1,720,975 research outputs found
Guida pratica al riconoscimento delle sostanze iscritte nella V edizione della Farmacopea Europea
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Introduction of a hydroxy function on N6 8-azaadenine substituents to improve the solubility and the effectiveness of antagonists towards A1 adenosine receptors
No full textNEW 1,2,3-TRIAZOLO[1,5-a]QUINOXALINES: SYNTHESIS AND BINDING TO BENZODIAZEPINE AND ADENOSINE RECEPTORS. II
No full textOn 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
1,2,3-Triazol-carboxanilides and 1,2,3-triazol-(N-benzyl)-carboxamides as BK-potassium channel activators. XII
No full textThe chemical structures of many synthetic activators of large-conductance calcium-activated potassium channels (BK channels) satisfy a simple pharmacophore model, consisting of two appropriately substituted phenyl rings connected by a linker of a heterogeneous nature. In this paper, a series of new compounds with modifications of the linker portion of the above pharmacophore are described. In particular, in these new derivatives, the linker portion is represented by a 1,2,3-triazole-carboxamide group, which can be viewed as a combination of two different kinds of linker, independently used in previous series of BK-openers: the amide function and the 1,2,3-triazole ring. The overall finding of this study indicated that the triazole-carboxamide derivatives were generally poorly effective and that this structural modification of the linker is deleterious for activity on BK channels. Therefore, it can be hypothesized that the increase of the steric hindrance of the linker and/or the increase of the distance between the two aromatic portions are negative for the interaction with the biological target. (C) 2008 Elsevier Masson SAS. All rights reserved
New N6-cycloalkyl-1H-1,2,3-triazolo[4,5-c]Pyridines as potent of A1 Adenosine Receptor Antagonists
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Steroeselectivity as an evidence for a double insertion of Antagonists within A1 Adenosine Receptors
No full textA 3D Model of the Human A1 Adenosine Receptor. An Evaluation of the Binding Free-Energy with Ligands
No full textA 3D model of human A1 adenosine receptor. An evaluation of the binding free energy with ligands
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