[Synthesis and pharmacologic study of 1,5-dialkyl-1,5-benzodiazepine-2,4-dithiones].
The synthesis and psychotropic activity of 1,5-diakyl-1,5-benzodiazepine-2,4-dithiones (alkyl = methyl, ethyl and benzyl radicals) were studied. Alkylation reactions were performed in catalytic conditions by phase transfer. These reactions allowed us to isolate only one kind of product N-alkyl. Acute toxicity studies were conducted according to European protocols in two species of appropriate mammals in order to discover the lethal doses. The activity of the compounds on the CNS was then studied, using a battery of compartmental tests used in psychopharmacology. No toxicity was demonstrated at therapeutic doses. Each product had a sedative effect more or less pronounced and different from the reference substance clobazam (Urbanyl). They also had myorelaxant and anxiolytic effects, even lengthening the hypnotic effect of thiopental (synergic action).
Zellou
A
A
Laboratoire de Pharmacologie et de Toxicologie, Faculté de Médecine et de Pharmacie, Rabat-Instituts, Maroc.
Keita
A
A
Cherrah
Y
Y
Essassi
E M
EM
Hassar
M
M
D000478:Alkylation; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000078306:Clobazam; D015195:Drug Design; D004357:Drug Synergism; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D051379:Mice; D015394:Molecular Structure; D003473:Neuromuscular Nondepolarizing Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D011619:Psychotropic Drugs / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013329:Structure-Activity Relationship; D013874:Thiopental / Q000494:pharmacology
D014151:Anti-Anxiety Agents; D006993:Hypnotics and Sedatives; D003473:Neuromuscular Nondepolarizing Agents; D011619:Psychotropic Drugs; D001569:Benzodiazepines; D000078306:Clobazam; D013874:Thiopental