Halogenated Antimicrobial Agents to Combat Drug-Resistant Pathogens

Pharmacol Rev. 2023 Oct 16:PHARMREV-AR-2023-000863. doi: 10.1124/pharmrev.123.000863. Online ahead of print.ABSTRACTAntimicrobial resistance presents us with a potential global crisis as it undermines the abilities of conventional antibiotics to combat pathogenic microbes. The history of antimicrobial agents is replete with examples of scaffolds containing halogens. In this review, we discuss the impacts of halogen atoms in various antibiotic types and antimicrobial scaffolds and their modes of action, structure-activity relationships, and the contributions of halogen atoms in antimicrobial activity and drug resistance. Other halogenated molecules, including carbohydrates, peptides, lipids, and polymeric complexes, are also reviewed, and the effects of halogenated scaffolds on pharmacokinetics, pharmacodynamics, and factors affecting antimicrobial and antivirulence activities are presented. Furthermore, the potential of halogenation to circumvent antimicrobial resistance and rejuvenate impotent antibiotics is addressed. This review provides an overview of the significance of halogenation, the abilities of halogens to interact in biomolecular settings and enhance pharmacological properties and their potential therapeutic usages in preventing a post-antibiotic era. Significance Statement Antimicrobial resistance and the increasing impotence of antibiotics are critical threats to global health. The roles and importance of halogens atoms in antimicrobial drug scaffolds have been ...
Source: Pharmacological Reviews - Category: Drugs & Pharmacology Authors: Source Type: research