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New substituted benzamides as 5-HT4 receptor antagonists

✍ Scribed by A Orjales; L Alonso-Cires; L Labeaga; A Innerárity; R Corcóstegui


Publisher
Elsevier Science
Year
1995
Tongue
French
Weight
364 KB
Volume
30
Category
Article
ISSN
0223-5234

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Azabicyclic indole esters as potent 5-HT
✍ Paul A. Wyman; Laramie M. Gaster; Frank D. King; Jonathon M. Sutton; Elizabeth S 📂 Article 📅 1996 🏛 Elsevier Science 🌐 English ⚖ 641 KB

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