title: Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists.
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.
authors.affiliation: Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Science, 381 Royal Parade, Parkville 3052, Australia.
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Conway
authors.forename: Celine
authors.initials: C
authors.lastname: Valant
authors.forename: Arthur
authors.initials: A
authors.lastname: Christopoulos
authors.forename: Alan D
authors.initials: AD
authors.lastname: Robertson
authors.forename: Ben
authors.initials: B
authors.lastname: Capuano
authors.forename: Ian T
authors.initials: IT
authors.lastname: Crosby
mesh_terms: D000818:Animals; D001067:Appetite Depressants / Q000138:chemical synthesis* / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism; D004873:Ergolines / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011485:Protein Binding; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D044405:Receptor, Serotonin, 5-HT2C / Q000737:chemistry / Q000378:metabolism*; D058826:Serotonin 5-HT2 Receptor Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D012702:Serotonin Antagonists / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D001067:Appetite Depressants; D004873:Ergolines; D010880:Piperidines; D011725:Pyridines; D044405:Receptor, Serotonin, 5-HT2C; D058826:Serotonin 5-HT2 Receptor Agonists; D012702:Serotonin Antagonists; C031649:mesulergine; D002118:Calcium