Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect

Abstract

a b s t r a c tThe 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.

Synthetic and computational efforts towards the development of peptidomimetics and small-molecule SARS-CoV 3CLpro inhibitors

“…Similarly, they have used another potent SARS-CoV 3CLpro inhibitor (i.e. Benzotriazole ester derivative) for designing the target molecule, which was developed by the Wong research group in 2006 90 . They synthesized the designed SMIs via Scheme 21 .…”

Synthesis and Evaluation of Anticancer Activity of Pyrazolone Appended Triarylmethanes (TRAMs)

“…The broad-spectrum of pharmacological properties of pyrazolone derivatives have been reported including antimicrobial, antitumor, CNS activity, anti-inflammatory, antioxidant, antitubercular, antiviral, lipid-lowering, antihyperglycemic, and protein inhibitory activities. [34] Furthermore, recently, Tao et al showed EGFR/HER-2 tyrosine kinase inhibitory activity of 1Hpyrazole-1-carboxamide analogs. [35] A series of 1H-pyrazole-1carbothioamide has been also reported for anticancer activity on MCF-7 cell lines.…”

Polyfluoroalkylated antipyrines in Pd-catalyzed transformations

“…[1][2][3][4][5][6][7][8][9][10] In this regard, pyrazolone derivatives are of particular interest because, based on them, an entire class of analgesic-antipyretics has been developed to be successfully applied in clinical practice for a long time. 11,12 The predecessor of this pyrazolone family is phenazone (antipyrine) (1) (Fig. 1) that is still part of some combination drugs, e.g., A/B otic drops (ear drops).…”

“…1) that is still part of some combination drugs, e.g., A/B otic drops (ear drops). 13 Research in recent years has shown that the pyrazolone core is a universal structure 14 to develop substances with various types of biological action including antimicrobial, 11 antitubercular, 15,16 antiviral, 17 anticancer, [18][19][20][21] analgesic, 22 anti-inammatory, 23 antioxidant, 24 and anti-diabetic 25 activities as well as action on CNS, 26,27 etc.…”