Synthesis and structure–Activity relationships of M 2-Selective muscarinic receptor ligands in the 1-[4-(4-Arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family

SW McCombie, SI Lin, JR Tagat, D Nazareno…

Index: McCombie, Stuart W.; Lin, Sue-Ing; Tagat, Jayaram R.; Nazareno, Dennis; Vice, Susan; Ford, Jennifer; Asberom, Theodros; Leone, Daria; Kozlowski, Joseph A.; Zhou, Guowei; Ruperto, Vilma B.; Duffy, Ruth A.; Lachowicz, Jean E. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 5 p. 795 - 798

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Citation Number: 15

Abstract

The synthesis and muscarinic binding properties of compounds based on the 1-[4-(4- arylsulfonyl) phenylmethyl]-4-(1-aroyl-4-piperidinyl)-piperazine skeleton are described. For compounds, substituted with appropriately configured methyl groups at the benzylic center and at the piperazine 2-position, high levels of selective, M2 subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.