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.

Benzodiazepine receptor ligands - III. Synthesis and biological evaluation of 2-and/or 3-substituted pyrazolo[5,1-c][l,2,4]benzotriazine 5-oxides

COSTA, BARBARA;MARTINI, CLAUDIA;LUCACCHINI, ANTONIO
1999

Abstract

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.
Guerrini, G; Costanzo, A; Bruni, F; Ciciani, G; Selleri, S; Gratteri, P; Costa, Barbara; Martini, Claudia; Lucacchini, Antonio
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/206021
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