6-(substituted methylene) penems, potent broad spectrum inhibitors of bacterial β-lactamase: V. chiral 1,2,3-triazolyl derivatives

Abstract

Structure-activity relationships in a series of (5R)-6-triazolylmethylene penems with potent β-lactamase inhibitory activity are described. In most cases, their in vitro synergistic activity with amoxycillin is superior to that of clavulanic acid, sulbactam and tazobactam (YTR 830). Against an Escherichia coli TEM-1 infection in mice, the compounds showed a broad range of potencies; an optimum polarity was found, however, which gave maximum potency. © 1991, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.