Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT 3 ligands

…, FJ Villasante, E Gálvez, L Labeaga, A Innerarity…

Index: Iriepa, Isabel; Villasante, Francisco J.; Galvez, Enrique; Labeaga, Luis; Innerarity, Ana; Orjales, Aurelio Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 2 p. 189 - 192

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Citation Number: 20

Abstract

A series of 4-amino-5-chloro-2-methoxybenzoates and benzamides containing the 5-and 6- isoquinuclidinyl system was synthesised and evaluated for binding to 5-HT3, 5-HT4 and D2 receptors. In general, the isoquinuclidine derivatives at the 5-position have shown to be more potent as 5-HT3 ligands but they also possess 5-HT4 and D2 properties. However, the results show that the derivatives at the 6-position afforded the most promising compounds ...