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

…, S Selleri, P Gratteri, B Costa, C Martini, A Lucacchini

Index: Guerrini; Costanzo; Bruni; Ciciani; Selleri; Gratteri; Costa; Martini; Lucacchini Farmaco, 1999 , vol. 54, # 6 p. 375 - 389

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Citation Number: 10

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 ...