Azabicyclic indole esters as potent 5-HT4 receptor antagonists.
Bioorg Med Chem
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.
|Title:||Azabicyclic indole esters as potent 5-HT4 receptor antagonists.|
|Keywords:||Animals, Colon, Guinea Pigs, In Vitro Techniques, Indoles, Myenteric Plexus, Receptors, Serotonin, Receptors, Serotonin, 5-HT4, Serotonin Antagonists, Stereoisomerism, Structure-Activity Relationship|
|UCL classification:||UCL > School of BEAMS
UCL > School of BEAMS > Faculty of Maths and Physical Sciences
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