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<p>Pyrimidinone, quinazolinone, and pyrazolone frameworks represent highly prominent privileged scaffolds in contemporary medicinal chemistry due to their remarkable structural adaptability and intrinsic capacity to mimic endogenous nitrogenous bases. This review provides a comprehensive and critical evaluation of recent advancements in the pharmacological profiling of these three crucial aza-heterocyclic families as essential motifs for the development of potent anticancer, antibacterial, anti-inflammatory, and antidiabetic agents. Moving beyond a descriptive narrative, this work delivers an informative analysis of structure–activity relationship (SAR) trends, detailing how crucial pharmacophoric features such as the flexible lactam system in pyrimidinones, rigid planar frameworks in quinazolinones, and stabilizing intramolecular hydrogen bonding networks in pyrazolones govern receptor interactions. Furthermore, we examine the distinct electronic and steric effects of peripheral substituents, highlighting how the deliberate integration of electron-withdrawing halogens or electron-donating groups modulates binding potency against key biological pathways and molecular targets. By bridging core architectural frameworks with mechanism-based biological profiles, this review offers critical insights for the rational design and optimization of next-generation, high-potency candidates capable of tackling complex global health concerns.</p> Graphical abstract <p></p>

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The pharmacological potency of advanced aza heterocyclic scaffolds

  • 期刊论文

  • 发表日期：

    2026年7月17日

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  • Ahmed A. Noser,
  • Israa Saeed Abbas,
  • Ibtehal Nasser Salman,
  • Thaer Shafi Hussein,
  • Maha M. Salem

摘要

Pyrimidinone, quinazolinone, and pyrazolone frameworks represent highly prominent privileged scaffolds in contemporary medicinal chemistry due to their remarkable structural adaptability and intrinsic capacity to mimic endogenous nitrogenous bases. This review provides a comprehensive and critical evaluation of recent advancements in the pharmacological profiling of these three crucial aza-heterocyclic families as essential motifs for the development of potent anticancer, antibacterial, anti-inflammatory, and antidiabetic agents. Moving beyond a descriptive narrative, this work delivers an informative analysis of structure–activity relationship (SAR) trends, detailing how crucial pharmacophoric features such as the flexible lactam system in pyrimidinones, rigid planar frameworks in quinazolinones, and stabilizing intramolecular hydrogen bonding networks in pyrazolones govern receptor interactions. Furthermore, we examine the distinct electronic and steric effects of peripheral substituents, highlighting how the deliberate integration of electron-withdrawing halogens or electron-donating groups modulates binding potency against key biological pathways and molecular targets. By bridging core architectural frameworks with mechanism-based biological profiles, this review offers critical insights for the rational design and optimization of next-generation, high-potency candidates capable of tackling complex global health concerns.

Graphical abstract