Novel benzodiazepine receptor partial agonists: oxadiazolylimidazobenzodiazepines

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...

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Veröffentlicht in:	Journal of medicinal chemistry 1989-10, Vol.32 (10), p.2282-2291
Hauptverfasser:	Watjen, F, Baker, R, Engelstoff, M, Herbert, R, MacLeod, A, Knight, A, Merchant, K, Moseley, J, Saunders, J, Swain, C J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzodiazepines - chemical synthesis Benzodiazepines - pharmacology Cell Membrane - metabolism Cerebral Cortex - metabolism Models, Molecular Molecular Conformation Molecular Structure Oxadiazoles - chemical synthesis Oxadiazoles - pharmacology Rats Rats, Inbred Strains Receptors, GABA-A - drug effects Receptors, GABA-A - metabolism Structure-Activity Relationship X-Ray Diffraction
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