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Design, Synthesis and Biological evaluation of Pyrazole analogues of Natural Piperine

Author(s): AnnyMathew | Mary Sheeja T.L | Arun Kumar.T | K.Radha

Journal: Hygeia : Journal for Drugs and Medicines
ISSN 0975-6221

Volume: 3;
Issue: 2;
Start page: 48;
Date: 2011;
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Keywords: Piperine | piperonal | pyrazole | anti-inflammatory | anticancer | Cyclooxygenase | farnasyl transferase

A series ofpyrazole analogues of natural piperine were synthesized by removing the basicpiperidine moiety from the piperine nucleus. Piperine upon hydrolysis andoxidation, converted to piperonal and allowed to condense with substitutedacetophenone gave chalcone derivative and cyclized finally withthiosemicarbazide to form pyrazole derivatives of piperine. Docking studies were carried out againstdifferent targets like Cyclooxygenase, farnasyl transferase receptors. Majorityof the synthesized chemical compounds showed good fit with the active site ofall the docked targets.Compound 6a have shown significant anti inflammatory activity and 6d and 6chave shown significant anticancer activity when compared with standard drugs.
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