Synthesis and structure-activity relationships of novel THF 1β- methylcarbapenems

Yang I. Lin, Panayota Bitha, Subas M. Sakya, Timothy W. Strohmeyer, Zhong Li, Ving J. Lee, Stanley A. Lang, Youjun Yang, Niraja Bhachech, William J. Weiss, Peter J. Petersen, Nilda V. Jacobus, Karen Bush, Raymond T. Testa, Francis P. Tally

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

A series of twelve highly active aminomethyl-THF 1β-methylcarbapenems 3a-1 were synthesized. Of these, carbapenems 3a-f demonstrated a spectrum of antimicrobial activity comparable to those of imipenem and meropenem with the exception of only moderate anti-pseudomonal activity. Most importantly, they demonstrated moderate intrinsic oral activity against an E. coli infection in mice.

Original languageEnglish
Pages (from-to)1671-1676
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume7
Issue number13
DOIs
StatePublished - 8 Jul 1997

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