Mulè, Antonio Calogero and Pirisino, Gerolamo Antonio and Moretti, Mario Domenico Luigi and Savelli, Francesco and Boido, A. and Satta, M. and Peana, Alessandra Tiziana (1994) Cyclopenta[e] [1,5] benzodiazepin-10 (9H)-one derivatives as CNS depressant agents. Bollettino chimico farmaceutico, Vol. 133 (3), p. 167-172. ISSN 0006-6648. Article.
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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.
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