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Abstract <p>Triazole-thiazole hybrids represent highly privileged scaffolds in medicinal chemistry, characterized by exceptional structural versatility and a broad spectrum of pharmacological profiles, including anticancer, antimicrobial, antidiabetic, and anti-inflammatory activities. This review provides a critical overview of recent advancements in the synthesis, structure–activity relationships (SAR), and therapeutic applications of these dual-heterocyclic frameworks. We highlight strategic methodologies for integrating triazole and thiazole cores with complementary pharmacophores to enhance potency, optimize pharmacokinetic profiles, and circumvent multi-drug resistance. Furthermore, current optimization bottlenecks and emerging computational paradigms are systematically evaluated. Ultimately, this survey delineates key design principles for leveraging the modularity of triazole-thiazole scaffolds in the development of next-generation, multi-target directed ligands (MTDLs) against complex etiologies.</p>

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Beyond Single Targets: A Review of Triazole-Thiazole Hybrids in Modern Drug Design

  • 期刊论文

  • 发表日期：

    2026年8月4日

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  • Prashant J. Burange,
  • Pinkal H. Patel,
  • Tejaswini P. Masne

摘要

Abstract

Triazole-thiazole hybrids represent highly privileged scaffolds in medicinal chemistry, characterized by exceptional structural versatility and a broad spectrum of pharmacological profiles, including anticancer, antimicrobial, antidiabetic, and anti-inflammatory activities. This review provides a critical overview of recent advancements in the synthesis, structure–activity relationships (SAR), and therapeutic applications of these dual-heterocyclic frameworks. We highlight strategic methodologies for integrating triazole and thiazole cores with complementary pharmacophores to enhance potency, optimize pharmacokinetic profiles, and circumvent multi-drug resistance. Furthermore, current optimization bottlenecks and emerging computational paradigms are systematically evaluated. Ultimately, this survey delineates key design principles for leveraging the modularity of triazole-thiazole scaffolds in the development of next-generation, multi-target directed ligands (MTDLs) against complex etiologies.