On pursuing research about 1,2,3-triazolo[1,5-a]quinoxalines. in this paper we report synthesis and binding assays toward the benzodiazepine and A(1) and A(2A) adenosine receptors. of a new series of derivatives, bearing some structural changes (introduction of fluorine and trifluoromethyl in the seventh position, amino substituents in the fourth position, benzyl group in the fifth position and aroyl substituents in the third position). The biological tests have shown that only the 7-fluorosubstituted compounds 3a and 4a and the N-benzyl derivative 7 have a good affinity toward the benzodiazepine receptors, while only the 7-trifluoromethyl substituted compound 3b presents a moderate affinity with low selectivity toward the A, adenosine receptors. The other structural modifications strongly decreased biological activity. (C) 2002 Published by Editions scientifiques et medicales Elsevier SAS.
NEW 1,2,3-TRIAZOLO[1,5-a]QUINOXALINES: SYNTHESIS AND BINDING TO BENZODIAZEPINE AND ADENOSINE RECEPTORS. II
GIORGI, IRENE;LIVI, ORESTE;BETTI, LAURA;GIANNACCINI, GINO;TRINCAVELLI, MARIA LETIZIA
2002-01-01
Abstract
On pursuing research about 1,2,3-triazolo[1,5-a]quinoxalines. in this paper we report synthesis and binding assays toward the benzodiazepine and A(1) and A(2A) adenosine receptors. of a new series of derivatives, bearing some structural changes (introduction of fluorine and trifluoromethyl in the seventh position, amino substituents in the fourth position, benzyl group in the fifth position and aroyl substituents in the third position). The biological tests have shown that only the 7-fluorosubstituted compounds 3a and 4a and the N-benzyl derivative 7 have a good affinity toward the benzodiazepine receptors, while only the 7-trifluoromethyl substituted compound 3b presents a moderate affinity with low selectivity toward the A, adenosine receptors. The other structural modifications strongly decreased biological activity. (C) 2002 Published by Editions scientifiques et medicales Elsevier SAS.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
