The synthesis of new 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and their binding activities at the central benzodiazepine receptor (BZR) are reported. The derivatives substituted at the 3-position with electron-rich five-membered rings, such as pyrrole 11, 2-thiophene 13c, or 3-thiophene 13d, showed good affinity values for BZR. In in vivo tests the 3-(thien-3-yl)-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide; (13d) showed selective anticonvulsant activity.
Autori interni: | |
Autori: | Costanzo A; Guerrini G; Ciciani G; Bruni F; Selleri S; Costa B; Martini C; Lucacchini A; Aiello PM; Ipponi A |
Titolo: | Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides |
Anno del prodotto: | 1999 |
Digital Object Identifier (DOI): | 10.1021/jm981126y |
Appare nelle tipologie: | 1.1 Articolo in rivista |
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