Bioorganic and Medicinal Chemistry Letters p. 991 - 996 (1999)
Update date:2022-09-26
Topics:
Bitha, Panayota
Li, Zhong
Francisco, Gerardo D.
Rasmussen, Beth A.
Lin, Yang-I
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.
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