QSAR STUDIES OF PYRROLIDINES DERIVATIVES AS POTENT FUNCTIONAL ANTAGONISTS OF HUMAN MELANOCORTIN-4 RECEPTOR

摘要

Melanocortin-4 receptor (MC4R) plays as vital role in regulating feeding behavior and other biological function. It is a member of G-Protien-Coupled receptor (GPCR). A number of its antagonists are found to reverse mass loss and enhance intake of food in animal model of cachexia which suggests that it can be used for treatment of cancer cachexia.In order to find important essential structural and physicochemical parameters, that effect the inhibitory activity of pyrrolidines derivatives (Fig : 1), antagonists of MC4R, QSAR study was performed using linear free relationship (LFER) approach and is reported in this paper. The QSAR studies have been carried out considering anticancer activity as dependent and different physicochemical parameters like hydrophobic (π), steric (MR) and electronic (f, R, σ) as independent parameters.