In vitro activities of aminomethyl-substituted analogs of novel tetrahydrofuranyl carbapenems

William J. Weiss, Peter J. Petersen, Nilda V. Jacobus, Yang I. Lin, Panayota Bitha, Raymond T. Testa

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

CL 188,624, CL 190,294, and CL 191,121 are novel aminomethyl tetrahydrofuranyl (THF)-1β-methylcarbapenems. The in vitro antibacterial activities of these THF Carbapenems were evaluated and compared with those of biapenem, imipenem, and meropenem against 554 recent clinical isolates obtained from geographically distinct medical centers across North America. The antibacterial activities of the THF carbapenems were equivalent to that of biapenem, and the THF carbapenems were slightly more active than imipenem and less active than meropenem against most of the members of the family Enterobacteriaceae but lacked significant activity against Pseudomonas isolates. In general, CL 191,121 was two- to fourfold more active than CL 188,624 and CL 190,294 against the staphylococcal and enterococcal isolates tested. CL 191,121 was twofold less active than imipenem against methicillin- susceptible staphylococci and was as activity as imipenem against Enterococcus faecalis isolates. Biapenem and meropenem were two- and fourfold less active than CL 191,121, respectively, against the methicillin- susceptible staphylococci and E. faecalis. All the carbapenems displayed equivalent good activities against the streptococci. Biapenem was slightly more active than the other carbapenems against Bacteroides fragilis isolates. Time-kill curve studies demonstrated that the THF carbapenems were bactericidal in 6 h against Escherichia coli and Staphylococcus aureus isolates. The postantibiotic effect exerted by CL 191,121 was comparable to or slightly longer than that of imipenem against isolates of S. aureus, E. coli, and Klebsiella pneumoniae.

Original languageEnglish
Pages (from-to)454-459
Number of pages6
JournalAntimicrobial agents and chemotherapy
Volume43
Issue number3
DOIs
StatePublished - Mar 1999

Fingerprint Dive into the research topics of 'In vitro activities of aminomethyl-substituted analogs of novel tetrahydrofuranyl carbapenems'. Together they form a unique fingerprint.

  • Cite this