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Synthesis and Biological Activity of Novel Acyl Hydrazone Derivatives of 3-(4,5-diphenyl-1,3-oxazol-2-yl) propanoic acid as Anticancer, Analgesic and Anti-inflammatory Agents

Journal: Journal of Pharmacy Research (Vol.9, No. 2)

Publication Date:

Authors : ; ; ; ; ; ;

Page : 157-164

Keywords : Acyl hydrazones; Analgesic activity; Anti-inflammatory activity; Cytotoxicity; Oxaprozin.;

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Abstract

A series of acyl hydrazone derivatives of 3-(4,5-diphenyl-1,3-oxazol-2-yl) propanoic acid have been synthesized and screened for in vivo anti inflammatory, analgesic and in vitro anti cancer activities. The key intermediate N-acylhydrazine is prepared in good yield from NSAID oxaprozin, was coupled with a variety of aromatic aldehydes under conventional as well as microwave irradiation conditions. The microwave approach utilized solvent free condition, required short time and resulted in very good yields. The newly synthesized compounds have been characterized by IR, 1H NMR, 13C NMR and Mass analysis. The results of the biological activities showed that the compounds 5b, 5d and 5e exhibited significant in vivo analgesic and anti inflammatory activities than reference compound oxaprozin. Compounds 5a, 5b, 5e, 5g, 5h, 5i and 5j revealed promising in vitro cytotoxicity than reference compound Cisplatin.

Last modified: 2015-12-11 13:16:34