Current Advances in Synthesis and Therapeutic Applications of Thiazole and its Derivatives

Abstract

Thiazole, a five-membered heterocyclic compound with sulfur and nitrogen atoms, serves as a fundamental scaffold in medicinal chemistry. The aromatic nature and diverse substitution patterns of the thiazole ring system enable its extensive applications in drug development. Multiple synthetic routes, from classical Hantzsch synthesis to modern methods, yield varied thiazole derivatives under specific reaction conditions. The biological importance of thiazole-containing compounds extends to anticancer, antimicrobial, and antidepressant activities. Several thiazole-based drugs have demonstrated significant therapeutic effects - dasatinib and dabrafenib as antitumor agents target specific kinases to inhibit cancer cell growth, while ampicillin and myxothiazole exhibit broad-spectrum antimicrobial properties. Structure-activity relationship studies have revealed that substituents at different positions of the thiazole ring significantly influence the biological activity. For instance, attachment of thiourea linker at position 2 enhances anticancer properties, while aryl/alkyl substitutions affect chemical stability and pharmacokinetic properties. The mechanistic understanding of thiazole-based compounds has led to targeted drug development. Recent synthetic methods have produced novel thiazole derivatives with enhanced therapeutic properties, particularly in antimalarial activity where thiazolyl benzenesulfonamide carboxylates show promising results against Plasmodium falciparum