The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD SPECTRUM INHIBITORS OF BACTERIAL β-LACTAMASE
III. STRUCTURE-ACTIVITY RELATIONSHIPS OF THE 5-MEMBERED HETEROCYCLIC DERIVATIVES
I. BENNETTN. J. P. BROOMG. BRUTONS. CALVERTB. P. CLARKEK. COLEMANR. EDMONDSONP. EDWARDSD. JONESN. F. OSBORNEG. WALKER
Author information
JOURNAL FREE ACCESS

1991 Volume 44 Issue 3 Pages 331-337

Details
Abstract

Sodium (5RS)-Z-6-(heterocyclylmethylene)penem-3-carboxylates (2) are a series of extremely potent inhibitors of bacterial β-lactamases. A variety of 5-membered heteroaromatic derivatives have been prepared and structure-activity studies reveal a preferred substituent orientation.
One of these derivatives, the 1-methyl-1, 2, 3-triazolyl compound (5m) is a more potent synergist of amoxycillin than clavulanic acid, sulbactam or tazobactam.

Content from these authors
© Japan Antibiotics Research Association
Previous article Next article
feedback
Top