Document Report Card

ID: ALA1122390

Journal: J Med Chem

Title: 2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents.

Authors: Trybulski EJ, Benjamin LE, Earley JV, Fryer RI, Gilman NW, Reeder E, Walser A, Davidson AB, Horst WD, Sepinwall J.

Abstract: A series of 5H-pyrimido[5,4-d][2]benzazepines has been synthesized, starting from the corresponding 2-benzazepin-5-ones, and evaluated as potential anxiolytic agents. Selected compounds from this series show a pharmacological profile of action different than that of diazepam. They are more potent than diazepam in the anti-pentylenetetrazole test and in the [3H]diazepam binding assay, yet show less activity in the inclined screen test. A pharmacological data profile is given for 9-chloro-7-(2-chlorophenyl)-5H-pyrimido[5,4-d] [2]benzazepine (7c). The structure-activity relationships of these potential anxiolytic agents are discussed.

CiteXplore: 6138436

DOI: 10.1021/jm00365a008