Title : Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family - McCombie_2002_Bioorg.Med.Chem.Lett_12_795 |
Author(s) : 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 |
Ref : Bioorganic & Medicinal Chemistry Lett , 12 :795 , 2002 |
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. |
PubMedSearch : McCombie_2002_Bioorg.Med.Chem.Lett_12_795 |
PubMedID: 11859005 |
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 Lett
12 :795
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)
Bioorganic & Medicinal Chemistry Lett
12 :795