Novel imidazole substituted 6-methylidene-penems as broad-spectrum β-lactamase inhibitors
作者： Aranapakam M. Venkatesan , Atul Agarwal , Takao Abe , Hideki Ushirogochi , Itsuki Yamamura
DOI: 10.1016/J.BMC.2004.08.039
关键词:
摘要: Abstract β-Lactamases are serine and metallo-dependent enzymes produced by the bacteria in defense against β-lactam antibiotics. Production of class-A, class-B, class-C make use antibiotics ineffective certain cases. To overcome resistance to antibiotics, several β-lactamase inhibitors such as clavulanic acid, sulbactam, tazobactam widely used clinic combination with However, single point mutations within these have allowed inhibitory effect commercially approved inhibitors. Although available inhibitor/β-lactam antibiotic combinations effective class-A producing many extended spectrum (ESBL’s) they less expressing bacteria. circumvent this problem, based on modeling studies novel imidazole substituted 6-methylidene-penem derivatives were synthesized tested various isolates. The present paper deals synthesis structure–activity relationships (SAR) compounds.
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