2-(2'-Hydroxyphenyl)-4-aryl-1,5-benzodiazepines as CNS active agents.
1-Aryl-3(2'-hydroxyphenyl)-propane-1,3-diones (III) have been prepared by the Baker-Venkataraman transformation of the corresponding 2-substituted benzoyl-oxyacetophenones (II). The aforesaid propane-1,3-diones (III) were condensed with o-phenylene diamine to give eight benzodiazepines (IV) which have been found to be very good MAO inhibitors (in vitro), and anticonvulsant and hypnotic (in vivo) agents. Some chemical leads on pharmacological activities have been observed.
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D001921:Brain / Q000201:enzymology; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis; D010424:Pentobarbital / Q000494:pharmacology; D011619:Psychotropic Drugs / Q000138:chemical synthesis*; D051381:Rats; D012890:Sleep / Q000187:drug effects
D000927:Anticonvulsants; D008996:Monoamine Oxidase Inhibitors; D011619:Psychotropic Drugs; D001569:Benzodiazepines; D010424:Pentobarbital