European Journal of Medicinal Chemistry p. 113 - 122 (1998)
Update date:2022-07-31
Topics:
Bertelli, Lucia
Biagi, Giuliana
Giorgi, Irene
Manera, Clementina
Livi, Oreste
Scartoni, Valerio
Betti, Laura
Giannaccini, Gino
Trincavelli, Letizia
Barili, Pier Luigi
This paper reports the synthesis and binding assays toward benzodiazepine and adenosine A1 and A(2A) receptors of new 1,2,3-triazolo[1,5-a]quinoxalin-4-one derivatives. The prepared compounds show good affinity toward the benzodiazepine receptor (K(i) 53-314 nM); the GABA ratio values suggest an inverse agonist activity for the N(5) unsubstituted compounds 6b-d and an agonist activity for the N(5) methylated compounds 7a-c. Some derivatives of both series show good affinity (K(i) < 100 nM) and selectivity toward the adenosine A1 receptorial subtype.
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Doi:10.1271/bbb.62.521
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