1.
Bioorg Med Chem Lett
; 12(5): 795-8, 2002 Mar 11.
Article
in English
| MEDLINE
| ID: mdl-11859005
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.
Subject(s)
Piperazines/chemical synthesis , Piperazines/metabolism , Receptors, Muscarinic/metabolism , Binding Sites , Ligands , Molecular Structure , Piperazines/chemistry , Receptor, Muscarinic M1 , Receptor, Muscarinic M2 , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 12(5): 791-4, 2002 Mar 11.
Article
in English
| MEDLINE
| ID: mdl-11859004
ABSTRACT
A novel series of 2-(R)-methyl-substituted piperazines (e.g., 2) is described. They are potent M(2) selective ligands that have >100-fold selectivity versus the M(1) receptor. In the rat microdialysis assay, compound 14 showed significantly enchanced levels of acetylcholine after oral administration.