STRUCTURE-ACTIVITY RELATIONSHIP OF s-TRIAZOLO 1, 4-BENZODIAZEPINES IN CENTRAL NERVOUS DEPRESSANT ACTION

概要

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A variety of the central depressant effects of 1, 4-benzodiazepines have been well documented (1-3). Shimamoto and Takaori (4), and Nakajima et al. (5) also have reported the potent sedative, taming, muscle relaxant and anti-convulsive properties of 1-alkylcarbamoyl-1, 4-benzodiazepin-2-ones synthesized by Usui et al. (6). Most of the chemical studies in this area have been devoted to syntheses of the derivatives of 1, 4-benzodiazepines with relatively simple substituents at 1, 2 or 3 position or in phenyl ring as exemplified by chlordiazepoxide, diazepam, oxazepam and nitrazepam. On the other hand, Meguro and Kuwada (7) in this Chemical Laboratories have synthesized a number of novel 6-phenyl-4H-s-triazolo-[4, 3a] [1, 4] benzodiazepines with a tricyclic ring system.<BR> The present report deals with the anticonvulsive, muscle relaxant, sedative and taming effects of these novel compounds in small experimental animals. In these respects, it was proved that several derivatives including 8-chloro-6-phenyl-4H-s-triazolo-[4, 3a] [1, 4] benzodiazepine (D-40TA) and 1-methyl-8-chloro-6-phenyl-4H-s-triazolo [4, 3a] [1, 4] benzodiazepine (D-65MT) were more effective in the central depression than diazepam and nitrazepam.
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