A critical review on recent trends on pharmacological applications of pyrazolone endowed derivatives

4-Disubstituted Pyrazolin-3-Ones—Novel Class of Fungicides against Phytopathogenic Fungi

“…The five-membered pyrazolin-3-one (pyrazolone) ring is a privileged structural motif in medicinal chemistry with a wide range of biological activities [22] (Figure 1). The Agrochemicals 2023, 2 practical importance of pyrazolones attracts continuous interest to the development of their synthetic methodology and properties [23,24].…”

“…The history of the medical use of 4-unsubstituted pyrazolinones began as early as 1887 with the discovery of antipyrine (1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one), one of the first nonopioid analgesics and antipyretics. This discovery prompted the study of pyrazolone derivatives, including C4-monosubstituted pyrazolones, pyrazolone-based Schiff bases, and their metal complexes, which possess anti-inflammatory, antipyretic and analgesic [22,[25][26][27], antitumor/cytotoxic [22,25,[28][29][30], antimicrobial [22,25,[31][32][33], antioxidant [22,26], and protein denaturation inhibiting [27] activities. The interest of medicinal chemists to pyrazolones has been maintained and is increasing at the present time [22].…”

“…This discovery prompted the study of pyrazolone derivatives, including C4-monosubstituted pyrazolones, pyrazolone-based Schiff bases, and their metal complexes, which possess anti-inflammatory, antipyretic and analgesic [22,[25][26][27], antitumor/cytotoxic [22,25,[28][29][30], antimicrobial [22,25,[31][32][33], antioxidant [22,26], and protein denaturation inhibiting [27] activities. The interest of medicinal chemists to pyrazolones has been maintained and is increasing at the present time [22]. Recently, C4-disubstituted pyrazolones, primarily spiropyrazolones, have also attracted increasing attention as biologically active compounds [34][35][36].…”

Pyrazolone-type compounds (part II): in vitro and in silico evaluation of antioxidant potential; structure–activity relationship

“…4 Such an outcome was triggered by the diversity of pyrazolone-based compounds and their richness in benecial biological virtues. 2,7 Pyrazolonecored derivatives mostly wield antimicrobial, [8][9][10][11][12][13] anticancer, 7,12,14,15 antiproliferative, 14,16 and antiinammatory potency, [17][18][19][20][21][22] but they were also identied as analgesics, 18,22,23 antivirals, [24][25][26] hypoglycaemics, 27 and antioxidants. 11,28,29 The utilisation of pyrazolone synthon produced numerous hybrid molecules acting as multitarget agents.…”

“…Namely, edaravone acts as a potent free radical scavenger that prevents oxidative damage to the cell membrane, i.e., peroxidation of the cell membrane's fatty acids, and therefore, neuronal death and brain edema. 2 The overproduction of free radicals leading to oxidative stress is designated as one of the leading causes of brain ischemic injury. 41,42 Regarding this, the benecial action of edaravone lies in its ability to quench cOH radicals, as well as other harmful reactive oxygen/nitrogen radical species (ROS and RNS).…”