Benzodiazepine receptor (BZR) ligands. 6 new 3-(2-,3- or 4-substituted benzyloxycarbonyl) derivatives of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide: Receptor affinity and in vivo testing

Authors
Costanzo, A Guerrini, G Ciciani, G Bruni, F Costagli, C Selleri, S Costa, B Martini, C Aiello, PM
Citation
A. Costanzo et al., Benzodiazepine receptor (BZR) ligands. 6 new 3-(2-,3- or 4-substituted benzyloxycarbonyl) derivatives of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide: Receptor affinity and in vivo testing, MED CHEM RE, 10(6), 2001, pp. 366-377
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
MEDICINAL CHEMISTRY RESEARCH
ISSN journal
10542523 → ACNP
Volume
10
Issue
6
Year of publication
2001
Pages
366 - 377
Database
ISI
SICI code
1054-2523(2001)10:6<366:BR(L6N>2.0.ZU;2-G
Abstract
The synthesis of new 3-(2-, 3- or 4-substituted benzyloxycarbonyl) derivati ves of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide and their bi nding affinities at the central benzodiazepine receptor (BZR) are reported. Among the synthesized compounds, the eater 12, having the best affinity (K -i = 1 nM), and compounds 5 and 10 were chosen for in vivo testing.