Structural Modification of Heterocyclic Scaffolds: A Strategy for Antibacterial Drug Discovery

ABSTRACT Multidrug‐resistant (MDR) bacterial infections are on the rise worldwide, and there are fewer clinically available medications to treat them. Methicillin‐resistant Staphylococcus aureus (MRSA) is one of the most compelling and harmful bacteria. MRSA has surfaced, spread widely, and gained recognition as a leading source of bacterial infections in both community and clinical settings. The most dangerous feature of MRSA is its quick evolution of resistance to all known antibiotics, including vancomycin. Finding novel, powerful, and less hazardous antibiotic moieties is essential to combating MRSA isolates. In medicinal chemistry, the electron‐withdrawing groups—primarily the –Cl, NO 2 , F, and Br groups—can play an important role. A curative or diagnostic small molecule aspirant's pharmacokinetic and physicochemical characteristics, such as increased membrane permeability for MRSA and better metabolic stability, can be improved by the selective setup of EWGs. In this study, we reviewed the benefits of using EWGs to boost antibacterial effectiveness against different types of bacterial pathogens and talked about how it might be used in antibacterial drug discovery.