6-(substituted methylene)penems, potent broad spectrum inhibitors of bacterial beta-lactamase. III. Structure-activity relationships of the 5-membered heterocyclic derivatives |
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| Authors: | I Bennett N J Broom G Bruton S Calvert B P Clarke K Coleman R Edmondson P Edwards D Jones N F Osborne |
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| Affiliation: | Smith Kline Beecham Pharmaceuticals, Chemotherapeutic Research Centre, Surrey, UK. |
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| Abstract: | Sodium (5RS)-Z-6-(heterocyclylmethylene)penem-3-carboxylates (2) are a series of extremely potent inhibitors of bacterial beta-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. |
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