229309-35-7Relevant academic research and scientific papers
6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C β-lactamases I
Bitha, Panayota,Li, Zhong,Francisco, Gerardo D.,Rasmussen, Beth A.,Lin, Yang-I
, p. 991 - 996 (2007/10/03)
Five 6-(1-hydroxyalkyl)penam sulfone derivatives and two 6- (hydroxymethyl)penams were synthesized for β-lactamase inhibitor screens. The substituent effects and stereochemical requirements of 6α-and 6β-(1- hydroxyalkyl) groups for the biological activity of penam sulfone derivatives were investigated. Of these substituents, only the 6β-hydroxymethyl group of 15 improved the activity of sulbactam against both TEM-1 and AmpC β- lactamases. The sulfone moiety is required for the enhancement of the β- lactamase inhibitory activity. 6β-Hydroxymethylsulbactam (15) was able to restore the activity of piperacillin in vitro and in vivo against various β- lactamase producing microorganisms.
