Hygeia journal for drugs and medicines


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

Hygeia.JD.Med.Vol.3 (2),Oct.2011-March 2012,48-56.

Article title: Design, Synthesis and Biological evaluation ofPyrazole analogues of Natural Piperine

Authors: AnnyMathew1*, Mary Sheeja T.L2, Arun Kumar.T3, K.Radha4

1, 2, 4.College of Pharmaceutical Sciences, Govt. Medical college,Thiruvananthapuram,, Kerala, India ,695011 . 

3. Department of Molecular Biology,Rajiv Gandhi Centre for Biotechnology, Jagathy, Thiruvananthapuram,, Kerala,India

Article history:Received: 2 August, 2011, revised: 25August 2011, accepted: 27August2011, Available online: 1 October 2011



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.

Key words: Piperine, piperonal, pyrazole, anti-inflammatory, anticancer, Cyclooxygenase,farnasyl transferase

Article outline



3.Scheme of synthesis

4.Cytotoxicity study, Anti cancer activity of the compounds against various cancer cell lines

5.Anti inflammatory activity (HRBCMembrane Stabilization Method)

6.Docking studies

7.Results and discussion

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Anny Mathew*, Mary Sheeja TL, Arun Kumar T, K Radha,H.J.D.Med., Vol. 3 (2), October 2011,pp.48-56.

© 2011 Hygeia journal for drugs and medicines, allrights reserved.  22293590, 0975 6221


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