Synthesis and biological activity of 1 beta-methyl-2-[5 '-isoxazoloethenylpyrrolidin-3 '-ylthio]carbapenems

Abstract

A new series of 1 beta -methylcarbapenems 1a-i bearing isoxazoloethenyl groups on the pyrrolidine ring has been prepared and evaluated for in vitro antibacterial activity and stability to DHP-I. Most compounds showed excellent antibacterial activity and high stability to DHP-I superior to that of meropenem. Of these new carbapenems, 1a,b,h exhibited the best combination of antibacterial activity and DHP-I stability. (C) 2000 Elsevier Science Ltd. All rights reserved.