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 ...
![7-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carbonitrile结构式](https://image.chemsrc.com/caspic/050/106937-66-0.png)
![7-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid结构式](https://image.chemsrc.com/caspic/018/84378-33-6.png)
![Formamide, N-[[5-(1-methylethyl)-1,2,4-oxadiazol-3-yl]methyl]- (9CI)结构式](https://image.chemsrc.com/caspic/373/122384-65-0.png)
