Azabicyclic indole esters as potent 5-HT4 receptor antagonists

The synthesis of a series of azabicyclic indole esters is described and their potency reported as 5-HT4 receptor antagonists. Optimization of the most potent compound (19) by preparing the corresponding oxazino[3,2-a]indole ester afforded 34, which had a pIC50 of 9.5 in the guinea pig distal colon l...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 1996-02, Vol.4 (2), p.255-261
Hauptverfasser:	Wyman, P A, Gaster, L M, King, F D, Sutton, J M, Ellis, E S, Wardle, K A, Young, T J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Colon - drug effects Colon - metabolism Guinea Pigs In Vitro Techniques Indoles - chemistry Indoles - metabolism Indoles - pharmacology Myenteric Plexus - drug effects Myenteric Plexus - metabolism Receptors, Serotonin - drug effects Receptors, Serotonin, 5-HT4 Serotonin Antagonists - chemical synthesis Serotonin Antagonists - pharmacology Stereoisomerism Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The synthesis of a series of azabicyclic indole esters is described and their potency reported as 5-HT4 receptor antagonists. Optimization of the most potent compound (19) by preparing the corresponding oxazino[3,2-a]indole ester afforded 34, which had a pIC50 of 9.5 in the guinea pig distal colon longitudinal muscle myenteric plexus preparation.
ISSN:	0968-0896
DOI:	10.1016/0968-0896(96)00037-5