Heterocyclic compounds as antimicrobial agents

Abstract

Heterocyclic compounds represent the largest and diverse cornucopia of natural or synthetic organic compounds with no distinct demarcations. Apart from being the vast majority of the marketed compounds, heterocycles play a central role in modern drug design and discovery due to the production of wide variety of scaffolds and compounds through robust synthetic research approaches. Current advances in the synthetic methodologies allow instant access to a range of functionalized heterocyclic compounds contributing to expansion of the drug-like chemical compounds in the drug discovery process. Of several advantages, heterocyclic compounds provide with the optimization of lipophilicity, solubility, polarity, H-bonding capacity, etc., which may lead to improved ADMET profile, physicochemical, and pharmacological properties of drug-like candidates. Extensive research works have been conducted over the time in search of effective and safe antimicrobial agents based on heterocyclic scaffolds, particularly to overcome the ever increasing microbial resistance and to reduce the high late-stage attrition rate in the drug development process. This chapter will discuss the progress in important active heterocyclic scaffolds and compounds possessing considerable antimicrobial activities, and will also highlight the potential compounds undergoing clinical development. © 2023 Elsevier Inc. All rights reserved.