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Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family. 2002
Stuart W McCombie, and
Sue Ing Lin, and
Jayaram R Tagat, and
Dennis Nazareno, and
Susan Vice, and
Jennifer Ford, and
Theodros Asberom, and
Daria Leone, and
Joseph A Kozlowski, and
Guowei Zhou, and
Vilma B Ruperto, and
Ruth A Duffy, and
Jean E Lachowicz
Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. stuart.mccombie@spcorp.com
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, M(2) subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.
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