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

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Abstract
A series of 5H-pyrimido[5,4-d][2]benzazepines was synthesized, starting from the corresponding 2-benzazepin-5-ones and evaluated as potential anxiolytic agents [in rats, mice, squirrel monkeys or cats]. Selected compounds from this series show a pharmacological profile of action different from 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.