Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines

F Watjen, R Baker, M Engelstoff, R Herbert…

Index: Watjen, Frank; Baker, Raymond; Engelstoff, Mogens; Herbert, Richard; MacLeod, Angus; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 10 p. 2282 - 2291

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Citation Number: 138

Abstract

The synthesis and biochemical evaluation of a series of oxadiazole derivatives of imidazobenzodiazepines related to the benzodiazepine antagonist Ro 15-1788 (2a) are reported. Although the oxadiazole ring is seen as an isosteric replacement for the ester linkage, significant differences in structure-activity trends were observed. Specifically, oxadiazoles 9-12 invariably had increased receptor efficacy (as witnessed by ...