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 / Costanzo A.; Guerrini G.; Ciciani G.; Bruni F.; Selleri S.; Costa B.; Martini C.; Lucacchini A.; Malmberg Aiello P.; Ipponi A.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 1520-4804. - ELETTRONICO. - 42:(1999), pp. 2218-2226. [10.1021/jm981126y]
Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5- oxides
Costanzo A.;Ciciani G.;Bruni F.;Selleri S.;Costa B.;Malmberg Aiello P.;
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.
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