Author/Authors :
Panayota Bitha، نويسنده , , Zhong Li، نويسنده , , Gerardo D. Francisco، نويسنده , , Youjun Yang، نويسنده , , Peter J. Petersen، نويسنده , , Eileen Lenoy، نويسنده , , Yang-I Lin، نويسنده ,
Abstract :
Two stereoselective processes for the synthesis of novel 3,6-disubstituted penam sulfone derivatives were developed. One 6β-(1-hydroxyethyl) and four 6β-hydroxymethyl penam sulfone derivatives were synthesized. All four 6β-(hydroxymethyl)penam sulfone derivatives demonstrated good IC50 against both TEM-1 and AmpC β-lactamases. Of these, 6β-hydroxymethyl penam sulfone derivative 25 was the most active inhibitor which was able to restore the activity of piperacillin in vitro and in vivo against both TEM-1 and AmpC β-lactamases producing organisms.
