Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family |
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| Authors: | 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 |
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| Affiliation: | Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. stuart.mccombie@spcorp.com |
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| 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, M(2) subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted. |
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