Penicillin-derived inhibitors that simultaneously target both metallo- and serine-β-lactamases

被引：65

作者：

Buynak, JD ^{[1
]}

Chen, HS

Vogeti, L

Gadhachanda, VR

Buchanan, CA

Palzkill, T

Shaw, RW

Spencer, J

Walsh, TR

机构：

[1] So Methodist Univ, Dept Chem, Dallas, TX 75275 USA

[2] So Methodist Univ, Dept Biol Sci, Dallas, TX 75275 USA

[3] Baylor Coll Med, Verna & Marrs Mclean Dept Biochem & Mol Biol, Houston, TX 77030 USA

[4] Texas Tech Univ, Dept Chem & Biochem, Lubbock, TX 79409 USA

[5] Univ Bristol, Sch Med Sci, Dept Pathol & Microbiol, Bristol BS8 1TD, Avon, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 05期

关键词：

D O I：

10.1016/j.bmcl.2003.12.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and beta-lactamase inhibitory activity of four 6-(mercaptomethyl)penicillinates and the four corresponding 6-(hydroxymethyl)penicillinates are described. These penicillins include both C6 stereoisomers as well as the sulfide and sulfone oxidation states of the penam thiazolidine sulfur. All compounds were evaluated as inhibitors of representative metallo- and serine-beta-lactamases enzymes. Selected (mercaptomethyl)penicillinates are shown to inactivate both metallo- and serine-beta-lactamases and to display synergism with piperacillin against beta-lactamase producing strains. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：1299 / 1304

页数：6

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