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.
|Autori:||COSTANZO A.; GUERRINI G.; BRUNI F.; CICIANI G.; SELLERI S.; CAPPELLETTI S.; COSTA B; MARTINI C.; LUCACCHINI A.|
|Titolo:||Benzodiazepine receptor ligands-Part II. Synthesis and biological evaluation of pyrazolo[5,1-c][1,2,4]benzotriazine 4-oxide|
|Anno del prodotto:||1998|
|Digital Object Identifier (DOI):||10.1016/S0223-5234(98)80013-5|
|Appare nelle tipologie:||1.1 Articolo in rivista|