| Title : C(8)-substituted 1-azabicyclo[3.3.1]non-3-enes: a novel scaffold for muscarinic receptor ligands - Kim_2004_Bioorg.Med.Chem_12_2357 |
| Author(s) : Kim MG , Bodor ET , Harden TK , Kohn H |
| Ref : Bioorganic & Medicinal Chemistry , 12 :2357 , 2004 |
|
Abstract :
The [3.3.1]-bicyclic amine, exo-8-benzyloxymethyl-3-ethoxycarbonyl-4-hydroxy-1-azabicyclo[3.3.1]non-3-ene (1), has been shown to be a potent competitive antagonist against the hM(1)-hM(5) muscarinic receptors. This heterocyclic system has not been extensively evaluated despite the notable activities reported for other bicyclic amines. Synthetic strategies permitted the selective alteration of five structural sites in 1. Pharmacological evaluation demonstrated that modification of either the C(3) alkoxycarbonyl or the C(4) enol units in 1 gave compounds with high affinity for the hM(1)-hM(5) muscarinic receptors with selectivity for the hM(2) receptor. |
| PubMedSearch : Kim_2004_Bioorg.Med.Chem_12_2357 |
| PubMedID: 15080933 |
Kim MG, Bodor ET, Harden TK, Kohn H (2004)
C(8)-substituted 1-azabicyclo[3.3.1]non-3-enes: a novel scaffold for muscarinic receptor ligands
Bioorganic & Medicinal Chemistry
12 :2357
Kim MG, Bodor ET, Harden TK, Kohn H (2004)
Bioorganic & Medicinal Chemistry
12 :2357