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 N-oxide is gained.
Benzodiazepine receptor ligands - Part II. Synthesis and biological evaluation of pyrazolo[5,1-c][1,2,4]benzotriazine 4-oxide / Costanzo A.; Guerrini G.; Bruni F.; Ciciani G.; Selleri S.; Cappelletti S.; Costa B.; Martini C.; Lucacchini A.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - ELETTRONICO. - 33:(1998), pp. 237-244. [10.1016/S0223-5234(98)80013-5]
Benzodiazepine receptor ligands - Part II. Synthesis and biological evaluation of pyrazolo[5,1-c][1,2,4]benzotriazine 4-oxide
Costanzo A.;Bruni F.;Ciciani G.;Selleri S.;CAPPELLETTI, SILVIA;
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 N-oxide is gained.
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