Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones.
The syntheses of 2-amino-N-(2-benzoyl)-4-chlorophenyl)acetamides are reported. The pharmacological properties of these compounds were compared with data obtained from the corresponding cyclized products [5-(2,6-dichlorophenyl)-1,4-benzodiazepin-2-ones]. Evidence is presented which suggests that the central nervous system activity observed for 1,4-benzodiazepines is inherent only in the closed seven-membered ring and is not due to the ring-opened form.
D000081:Acetamides / Q000138:chemical synthesis*; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis*; D001570:Benzodiazepinones / Q000138:chemical synthesis*; D001667:Binding, Competitive / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D003975:Diazepam / Q000378:metabolism; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D000081:Acetamides; D014151:Anti-Anxiety Agents; D001570:Benzodiazepinones; D003975:Diazepam; D010433:Pentylenetetrazole