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

Bioorganic & Medicinal Chemistry Letters
2000.0

Abstract

A new series of 1beta-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.

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