Collect. Czech. Chem. Commun.
1983, 48, 123-136
https://doi.org/10.1135/cccc19830123
S-Substituted derivatives of 8-chloro-6-(2-chlorophenyl)-1-mercaptomethyl-4H-s-triazolo[4,3-a]-1,4-benzodiazepine; Synthesis and pharmacology
Zdeněk J. Vejdělek, Jan Metyš and Miroslav Protiva
Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3
Abstract
Reactions of 7-chloro-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-thione (XVIII) and its 5-(2-chlorophenyl) analogue XIX with hydrazines of methylthio-, ethylthio-, cyclohexylthio-, phenylthio-, 4-tolylthio-, 4-chlorophenylthio-, benzylthio-, S-(2-dimethylaminoethyl)thio-, 2-furfurylthio- and 3-pyridylmethylthioacetic acid in boiling butanol gave substance VII and the title compounds VIII-XVII. The synthesis of hydrazines XXVIII-XXXII is described. The compounds prepared are very little toxic, have strong discoordinating activity and are very potent as anticonvulsant agents. In this line they are substantially more active than alprazolam (II) and are not far behind triazolam (III).
