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<p>Pyridones and their derivatives are highly valued in drug discovery due to their marked pharmacological relevance in the pharmaceutical industry. Extensive research efforts towards these compounds have showcased their broad therapeutic potential. The pyridone scaffold has demonstrated to serve as key precursor to facilitate the synthesis of many new compounds. In addition, their worth has been further established by their notable bioactivity across their antibacterial, anticancer, anti-inflammatory, antimalarial, antiviral, and antioxidant applications. This review aims to explore the recent synthetic strategies employed in identifying promising bioactive leads, particularly focusing on the efficiency, regioselectivity, and sustainability of the pyridone derivatives. Synthetic methods discussed include hetero-cyclocondensation reactions, mediated cyclization reaction, nucleophillic cleavage of esters, oxidative amination of cyclopentenones, microwave-assisted synthesis, transition-metal catalysis, intramolecular heck coupling, cascade reaction, cycloaddition reaction, one-pot multicomponent reactions, oxidative annulation and green chemistry protocols <i>via</i> an aqueous medium. Overall, this review provides an overview of the recent advances employed for pyridone derivatives, emphasizing the innovative approaches, mechanistic insights, and sustainable methodologies, thereby offering guidance for future research aimed at developing new and potential bioactive pyridone derivatives.</p>

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Charting the synthetic frontier of pyridone based pharmacophoric hybrids

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年7月2日

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  • Oluwatosin Audu,
  • Olusola Ifedolapo Watti,
  • Natasha October

摘要

Pyridones and their derivatives are highly valued in drug discovery due to their marked pharmacological relevance in the pharmaceutical industry. Extensive research efforts towards these compounds have showcased their broad therapeutic potential. The pyridone scaffold has demonstrated to serve as key precursor to facilitate the synthesis of many new compounds. In addition, their worth has been further established by their notable bioactivity across their antibacterial, anticancer, anti-inflammatory, antimalarial, antiviral, and antioxidant applications. This review aims to explore the recent synthetic strategies employed in identifying promising bioactive leads, particularly focusing on the efficiency, regioselectivity, and sustainability of the pyridone derivatives. Synthetic methods discussed include hetero-cyclocondensation reactions, mediated cyclization reaction, nucleophillic cleavage of esters, oxidative amination of cyclopentenones, microwave-assisted synthesis, transition-metal catalysis, intramolecular heck coupling, cascade reaction, cycloaddition reaction, one-pot multicomponent reactions, oxidative annulation and green chemistry protocols via an aqueous medium. Overall, this review provides an overview of the recent advances employed for pyridone derivatives, emphasizing the innovative approaches, mechanistic insights, and sustainable methodologies, thereby offering guidance for future research aimed at developing new and potential bioactive pyridone derivatives.