6-(Substituted methylene)penems, potent broad spectrum inhibitors of bacterial .BETA.-lactamase. V. Chiral 1,2,3-triazolyl derivatives.
- 1 January 1991
- journal article
- Published by Japan Antibiotics Research Association in The Journal of Antibiotics
- Vol. 44 (9) , 969-978
- https://doi.org/10.7164/antibiotics.44.969
Abstract
Structure-activity relationships in a series of (5R)-6-triazolylmethylene penems with potent beta-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.Keywords
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