Bioorganic & Medicinal Chemistry Letters 2004-10-04

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.

Ian Egle, Nancy Barriault, Michel Bordeleau, Jillian Drage, Laurence Dube, Jack Peragine, Lucy Mazzocco, Jalaj Arora, Keith Jarvie, Ashok Tehim

Index: Bioorg. Med. Chem. Lett. 14(19) , 4847-50, (2004)

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Abstract

A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure-activity relationships studied. Potent ligands selective for human D(4) (hD(4)) over hD(2) and alpha(1) have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC(50) of 1500 nM.