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Azabicyclic indole esters as potent 5-HT4 receptor antagonists
P A Wyman1, L M Gaster, F D King
1SmithKline Beecham Pharmaceuticals, Harlow, Essex, U.K.
Bioorganic & Medicinal Chemistry
|February 1, 1996
Abstract:
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.