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

Richard Conway, Celine Valant, Arthur Christopoulos, Alan D Robertson, Benvenuto Capuano, Ian Travers Crosby

Research output: Contribution to journalArticleResearchpeer-review

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. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)2560 - 2564
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number7
DOIs
Publication statusPublished - 2012

Cite this

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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-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. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.",
author = "Richard Conway and Celine Valant and Arthur Christopoulos and Robertson, {Alan D} and Benvenuto Capuano and Crosby, {Ian Travers}",
year = "2012",
doi = "10.1016/j.bmcl.2012.01.122",
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pages = "2560 -- 2564",
journal = "Bioorganic and Medicinal Chemistry Letters",
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Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists. / Conway, Richard; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D; Capuano, Benvenuto; Crosby, Ian Travers.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 22, No. 7, 2012, p. 2560 - 2564.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

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AU - Conway, Richard

AU - Valant, Celine

AU - Christopoulos, Arthur

AU - Robertson, Alan D

AU - Capuano, Benvenuto

AU - Crosby, Ian Travers

PY - 2012

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AB - 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. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.

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U2 - 10.1016/j.bmcl.2012.01.122

DO - 10.1016/j.bmcl.2012.01.122

M3 - Article

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EP - 2564

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JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

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