Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists.

Richard J Conway, Celine Valant, Arthur Christopoulos, Alan D Robertson, Ben Capuano, Ian T Crosby

Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Science, 381 Royal Parade, Parkville 3052, Australia.

Bioorganic & medicinal chemistry letters 2012 Apr 1

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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-HT(2C) 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. Crown Copyright © 2012. Published by Elsevier Ltd. All rights reserved.

Citation

Richard J Conway, Celine Valant, Arthur Christopoulos, Alan D Robertson, Ben Capuano, Ian T Crosby. Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists. Bioorganic & medicinal chemistry letters. 2012 Apr 1;22(7):2560-4