Bioorganic and Medicinal Chemistry p. 255 - 261 (1996)
Update date:2022-08-03
Topics:
Wyman, Paul A.
Gaster, Laramie M.
King, Frank D.
Sutton, Jonathon M.
Ellis, Elizabeth S.
Wardle, Kay A.
Young, Timothy J.
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.
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