Thiazole Scaffold-based Anti-Tubercular Agents: A Review on Synthesis and Structural Modifications

Tuberculosis (TB), caused by Mycobacterium tuberculosis, remains a major global health challenge due to the rise of multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains. The urgent need for novel anti-tubercular agents has driven extensive research into heterocyclic scaffolds, with thiazole-based compounds emerging as promising candidates. Thiazole-based compounds exhibit potent anti-tubercular activity by targeting key bacterial enzymes, disrupting cell wall synthesis, and interfering with essential metabolic pathways. Thiazole ring shows significant biological activity due to their versatile chemical nucleophilic and electrophilic reactivity. This review provides a comprehensive analysis of the conventional and modern synthetic approaches for thiazole scaffold-based anti-tubercular agents. Additionally, it explores structural and functional groups modifications on thiazole core with their impact on anti-tubercular activity. Recent advancements in molecular modeling, hybrid molecule design, and medicinal chemistry strategies for optimizing thiazole derivatives are also discussed. The insights presented in this review highlight the potential of thiazole scaffolds in TB drug discovery and underscore the need for further medicinal chemistry, preclinical and clinical investigations to develop effective and safer TB therapeutics.

Publication History

Received: 09 April 2025

Accepted after revision: 16 June 2025

Accepted Manuscript online:
17 June 2025