CP0569, a new broad-spectrum injectable carbapenem. Part 1: Synthesis and structure-activity relationships

被引：7

作者：

Aihara, K ^{[1
]}

Kano, Y ^{[1
]}

Shiokawa, S ^{[1
]}

Sasaki, T ^{[1
]}

Setsu, F ^{[1
]}

Sambongi, Y ^{[1
]}

Ishii, M ^{[1
]}

Tohyama, K ^{[1
]}

Ida, T ^{[1
]}

Tamura, A ^{[1
]}

Atsumi, K ^{[1
]}

Iwamatsu, K ^{[1
]}

机构：

[1] Meiji Seika Kaisha Ltd, Pharmaceut Res Ctr, Kohoku Ku, Yokohama, Kanagawa 2228567, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0968-0896(03)00304-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 10-methylcarbapenems bearing an (imidazo[5,1-b]thiazolium-6-yl)methyl moiety, a 5,5-fused heterobicycle, at the C-2 position was synthesized and evaluated for in vitro antibacterial activities. CP0569 (1r) and its analogues showed potent antibacterial activities against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative bacteria, including Pseudomonas aeruginosa. Moreover, CP0569 (1r) exhibited stronger antibacterial activity against MRSA and higher resistance to renal dehydropeptidase-1 (DHP-1) than any currently marketed carbapenems, that is, imipenem (IPM), panipenem (PAPM), and meropenem (MEPM). (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3475 / 3485

页数：11

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