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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McCombie SW, Lin SI, Tagat JR, Nazareno D, Vice S, Ford J, Asberom T, Leone D, Kozlowski JA, Zhou G, Ruperto VB, Duffy RA, Lachowicz JE (2002) Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family Bioorganic & Medicinal Chemistry Lett12: 795-8