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.

Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides

COSTA, BARBARA;MARTINI, CLAUDIA;LUCACCHINI, ANTONIO;
1999

Abstract

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.
Costanzo, A; Guerrini, G; Ciciani, G; Bruni, F; Selleri, S; Costa, Barbara; Martini, Claudia; Lucacchini, Antonio; Aiello, Pm; Ipponi, A.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/203422
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