Syntheses and structure-activity relationships of 6-aryl-4H-s-triazolo[3,4-c]thieno[2,3-e] [1,4]diazepines.
A variety of 6-aryl-4H-s-triazolo[3,4-c]thieno-[2,3-e][1,4]diazepines was synthesized and tested for antipentylenetetrazole activity and inhibition of fighting episodes. The structure-activity relationships are discussed. Some compounds were more active than diazepam in the two assays. Among them, 6-(o-chlorophenyl)-8-ethyl-1-methyl-4H-s-triazolo[3,4-c]thieno[2,3-e][1,4]diazepine was found to have favourable properties as an anxiolytic drug with very low toxicity. Clinical studies of this compound (Y-7131) are under way.
D000374:Aggression / Q000187:drug effects; D000818:Animals; D001381:Azepines / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006801:Humans; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D011619:Psychotropic Drugs / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D001381:Azepines; D011619:Psychotropic Drugs; D010433:Pentylenetetrazole