Synthesis, absolute configuration, conformational analysis and binding affinity properties of enantiomeric forms of DAU 5750, a novel M1–M3 muscarinic receptor antagonist

Synthesis, absolute configuration, conformational analysis and binding affinity properties of enantiomeric forms of DAU 5750, a novel M1–M3 muscarinic receptor antagonist

Both the enantiomeric forms of DAU 5750, a novel muscarinic receptor antagonist, have been synthesized in order to assess the relevance of configurational/conformational features for high affinity binding to muscarinic receptor subtypes. The attribution of absolute stereochemistry and conformational...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry 1994-12, Vol.2 (12), p.1375-1383
Hauptverfasser: Turconi, Marco, Gozzo, Andrea, Schiavi, Giovanbattista, Fronza, Giovanni, Mele, Andrea, Bravo, Pierfrancesco
Format: Artikel
Sprache:eng
Schlagworte:
Chymotrypsin - metabolism
Magnetic Resonance Spectroscopy
Molecular Conformation
Molecular Structure
Muscarinic Antagonists - chemical synthesis
Muscarinic Antagonists - chemistry
Muscarinic Antagonists - metabolism
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - metabolism
Receptors, Muscarinic - metabolism
Stereoisomerism
Tropanes - chemical synthesis
Tropanes - chemistry
Tropanes - metabolism
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Both the enantiomeric forms of DAU 5750, a novel muscarinic receptor antagonist, have been synthesized in order to assess the relevance of configurational/conformational features for high affinity binding to muscarinic receptor subtypes. The attribution of absolute stereochemistry and conformational analysis by means of molecular modelling and NMR techniques are also reported. Graphic
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(00)82089-1