- Syntheses and structure-activity relationships of 6-Aryl-4H-s-triazolo[3,4-c]thieno[2,3-e][1,4]diazepines
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A variety of 6 aryl 4H s triazolo [3,4-c]thieno [2,3-e] [1,4]diazepines was synthesized and tested for anti-pentylenetetrazole 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.
- Tahara,Araki,Shiroki,Matsuo,Munakata
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p. 1153 - 1158
(2007/10/08)
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