Carbapenems: Past, Present, and Future

Antimicrobial Agents and Chemotherapy - Tập 55 Số 11 - Trang 4943-4960 - 2011
Krisztina M. Papp‐Wallace1,2, Andrea Endimiani1,3,2, Magdalena A. Taracila1, Robert A. Bonomo1,4,5,2
1Departments of Medicine, Case Western Reserve University, Cleveland, Ohio 44106
2Research Service, Louis Stokes Cleveland Department of Veterans Affairs Medical Center, Cleveland, Ohio 44106
3Institute for Infectious Diseases, University of Bern, 3010 Bern, Switzerland
4Molecular Biology and Microbiology, Case Western Reserve University, Cleveland, Ohio 44106
5Pharmacology, Case Western Reserve University, Cleveland, Ohio 44106

Tóm tắt

ABSTRACTIn this review, we summarize the current “state of the art” of carbapenem antibiotics and their role in our antimicrobial armamentarium. Among the β-lactams currently available, carbapenems are unique because they are relatively resistant to hydrolysis by most β-lactamases, in some cases act as “slow substrates” or inhibitors of β-lactamases, and still target penicillin binding proteins. This “value-added feature” of inhibiting β-lactamases serves as a major rationale for expansion of this class of β-lactams. We describe the initial discovery and development of the carbapenem family of β-lactams. Of the early carbapenems evaluated, thienamycin demonstrated the greatest antimicrobial activity and became the parent compound for all subsequent carbapenems. To date, more than 80 compounds with mostly improved antimicrobial properties, compared to those of 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 emphasize 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.

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Antimicrobial Agents and Chemotherapy

Tập 55 Số 11

4943-4960

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