Carbapenems: past, present, and future.

Link to article at PubMed

Carbapenems: past, present, and future.

Antimicrob Agents Chemother. 2011 Aug 22;

Authors: Papp-Wallace KM, Endimiani A, Taracila MA, Bonomo RA

In this review, we summarize the current "state of the art" of carbapenem antibiotics and their role in our antimicrobial armamentarium. Among the ?-lactams currently available, carbapenems are unique because they are relatively resistant to hydrolysis by most ?-lactamases, in some cases act as "slow substrates" or inhibitors of ?-lactamases, and still target penicillin binding proteins (PBPs). This "value added feature" of inhibiting ?-lactamases serves as a major rationale for expansion of this class of ?-lactams. We describe the initial discovery and development of the carbapenem family of ?-lactams. Of the early carbapenems evaluated, thienamycin demonstrated the greatest antimicrobial activity and became the parent compound for all subsequent carbapenems. To date, greater than 80 compounds with mostly improved antimicrobial properties, as compared to thienamycin, are described in the literature. We also highlight important features of the carbapenems that are presently in clinical use: imipenem-cilastatin, meropenem, ertapenem, doripenem, panipenem-betamipron, and biapenem. In closing, we highlight some major challenges and urge the medicinal chemist to continue development of these versatile and potent compounds, as they have served us well for more than 3 decades.

PMID: 21859938 [PubMed - as supplied by publisher]

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