Abstract
The ongoing emergence of bacterial strains resistant to even third- and fourth-generation β-lactam antibiotics is one of the most pressing and challenging issues in clinical therapy. Furthermore, under the pressure of antibiotics used ubiquitously over the last 80 years, functional mutations and new resistances are continuously increasing. Therefore, new drugs and new approaches to the infections produced by multidrug-resistant Gram-negative bacteria are categorically necessary and expected by the scientific community. This review describes the most deleterious known extended-spectrum β- lactamases and the molecules now available for targeting bacterial infections. The active-site chemical and geometric properties that are potentially exploitable for the design of both broad-spectrum and selective compounds are described.
Keywords: β-lactam antibiotics, β-lactamase binding site, β-lactamase inhibitors, carbapenemase, extended spectrum β- lactamases, molecular interaction fields, resistance.
Current Medicinal Chemistry
Title:The Inhibition of Extended Spectrum β-Lactamases: Hits and Leads
Volume: 21 Issue: 12
Author(s): Davide Farina, Francesca Spyrakis, Alberto Venturelli, Simon Cross, Donatella Tondi and Maria Paola Costi
Affiliation:
Keywords: β-lactam antibiotics, β-lactamase binding site, β-lactamase inhibitors, carbapenemase, extended spectrum β- lactamases, molecular interaction fields, resistance.
Abstract: The ongoing emergence of bacterial strains resistant to even third- and fourth-generation β-lactam antibiotics is one of the most pressing and challenging issues in clinical therapy. Furthermore, under the pressure of antibiotics used ubiquitously over the last 80 years, functional mutations and new resistances are continuously increasing. Therefore, new drugs and new approaches to the infections produced by multidrug-resistant Gram-negative bacteria are categorically necessary and expected by the scientific community. This review describes the most deleterious known extended-spectrum β- lactamases and the molecules now available for targeting bacterial infections. The active-site chemical and geometric properties that are potentially exploitable for the design of both broad-spectrum and selective compounds are described.
Export Options
About this article
Cite this article as:
Farina Davide, Spyrakis Francesca, Venturelli Alberto, Cross Simon, Tondi Donatella and Costi Paola Maria, The Inhibition of Extended Spectrum β-Lactamases: Hits and Leads, Current Medicinal Chemistry 2014; 21 (12) . https://dx.doi.org/10.2174/09298673113206660323
DOI https://dx.doi.org/10.2174/09298673113206660323 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Viral Infectivity Inhibition and Viral Biological Elements Destruction using Safe and Low Power Electrons Generated by Life Restoration Device
(LRD): An In Vitro Study
Current Biotechnology Prostate Cancer Molecular Background: The IGF-1Ec Story
Clinical Cancer Drugs Small Molecule 11β- Hydroxysteroid Dehydrogenase Type 1 Inhibitors
Current Topics in Medicinal Chemistry Cell Penetrating Peptide Delivery of Splice Directing Oligonucleotides as a Treatment for Duchenne Muscular Dystrophy
Current Pharmaceutical Design New Non-Nucleocide NS5B Protein Inhibitors for the Treatment of Chronic Hepatitis C Infection
Current Topics in Medicinal Chemistry Protein Homeostasis as a Therapeutic Target for Diseases of Protein Conformation
Current Topics in Medicinal Chemistry Pharmacological Management of PDA: Oral Versus Intravenous Medications
Current Clinical Pharmacology Editorial [Hot Topic:Melanin-Concentrating Hormone (MCH) (Guest Editor: Andrew J. Souers)]
Current Topics in Medicinal Chemistry Preface
Current Pediatric Reviews The Role of Nicotinamide Phosphoribosyltransferase in Cerebral Ischemia
Current Topics in Medicinal Chemistry A Therapeutic Journey of Potential Drugs Against COVID-19
Mini-Reviews in Medicinal Chemistry CDC25 Phosphatase Inhibitors: An Update
Mini-Reviews in Medicinal Chemistry Recent Advances in the Medicinal Chemistry of Polyamine Toxins
Mini-Reviews in Medicinal Chemistry Subject index to volume 3
Current Molecular Medicine Is Combination Therapy of Atosiban and Nifedipine More Effective in Preterm Labor than Each Drug Alone? A Prospective Study
Current Women`s Health Reviews Cytokine Storm and Immunomodulation in COVID-19: A Review
Coronaviruses Novel 1, 2, 3-Triazole-Linked Norcantharidin Analogues: Synthesis and Evaluation of Growth Inhibition in a Panel of Selected Tumor-Cell Lines
Letters in Drug Design & Discovery Cancer Cell Permeability-Glycoprotein as a Target of MDR Reverters: Possible Role of Novel Dihydropyridine Derivatives
Current Drug Targets Gene Therapy in In Vivo Isolated Perfusion Models
Current Gene Therapy Synthesis of Glutamate-Zinc-Aluminium-Layered Double Hydroxide Nanobiocomposites and Cell Viability Study
Current Nanoscience