Beta-Lactamases Inhibitors: A Perspective on the Existing and the Potential Admixtures to Synergize Beta-lactams Versus Resistant Superbugs.

Abdel-Nasser El-Shorbagi ^1,2*, Sachin Chaudhary ¹, Anurag Chaudhary³, Garima Agarwal³, Prabhash Nath Tripathi³, Shweta Dumoga³.

¹Department of Medicinal Chemistry, College of Pharmacy, University of Sharjah, Sharjah, United Arab Emirates.

²Faculty of Pharmacy, University of Assiut, Assiut, Egypt.

³Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, NH-58, Baghpat Road Crossing, Bypass Road, Meerut, Uttar Pradesh, India.

Corresponding Author E-mail: aelshorbagi@sharjah.ac.ae

Abstract: β-lactam antibiotics are considered the safest bactericides, and upon wide clinical use of benzyl penicillin G in 1945, outbreaks of resistance came out. The frequent semi-synthetic strategies revealed β-lactam generations that are of broad-spectrum activity. The new agents as well as their concomitant use with known inhibitors of β-lactamases potentiate their effectiveness versus higher numbers of resistant pathogens. However, the extremely resistant pathogens are still representing a burden. Efforts had been continued to find more inhibitors of β-lactamases to combine with β-lactams to provide good management of infections by extremely resistant microbes. The purpose of this work is to overview the conventional and the recently introduced β-lactamases in clinical applications, as well as some reported effective inhibitors of β-lactamases. The review pinpoints the inhibitors that can be mixed and/or merged with the beta-lactam antibiotics to effectively treat the microbial infections producing resistant-β-lactamases. ClogP for these drugs and candidate inhibitors is introduced as suggestions to open a door for developers to admix derivatives with suitable pharmacokinetics.

Keywords: Antibacterial; β-lactamases inhibitors; Clinical investigations; Multi-resistant strains

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