6-(1-Hydroxyalkyl) penam sulfone derivatives as inhibitors of class A and class C β-lactamases I

P Bitha, Z Li, GD Francisco, BA Rasmussen…

Index: Bitha, Panayota; Li, Zhong; Francisco, Gerardo D.; Rasmussen, Beth A.; Lin, Yang-I Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 7 p. 991 - 996

Full Text: HTML

Citation Number: 36

Abstract

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- ...