Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1, 2, 3, 6-tetrahydropyridines as 5-HT 2C agonists

…, A Christopoulos, AD Robertson, B Capuano…

Index: Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564

Full Text: HTML

Citation Number: 5

Abstract

A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1, 2, 3, 6- tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure– activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.