The synthesis and evaluation of 3-substituted-7(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors

Authors
Buynak, JD Doppalapudi, VR Adam, G
Citation
Jd. Buynak et al., The synthesis and evaluation of 3-substituted-7(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors, BIOORG MED, 10(9), 2000, pp. 853-857
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
9
Year of publication
2000
Pages
853 - 857
Database
ISI
SICI code
0960-894X(20000501)10:9<853:TSAEO3>2.0.ZU;2-V
Abstract
A series of 3-substituted-7-(alkylidene)cephaloporin sulfones were prepared and evaluated as inhibitors of representative class A and class C serine b eta-lactamase. Appropriate substituents resulted in a 1000-fold improvement in the inhibition of the class A enzymes and a simultaneous 20-fold improv ement in the inhibition of class C. These new compounds have achieved the g oal of creating broad scale inhibitors in the cephalosporin series. (C) 200 0 Elsevier Science Ltd. All rights reserved.