Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT_2C agonists

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• 作者：Richard J. Conway^a ; Celine Valant^b ; Arthur Christopoulos^b ; Alan D. Robertson^c ; ^&dagger ; ; Ben Capuano^a ; ^{ben.capuano@monash.edu} ; Ian T. Crosby^a ; ^&Dagger ; ; ^{i.crosby@latrobe.edu.au}
• 关键词：5-HT2C agonists ; Synthesis ; SAR ; Anti-obesity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：1 April, 2012
• 年：2012
• 卷：22
• 期：7
• 页码：2560-2564
• 全文大小：1278 K

文摘

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.