Design, Synthesis and Pharmacological Evaluation of Isoxazole Analogues Derived from Natural Piperine

Asian Journal of Pharmaceutical and Health Sciences,2012,2,1,256-260.
Published:February 2012
Type:Research Article
Author(s) affiliations:

Mary Sheeja TL*, Anny Mathew, Joyamma Varkey

Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Medicalcollege, Thiruvananthapuram, Kerala, India.


Piperine has attracted considerable attention Worldwide owing to its outstanding biological properties. Synthesis of some Isoxazole analogs of piperine under conventional and microwave conditions in moderate to excellent yields is reported here. Conversion of piperine to piperonal by hydrolysis and oxidation. Condensation of piperonal with substituted Acetophenone gave chalcone derivatives. Finally cyclized with hydroxylamine hydrochloride to form isoxazole analogues of piperine. Anxiolytic activity of the synthesized compounds were studied in Elevated plus Maze and Mirrored chamber using Albino Mice.

Compounds 7B and 7D in 3P07 showing stronger binding with the receptors