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.
Cyclopenta[e][1,5]benzodiazepin-10(9H)-one derivatives as CNS depressant agents / A., Mule'; G., Pirisino; M. D., Moretti; F., Savelli; A., Boido; M., Satta; Peana, Alessandra Tiziana. - In: BOLLETTINO CHIMICO FARMACEUTICO. - ISSN 0006-6648. - 133:3(1994), pp. 167-172.
Cyclopenta[e][1,5]benzodiazepin-10(9H)-one derivatives as CNS depressant agents
PEANA, Alessandra Tiziana
1994-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.