Structure-activity relationships of biphenyl tetrazoles as metallo-β-lactamase inhibitors

被引:44
|
作者
Toney, JH
Cleary, KA
Hammond, GG
Yuan, XL
May, WJ
Hutchins, SM
Ashton, WT
Vanderwall, DE
机构
[1] Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Infect Dis Res, Rahway, NJ 07065 USA
[3] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
关键词
D O I
10.1016/S0960-894X(99)00458-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Resistance to carbapenem antibiotics in Gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-P-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-P-lactamases as well as renal dehydropeptidase I to a lesser extent. (C) 1999 Elsevier Science Ltd. All rights reserved.
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页码:2741 / 2746
页数:6
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