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<p>Indole–thiazole hybrids have attracted increasing interest in medicinal chemistry in recent years, combining the privileged indole nucleus with the thiazole ring within a single framework. The indole unit offers opportunities for π–π interactions and hydrogen bonding, while the thiazole ring enables tuning of lipophilicity and electronic properties and can support additional heteroatom-mediated interactions. This review summarizes synthetic approaches, structure–activity relationships (SAR), computational studies, and reported biological activities of indole–thiazole hybrids. The discussed applications include anticancer and antimicrobial studies, antidiabetic activity, and selected enzyme inhibition. Emerging directions such as greener multicomponent routes, structure-based design and docking, and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) evaluation are highlighted. Finally, key challenges and perspectives for optimizing indole–thiazole hybrids as therapeutic leads are outlined.</p>

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Recent advances in indole–thiazole hybrid scaffolds: synthesis, molecular hybridization, and pharmacological potential

  • 期刊论文

  • 发表日期：

    2026年5月8日

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  • Doaa A. Abdelrheem,
  • Sally Mostafa Khadrawy,
  • Mohamed A. M. Ali,
  • Saleh Alkhedhairi,
  • Faris F. Aba Alkhayl,
  • Al Mokhtar Lamsabhi,
  • Emadeldin M. Kamel

摘要

Indole–thiazole hybrids have attracted increasing interest in medicinal chemistry in recent years, combining the privileged indole nucleus with the thiazole ring within a single framework. The indole unit offers opportunities for π–π interactions and hydrogen bonding, while the thiazole ring enables tuning of lipophilicity and electronic properties and can support additional heteroatom-mediated interactions. This review summarizes synthetic approaches, structure–activity relationships (SAR), computational studies, and reported biological activities of indole–thiazole hybrids. The discussed applications include anticancer and antimicrobial studies, antidiabetic activity, and selected enzyme inhibition. Emerging directions such as greener multicomponent routes, structure-based design and docking, and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) evaluation are highlighted. Finally, key challenges and perspectives for optimizing indole–thiazole hybrids as therapeutic leads are outlined.