BENZODIAZEPINE RECEPTOR LIGANDS - PART-II - SYNTHESIS AND BIOLOGICAL EVALUATION OF PYRAZOLO[5,1-C][1,2,4]BENZOTRIAZINE 4-OXIDE

Authors
COSTANZO A GUERRINI G BRUNI F CICIANI G SELLERI S CAPPELLETTI S COSTA B MARTINI C LUCACCHINI A
Citation
A. Costanzo et al., BENZODIAZEPINE RECEPTOR LIGANDS - PART-II - SYNTHESIS AND BIOLOGICAL EVALUATION OF PYRAZOLO[5,1-C][1,2,4]BENZOTRIAZINE 4-OXIDE, European journal of medicinal chemistry, 33(3), 1998, pp. 237-244
Citations number
18
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
33
Issue
3
Year of publication
1998
Pages
237 - 244
Database
ISI
SICI code
0223-5234(1998)33:3<237:BRL-P->2.0.ZU;2-E
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) af finities were evaluated in vitro in comparison with their 5-oxide isom ers 2. The 4-oxide compounds 3c,m,n,o showed a better receptor affinit y than their corresponding 5-oxide isomers, with an efficacy trend of antagonist/partial inverse agonist. From a structure-affinity relation ship point of view some insight in the role played by N-4 and Id-oxide is gained. (C) Elsevier, Paris.