Pyrazolopyrimidinone and Pyrazolopyrimidine Scaffolds: Emerging Synthetic Strategies and Biological Properties

Introduction: Pyrazolopyrimidine and pyrazolopyrimidinone are leading bioactive molecular scaffolds in medicinal chemistry and drug discovery. Their importance stems from their unique pharmacophore, which combines pyrazole and pyrimidine rings, giving them significant biological activity. A major reason for this activity is the structural analogy of pyrazolopyrimidines with purines (adenine, guanine). Cette ressemblance leur permet d'agir comme des leurres moléculaires, se liant aux enzymes et aux récepteurs à la place des purines naturelles, et modulant ainsi leurs fonctions biologiques. Moreover, the presence of nitrogen atoms in these cycles is fundamental, as they can establish essential hydrogen bonds for anchoring the molecule to its biological target. The great diversity of biological activities of these compounds also stems from the possibility of functionalizing the pyrazole and pyrimidine rings. Cette modularité permet d'optimiser leur affinité et leur sélectivité. Thanks to these characteristics, these molecules are valuable candidates for pharmaceutical development, with a wide range of potential applications, such as anticancer, anti-inflammatory, antimicrobial, and antiviral activities. This review aims to present recent progress regarding the synthesis and biological properties of pyrazolopyrimidine and pyrazolopyrimidinone compounds, focusing on significant advances reported between 2018 and 2025. Methods: This paper brings together the most recent studies and the most widely used synthesis methods, as well as biological studies on pyrazolopyrimidinone and pyrazolopyrimidine scaffolds in the period between 2018 and 2025. Results: Different methods for synthesising pyrazolopyrimidinone and pyrazolopyrimidine derivatives have been cited and studied in order to provide an overview of the majority of synthesis routes for these compounds, as well as their pharmaceutical potential and biological activities. Discussion: The methods for synthesising pyrazolopyrimidinone and pyrazolopyrimidine derivatives described in this review represent the pillars of synthesis for these compounds and an interesting approach that provides a basis for future research into obtaining other products of great biological and pharmaceutical interest. Conclusion: Pyrazolopyrimidinone and pyrazolopyrimidine are heterocyclic compounds that are of great interest in organic chemistry and biological studies due to their biological potential and high reactivity, making them valuable compounds in various fields.