Recent Advances in the Synthesis and Evaluation of Beta-Lactamase Inhibitors
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (10 March 2025) | Viewed by 3492
Special Issue Editor
Interests: HIV; RNA respiratory viruses; molecular epidemiology; evolution; drug resistance mutations; discovery of new antivirals; spiro-beta-lactam compounds
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Recent advances in the synthesis and evaluation of beta-lactamase inhibitors have marked significant strides in the battle against antibiotic resistance, a global health threat. Beta-lactamases are enzymes produced by bacteria that confer resistance to beta-lactam antibiotics, such as penicillins and cephalosporins. Over the years, the emergence of beta-lactamase-producing bacteria has compromised the effectiveness of these antibiotics, necessitating the development of novel inhibitors to restore their potency.
In the realm of synthesis, researchers have explored innovative methodologies to design and produce beta-lactamase inhibitors with enhanced efficacy and reduced toxicity. Rational drug design, combinatorial chemistry and structure-based approaches have been instrumental in creating molecules that exhibit improved binding affinity to beta-lactamases. The incorporation of computational techniques, such as molecular docking and dynamics simulations, has expedited the identification of key interactions between inhibitors and enzymes, facilitating the optimization of inhibitor structures.
The evaluation of beta-lactamase inhibitors involves rigorous testing for their ability to combat resistant bacterial strains effectively. Recent studies have focused on expanding the spectrum of inhibition to encompass a broad range of beta-lactamases, including those with mutations that confer resistance to existing inhibitors. This holistic approach aims to develop inhibitors that can overcome the diversity of beta-lactamase enzymes encountered in clinical settings.
Furthermore, researchers have explored combination therapies, wherein beta-lactamase inhibitors are used in tandem with existing antibiotics to enhance their efficacy. This synergistic approach not only addresses existing resistance, but also minimizes the likelihood of the emergence of new resistance mechanisms.
In conclusion, recent advances in the synthesis and evaluation of beta-lactamase inhibitors showcase a multifaceted strategy to combat antibiotic resistance. Through innovative synthesis methods and comprehensive evaluation techniques, researchers are paving the way for the development of potent inhibitors that can reinvigorate the effectiveness of beta-lactam antibiotics, providing a crucial line of defense against bacterial infections in the modern era.
Dr. Inês Bártolo
Guest Editor
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Keywords
- beta-lactamase inhibitors
- rational drug design
- combinatorial chemistry
- antibiotic resistance
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