Abstract

SYNTHESIS AND CHARACTERIZATION ANTI INFLAMMATORY ACTIVITY OF NOVEL PYRAZOLE DERIVATIVES

Shivam Jaiswal*, Rudra Pratap Singh, Shobhit Srivastava, Bhumika Yogi and Sujeet Kumar Gupta

ABSTRACT

In this research we have studied and attempt to synthesize a series of novel pyrazole derivatives (6a-e) and evaluate for anti-inflammatory activity using carragennan-induced rat paw edema method. Firstly, we synthesized an intermediate compound 3-methyl-1-(2,4-dinitrophenyl-1H-pyrazole-5-(4H)-one (3) by the reaction of 2,4-dinitrophenyl hydrazine and ethyl acetoacetate in the presence of ethanol. After that the compound (3) further undergoes Vilsmeier hack reaction (DMF & POCl3) at 0-50C formed compound 5-chloro-3-methyl-1-(2,4-dinitrophenyl)-H-pyrazole-4-carbaldehyde (4) The compound (4) allowed to react with different substituted amines and produces final a series of novel pyrazole derivatives (6a-e) The structures of final compounds are characterized by FTIR, 1H-NMR and Mass spectrometry. The therapeutic response of final drug screening by carragennan induces rat paw edema method for anti inflammatory activity. The compounds 6a and 6c were found to be most potent among all the synthesized derivatives, where Diclofenac sodium was used as standard drug.

Keywords: Vilsmeier Hack reagent (DMF & POCl3), Pyrazole anti-inflammatory activity, carragennan induces rat paw edema method.