期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 5, 页码 1859-1881出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01279
关键词
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资金
- Spanish Ministry of Economy and Competiveness [SAF2016-75638-R]
- Xunta de Galicia [ED431B 2018/04]
- European Regional Development Fund (ERDF)
- Spanish Ministry of Science, Innovation and Universities
- Xunta de Galicia [Centro Singular De Investigacion de Galicia Accreditation 2016-2019] [ED431G/09]
Infections caused by resistant bacteria are nowadays too common, and some pathogens have even become resistant to multiple types of antibiotics, in which case few or even no treatments are available. In recent years, the most successful strategy in anti-infective drug discovery for the treatment of such problematic infections is the combination therapy antibiotic + inhibitor of resistance. These inhibitors allow the repurposing of antibiotics that have already proven to be safe and effective for clinical use. Three main types of compounds have been developed to block the principal bacterial resistance mechanisms: (i) beta-lactamase inhibitors; (ii) outer membrane permeabilizers; (iii) efflux pump inhibitors. This Perspective is focused on beta-lactamase inhibitors that disable the most prevalent cause of antibiotic resistance in Gram-negative bacteria, i.e., the deactivation of the most widely used antibiotics, beta-lactams (penicillins, cephalosporines, carbapenems, and monobactams), by the production of beta-lactamases. An overview of the most recently identified beta-lactamase inhibitors and of combination therapy is provided. The article also covers the mechanism of action of the different types of beta-lactamase enzymes as a basis for inhibitor design and target inactivation.
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