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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article

Discovery and Development of Antibacterial Agents: Fortuitous and Designed

Author(s): Ravleen Kaur, Pooja Rani, Atanas G. Atanasov, Qushmua Alzahrani, Reena Gupta, Bhupinder Kapoor*, Monica Gulati* and Pooja Chawla

Volume 22, Issue 7, 2022

Published on: 19 January, 2022

Page: [984 - 1029] Pages: 46

DOI: 10.2174/1570193X19666211221150119

Price: $65


Today, antibacterial drug resistance has turned into a significant public health issue. Repeated intake, suboptimal and/or unnecessary use of antibiotics, and, additionally, the transfer of resistance genes are the critical elements that make microorganisms resistant to conventional antibiotics. A substantial number of antibacterials that were successfully utilized earlier for prophylaxis and therapeutic purposes have been rendered inadequate due to this phenomenon. Therefore, the exploration of new molecules has become a continuous endeavour. Many such molecules are at various stages of the investigation. A surprisingly high number of new molecules are currently in the stage of phase 3 clinical trials. A few new agents have been commercialized in the last decade. These include solithromycin, plazomicin, lefamulin, omadacycline, eravacycline, delafloxacin, zabofloxacin, finafloxacin, nemonoxacin, gepotidacin, zoliflodacin, cefiderocol, BAL30072, avycaz, zerbaxa, vabomere, relebactam, tedizolid, cadazolid, sutezolid, triclosan, and afabiacin. This article aims to review the investigational and recently approved antibacterials with a focus on their structure, mechanisms of action/resistance, and spectrum of activity. Delving deep, their success or otherwise in various phases of clinical trials is also discussed while attributing the same to various causal factors.

Keywords: Antimicrobials, microbial resistance, macrolides, aminoglycosides, pleuromutilins, tetracyclines, fluoroquinolones, oxazolidinones, fatty acid biosynthesis inhibitors, cephalosporins.

Graphical Abstract
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[382] is a database of privately and publicly funded clinical studies conducted around the world. Available from: (Accessed October 16, 2021).

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