A new series of 3-, 8-substituted pyrazolo[5,1-c][1,2,4]benzotriazine 4-oxides 3 were synthesized and their benzodiazepine receptor (BZR) affinities were evaluated in vitro in comparison with their 5-oxide isomers 2. The 4-oxide compounds 3c,m,n,o showed a better receptor affinity than their corresponding 5-oxide isomers, with an efficacy trend of antagonist/partial inverse agonist. From a structure-affinity relationship point of view some insight in the role played by N-4 and Id-oxide is gained. (C) Elsevier, Paris.

Benzodiazepine receptor ligands-Part II. Synthesis and biological evaluation of pyrazolo[5,1-c][1,2,4]benzotriazine 4-oxide

COSTA, BARBARA;MARTINI, CLAUDIA;LUCACCHINI, ANTONIO
1998

Abstract

A new series of 3-, 8-substituted pyrazolo[5,1-c][1,2,4]benzotriazine 4-oxides 3 were synthesized and their benzodiazepine receptor (BZR) affinities were evaluated in vitro in comparison with their 5-oxide isomers 2. The 4-oxide compounds 3c,m,n,o showed a better receptor affinity than their corresponding 5-oxide isomers, with an efficacy trend of antagonist/partial inverse agonist. From a structure-affinity relationship point of view some insight in the role played by N-4 and Id-oxide is gained. (C) Elsevier, Paris.
Costanzo, A.; Guerrini, G.; Bruni, F.; Ciciani, G.; Selleri, S.; Cappelletti, S.; 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/11568/205746
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