Abstract

DESIGN AND SYNTHESES OF SOME NEW PYRAZOLO[3,4-d]-4- (PHENYL)-1,2,4-(8H)-TRIAZOLO-[2,3-a]-PYRIMIDIN-4(1H)-ONE DERIVATIVES AS POTENT ANTI-INFLAMMATORY AGENT

D. P. Kawade*, P. B. Khedekar2

ABSTRACT

Nitrogen containing heterocyclic ring such as pyrimidine is a promising structural moiety for drug designing. The titled compounds(19-38) were synthesized from the compound N-(4- carboethoxypyrazol-3-yl)N’-arylthioureas which was obtained by reacting ethyl 5-amino-1H-pyrazole-4-carboxylate and appropriate phenylisothiocyanate in the presence of toluene. The intermediate compound was obtained by cyclization reaction with hydrazine hydrate in absolute ethanol. Finally, A mixture of 2-phenylamino-3- aminopyrazolo [3,4-d] pyrimidin-4(1H)-one, p-toluenesulphonic acid and triethylorthoformate was heated under reflux to formed titled compounds (19-38). The synthesized compounds were characterized by FT-IR, 1HNMR, mass spectral data, elemental analysis and evaluated for anti-inflammatory activity. The most active compounds (27) and (32) was evaluated for its ulcerogenicity. The results of antiinflammatory activity (in vivo) indicated that the compounds (27) and (32) possessed significant anti-inflammatory activity as compared to standard drug, Indomethacin.

Keywords: Pyrimidin-4(1H)-one, triethylorthoformate, p-toluenesulphonic acid, carageenaninduced rat paw oedema model, anti-inflammatory activity.