BENZODIAZEPINE RECEPTOR LIGANDS. SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF 3-, 7- AND 8-SUBSTITUTED [5, 1-C] [1, 2, 4] BENZOTRIAZEPINES AND 5-OXIDE DERIVATIVES. PART I

Abstract

Summary A new series of 3-, 7- and 8-substituted pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and a series of pyrazolo[5,1-c] [1,2,4]benzotriazines were synthesized and their benzodiazepine receptor affinities were evaluated in vitro. A study of structureaffinity relationships within the series is briefly discussed, considering the role of various substituents at the 3-, 7- and 8-positions and the role of N5-oxide. Compounds 1b, 1c, 1cR, 4c, 4cR, 9d, 12d and 12dR were evaluated in vivo for their anticonvulsant effects