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<p>Thiazole-hydrazone compounds serve as an essential bis-heterocyclic scaffold in drug discovery, combining the features of a thiazole ring and a hydrazone linkage. This combination offers enhanced biological activity and versatility due to the distinct characteristics of each component. The thiazole ring provides electron density through its sulfur and nitrogen atoms, contributing to lipophilicity and improved membrane permeability, which enhances the drug’s ability to reach intracellular targets. Thiazoles are recognized for their numerous biological attributes encompassing anticancer, antibacterial, anti-inflammatory, and use for neurological and metabolic disorders in biological activities, including antimicrobial, anticancer, and anti-inflammatory effects. Meanwhile, the hydrazone group introduces a flexible linkage with potential hydrogen-bond donor and acceptor sites. It allows strong interactions with biological targets, making it ideal for targeting enzyme active sites and receptor pockets. The review article explores the recent developments in these versatile heterocyclic combinations and their promising pharmacological activity, particularly in anticancer, anti-inflammatory, antimicrobial, and anti-tubercular treatment. Many compounds featuring this scaffold are under investigation for their efficacy in treating cancer and infectious diseases in numerous clinical phase trials.</p> Graphical abstract <p></p>

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A perspective on the synthetic methodologies and biological attributes of thiazole-hydrazone compounds: a medicinal chemistry-based investigation

  • 期刊论文

  • 发表日期：

    2025年7月28日

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  • Pallishree Bhukta,
  • Akash Verma,
  • Roshan Kumar,
  • Arockia Babu Marianesan,
  • Suhas Ballal,
  • Amrita Pal,
  • Thakur Gurjeet Singh,
  • Ganesh Bushi,
  • Abhay M. Gaidhane,
  • Deepankar Rath,
  • Prateek Pathak,
  • Ashish Ranjan Dwivedi

摘要

Thiazole-hydrazone compounds serve as an essential bis-heterocyclic scaffold in drug discovery, combining the features of a thiazole ring and a hydrazone linkage. This combination offers enhanced biological activity and versatility due to the distinct characteristics of each component. The thiazole ring provides electron density through its sulfur and nitrogen atoms, contributing to lipophilicity and improved membrane permeability, which enhances the drug’s ability to reach intracellular targets. Thiazoles are recognized for their numerous biological attributes encompassing anticancer, antibacterial, anti-inflammatory, and use for neurological and metabolic disorders in biological activities, including antimicrobial, anticancer, and anti-inflammatory effects. Meanwhile, the hydrazone group introduces a flexible linkage with potential hydrogen-bond donor and acceptor sites. It allows strong interactions with biological targets, making it ideal for targeting enzyme active sites and receptor pockets. The review article explores the recent developments in these versatile heterocyclic combinations and their promising pharmacological activity, particularly in anticancer, anti-inflammatory, antimicrobial, and anti-tubercular treatment. Many compounds featuring this scaffold are under investigation for their efficacy in treating cancer and infectious diseases in numerous clinical phase trials.

Graphical abstract