Cyclopenta[e] [1,5] benzodiazepin-10 (9H)-one derivatives as CNS depressant agents.
A series of dialkylaminoalkyl derivatives of cyclopenta[e] [1,5] benzodiazepin-10(9H)-one (E1-4) and its 6-chloro derivative (E5-8) was prepared to evaluate their CNS activity in comparison with that of isosteric pyridodiazepinones (A1-4) previously described. The results of the pharmacological screening show a significant depressant activity more remarkable in 6-chloro derivatives, which also revealed a high and lasting analgesic activity. The replacement of pyridine with benzene nucleus did not show any significant or homogeneous activity variation.
Istituto di Tecnica Farmaceutica, Università di Sassari.
A
A
Mulé
G
G
Pirisino
M D
MD
Moretti
F
F
Savelli
A
A
Boido
M
M
Satta
A
A
Peana
D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D002492:Central Nervous System Depressants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D005260:Female; D007928:Lethal Dose 50; D051379:Mice
D000700:Analgesics; D002492:Central Nervous System Depressants; D001569:Benzodiazepines