Abstract
Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.
Highlights
Pyrazoles are five-membered heterocycles that constitute a class of compounds useful in organic synthesis
A series of novel pyrazole derivatives were synthesized by Desai et al and screened for their in vitro antibacterial activity against S. aureus, S. pyogenes, E. coli, P. aeruginosa
A series of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives has been synthesized by Chimenti et al and tested for their ability to inhibit the activity of the A and B isoforms of human monoamine oxidase
Summary
Pyrazoles are five-membered heterocycles that constitute a class of compounds useful in organic synthesis. Cyclocondensation of Hydrazine and Its Derivatives on 1,3-Difunctional Systems The leading method used for obtaining substituted pyrazoles is a cyclocondensation reaction. Bishop et al were interested in the factors determining the regioselectivity of this type of reaction in the framework of the synthesis of 3,5-diarylpyrazoles They studied the cyclocondensation Moofleacucleesty2l0e1n8,i2c3,k1e3t4ones on methylhydrazine or aryl hydrazines in ethanol, which provides otfw86o difficultly separable regioisomeric pyrazoles and (Scheme 8) [18]. Was dSiemSsccirlhaiberelmydS,.ecahC1mey2mc.eletSohyc1oo2nd.ntShdfyoeenrnstitshshaeetosiiofssny4on-foat4hfl-keatshlykielsy-1loα-,1f,3β,13,-5,,e35-t-,t5htrr-yiitaarlerrisynyulilpcbpysykrtairetzatuooztnleoeedslef4psr1oyfmrrwaozαimto,hβleα-pes,thβhfrey-onelmeytnhlhiaycynlkdeeαnrta,oiβzcn-ieeknstee.hty(o1lne.2nesiec.qk.)et5onine acetiScimaciildarlayn,da imnettheodprfoersetnhceesyonf tihoedsins eof(1.,03,5e-qtr.)isaufbfsotrituedtedthpeycroazrroelseps ofrnodminagnpαy,βra-eztohlyele4n2icinkegtoonde wyiaesldd(e7s0c%rib)e(dS.chCeymcleoc1o3n)d[2e2n]s.ation of the α,β-ethylenic ketone with phenylhydrazine (1.2 eq.) 5 in acetic acid and in the presence of iodine (1.0 eq.) afforted the corresponding pyrazole in good yield (70%) (Scheme 13) [22]. Synthesis of pyrazoles by cyclocondensation reaction of the α,β-ethylenic ketone
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