Recent Advances in the Synthesis and Evaluation of Beta-Lactamase Inhibitors

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

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

• beta-lactamase inhibitors
• rational drug design
• combinatorial chemistry
• antibiotic resistance