Discovery of RWJ-54428 (MC-02,479), a new cephalosporin active against resistant Gram-positive bacteria

被引：18

作者：

Hecker, SJ ^{[1
]}

Glinka, TW ^{[1
]}

Cho, A ^{[1
]}

Zhang, ZJJ ^{[1
]}

Price, ME ^{[1
]}

Chamberland, S ^{[1
]}

Griffith, D ^{[1
]}

Lee, VJ ^{[1
]}

机构：

[1] Microcide Pharmaceut Inc, Mt View, CA 94043 USA

来源：

JOURNAL OF ANTIBIOTICS | 2000年 / 53卷 / 11期

关键词：

D O I：

10.7164/antibiotics.53.1272

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

The discovery of RWJ-54428 (MC-02,479), a new cephalosporin displaying promising activity against sensitive and resistant Gram-positive bacteria, is described. Progressive structural modification from the previously reported 3-phenylthiocephem MC-02,331 afforded an overall increase in potency against MRSA while retaining other key properties such as acceptable solubility and serum binding. Evaluation of the iii vitro potency and lit vivo efficacy of a series of closely related compounds resulted in selection of RWJ-54428 (MC-02,479) for further studies.

引用

页码：1272 / 1281

页数：10

共 9 条

[1] COMPARATIVE EFFECTS OF AMOXYCILLIN AND AMPICILLIN IN TREATMENT OF EXPERIMENTAL MOUSE INFECTIONS [J].