Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

The pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives. [Display omitted] •The pyrazolone structural motif is a critical element of drugs aimed at different biological end-points.•The pyrazolone analogues have been carried out to drug-like candidates with broad range of medicinal properties.•This review wishes to give an overall retrospect and prospect on the pyrazolone derivatives.