Papp-Wallace, Krisztina M; Endimiani, Andrea; Taracila, Magdalena A; Bonomo, Robert A (2011). Carbapenems: past, present, and future. Antimicrobial agents and chemotherapy, 55(11), pp. 4943-60. Washington, D.C.: American Society for Microbiology 10.1128/AAC.00296-11
Full text not available from this repository. (Request a copy)In 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.
Item Type: |
Journal Article (Further Contribution) |
|---|---|
Division/Institute: |
04 Faculty of Medicine > Service Sector > Institute for Infectious Diseases |
UniBE Contributor: |
Endimiani, Andrea |
ISSN: |
0066-4804 |
Publisher: |
American Society for Microbiology |
Language: |
English |
Submitter: |
Factscience Import |
Date Deposited: |
04 Oct 2013 14:24 |
Last Modified: |
05 Dec 2022 14:07 |
Publisher DOI: |
10.1128/AAC.00296-11 |
PubMed ID: |
21859938 |
Web of Science ID: |
000296375600001 |
URI: |
https://boris.unibe.ch/id/eprint/8282 (FactScience: 213799) |
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