A series of 1- and 2-[3-[4-(X)-1-piperazinyl]-propyl]benzotriazoles were prepared and evaluated for their trazodone-like pharmacological profile; as preliminary pharmacological screening, the compounds were tested for their antiserotonergic, antiadrenergic and antihistamine in vitro activity as well as for their analgesic in vivo action. Structure-activity relationships showed that among the synthesized compounds, the analogues bearing on the 4-piperazine nitrogen either an unsubstituted phenyl ring or a 2- or 3-chloro phenyl moiety show a pharmacological profile similar to that of the antidepressant trazodone.
Synthesis and trazodone-like pharmacological profile of 1- and 2-[3-[4(X)-1-piperazinyl]-propyl]-benzotriazoles / Caliendo, Giuseppe; Di Carlo, R.; Meli, Rosaria; Perissutti, Elisa; Santagada, Vincenzo; Silipo, C.; Vittoria, A.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 28:12(1993), pp. 969-974. [10.1016/0223-5234(93)90053-H]
Synthesis and trazodone-like pharmacological profile of 1- and 2-[3-[4(X)-1-piperazinyl]-propyl]-benzotriazoles
CALIENDO, GIUSEPPE;MELI, ROSARIA;PERISSUTTI, ELISA;SANTAGADA, VINCENZO;
1993
Abstract
A series of 1- and 2-[3-[4-(X)-1-piperazinyl]-propyl]benzotriazoles were prepared and evaluated for their trazodone-like pharmacological profile; as preliminary pharmacological screening, the compounds were tested for their antiserotonergic, antiadrenergic and antihistamine in vitro activity as well as for their analgesic in vivo action. Structure-activity relationships showed that among the synthesized compounds, the analogues bearing on the 4-piperazine nitrogen either an unsubstituted phenyl ring or a 2- or 3-chloro phenyl moiety show a pharmacological profile similar to that of the antidepressant trazodone.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
