prepared and evaluated for activity against resistant gram-positive bacteria. Based on a combination of excellent in vitro antibacterial activity, acceptable mouse acute toxicity, and a desirable fragmentation pattern on beta-lactam ring opening, the analog 2g (L-786,392) was selected for extended evaluation. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：679 / 684

页数：6

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