Recent highlights in the synthesis and biological significance of pyrazole derivatives

Aza-heterocyclic scaffolds are privileged cores in the composition of their potential therapeutic profiles and versatile synthetic intermediates. Pyrazole is one of the frequently studied compounds of “azole” family and consists of nitrogen in a 1,2 linking sequence. These motifs possess a wide-spectrum of applications in the field of pharmaceuticals, agrochemicals, polymer chemistry, cosmetics, food industries and more. In addition, functionalized pyrazole derivatives are frequently used as ligands in coordination chemistry and metal-catalysed reactions. As exemplified by numerous recent reports, pyrazoles are highly promising pharmacophores with excellent therapeutic applications. Owing to their aromaticity, the ring structures have many reactive positions, where electrophilic, nucleophilic, alkylation and oxidative reactions might occur. The structural adroitness and diversity of pyrazole cores further emanated numerous fused bicyclic skeletons with various biological applications. In this review, we highlight the recent synthetic methods developed for the preparation of functionalized pyrazole derivatives (From 2017 to present). In addition, we have also covered the notable biological activities (anti-cancer, anti-inflammatory, anti-bacterial and anti-viral) of this ubiquitous core. Herein, we emphasised the synthesis of pyrazoles from variety of precursors such as, alkynes, α,β-unsaturated carbonyl compounds, diazo reagents, nitrile imines, diazonium salts, 1,3-dicarbonyl compounds and etc. Moreover, the recent synthetic methodologies focusing on the preparation of pyrazolines and pyrazolones and variously fused-pyrazoles are also included. Authors expect this review could significantly help the researchers in finding elegant novel tools to synthesize pyrazole skeletons and expand their biological evaluation. [Display omitted]