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

Autor: Conway RJ; Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Science, 381 Royal Parade, Parkville 3052, Australia., Valant C, Christopoulos A, Robertson AD, Capuano B, Crosby IT
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Apr 01; Vol. 22 (7), pp. 2560-4. Date of Electronic Publication: 2012 Feb 09.
DOI: 10.1016/j.bmcl.2012.01.122
Abstrakt: 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.)
Databáze: MEDLINE