Azabicyclic indole esters as potent 5-HT4 receptor antagonists

Article abstract of DOI:10.1016/0968-0896(96)00037-5

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.