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.

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis of heterocycles from alkyl 3-(dimethylamino)propenoates and related enaminones.

The present invention provides a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.

Compositions useful as inhibitors of protein kinases

Triazole derivatives and their anti-tubercular activity

Recent progress in synthesis and bioactivity studies of indolizines.

A simple synthesis of aplysinopsin analogues by dimethylamine substitution in N,N-(dimethylamino)methylidene derivatives of five-membered heterocycles

Regioselective synthesis of ethyl pyrazolecarboxylates from ethyl 3-[(dimethylamino)methylidene]pyruvate and diethyl 3-[(dimethylamino)methylidene]-2-oxosuccinate. Isolation of ethyl 4,5-dihydro-1-heteroaryl-5-hydroxy-1H-pyrazole-5-carboxylates as stable intermediates in the pyrazole ring formation

Synthesis and antimycobacterial activity of alkyl 1‐heteroaryl‐1H‐1,2,3‐triazole‐4‐carboxylates

Cyclocondensations of (+)-camphor derived enaminones with hydrazine derivatives

(1R,3R,4R)-3-(1,2,4-Triazolo[4,3-x]azin-3-yl)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-ones were prepared in 68–94% d.e. in three steps from (1R)-(+)-camphor via coupling of (1R,4R)-3-[(E)-(dimethylamino)methylidene]-1,7,7-trimethylbicyclo[2.2.1]heptan-2-one with hydrazinoazines followed by oxidative cyclisation of the intermediate hydrazones with methanolic bromine. The structures were determined by 2D NMR techniques and NOESY spectroscopy as well as by X-ray diffraction.

Simon Recnik

Papers

A simple synthesis of aplysinopsin analogues by dimethylamine substitution in N,N-(dimethylamino)methylidene derivatives of five-membered heterocycles

Regioselective synthesis of ethyl pyrazolecarboxylates from ethyl 3-[(dimethylamino)methylidene]pyruvate and diethyl 3-[(dimethylamino)methylidene]-2-oxosuccinate. Isolation of ethyl 4,5-dihydro-1-heteroaryl-5-hydroxy-1H-pyrazole-5-carboxylates as stable intermediates in the pyrazole ring formation

Synthesis and antimycobacterial activity of alkyl 1‐heteroaryl‐1H‐1,2,3‐triazole‐4‐carboxylates

Cyclocondensations of (+)-camphor derived enaminones with hydrazine derivatives

Stereoselective synthesis of (1R,3R,4R)-3-(1,2,4-triazolo[4,3-x]azin-3-yl)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-ones