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Novel Piperine Derivatives with Antidiabetic Effect as PPAR‐γ Agonists
Author(s) -
Kharbanda Chetna,
Alam Mohammad Sarwar,
Hamid Hinna,
Javed Kalim,
Bano Sameena,
Ali Yakub,
Dhulap Abhijeet,
Alam Perwez,
Pasha M. A. Qadar
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12760
Subject(s) - piperine , chemistry , benzothiazole , rosiglitazone , pharmacology , alkaloid , piper , stereochemistry , biochemistry , traditional medicine , organic chemistry , receptor , medicine
Piperine is an alkaloid responsible for the pungency of black pepper. In this study, piperine isolated from Piper nigrum L. was hydrolyzed under basic condition to obtain piperic acid and was used as precursor to carry out the synthesis of twenty piperine derivatives containing benzothiazole moiety. All the benzothiazole derivatives were evaluated for their antidiabetic potential by OGT test followed by assessment of active derivatives on STZ‐induced diabetic model. It was observed that nine of twenty novel piperine analogues ( 5b, 6a‐h) , showed significantly higher antidiabetic activity in comparison with rosiglitazone (standard). Furthermore, these active derivatives were evaluated for their action as PPAR‐γ agonists demonstrating their mechanism of action. The effects on body weight, lipid peroxidation, and hepatotoxicity after administration with active derivatives were also studied to further establish these derivatives as lead molecules for treatment of diabetes with lesser side‐effects.