A new series of 2- and/or 3-substituted pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and their 8-chloro derivatives were synthesized, and their benzodiazepine receptor (BZR) affinities were evaluated in vitro in comparison to lead compound 3-ethoxycarbonyl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine-5-oxide (29) [1,2]. None of the new compounds showed significant affinity for BZR. On the basis of a pharmacophore/receptor model suggested for lead compound 29, some hypotheses to explain the inactivity of new derivatives are discussed. (C) 1999 Elsevier Science S.A. All rights reserved.
|Autori:||Guerrini G; Costanzo A; Bruni F; Ciciani G; Selleri S; Gratteri P; Costa B; Martini C; Lucacchini A|
|Titolo:||Benzodiazepine receptor ligands - III. Synthesis and biological evaluation of 2-and/or 3-substituted pyrazolo[5,1-c][l,2,4]benzotriazine 5-oxides|
|Anno del prodotto:||1999|
|Digital Object Identifier (DOI):||10.1016/S0014-827X(99)00044-0|
|Appare nelle tipologie:||1.1 Articolo in rivista|