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

…, A Christopoulos, AD Robertson, B Capuano…

文献索引:Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564

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被引用次数: 5

摘要

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.