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

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

  • Bioorg Med Chem Lett. 2012 Apr 1;22(7):2560-4. doi: 10.1016/j.bmcl.2012.01.122.
Richard J Conway 1,  Celine Valant,  Arthur Christopoulos,  Alan D Robertson,  Ben Capuano,  Ian T Crosby
Affiliations

Affiliation

  • 1 Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Science, 381 Royal Parade, Parkville 3052, Australia.
PMID: 22381048 DOI: 10.1016/j.bmcl.2012.01.122
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-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.

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