Tahara T, Araki K, Shiroki M, Matsuo H, Munakata T
Arzneimittelforschung. 1978;28(7):1153-8. doi: 10.1002/chin.197844214.
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.
合成了多种6-芳基-4H-s-三唑并[3,4-c]噻吩并[2,3-e][1,4]二氮杂卓，并测试了其抗戊四氮活性和对打斗发作的抑制作用。讨论了构效关系。在这两种试验中，一些化合物比地西泮更具活性。其中，6-(邻氯苯基)-8-乙基-1-甲基-4H-s-三唑并[3,4-c]噻吩并[2,3-e][1,4]二氮杂卓被发现具有作为一种毒性极低的抗焦虑药物的良好特性。该化合物（Y-7131）的临床研究正在进行中。
