A series of 1,3-disubstituted[1]benzopyrano[2,3-c]pyrazol-4-ones were synthesized and tested in vitro as A1 and A2 adenosine receptor ligands. The binding results and a molecular modelling study indicated that the presence of a proton donor group in the N6-H region of adenosine and the 7-NH region of xanthine, respectively and occupancy of the A2 lipophilic area by a moiety endowed with an electrostatic effect are essential for receptor affinity and A2-selectivity.

NOVEL ADENOSINE RECEPTOR LIGANDS - 1,3-DISUBSTITUTED[1]BENZOPYRANO[2,3-C]PYRAZOL-4-ONES - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS

MARTINI, CLAUDIA;LUCACCHINI, ANTONIO
1993

Abstract

A series of 1,3-disubstituted[1]benzopyrano[2,3-c]pyrazol-4-ones were synthesized and tested in vitro as A1 and A2 adenosine receptor ligands. The binding results and a molecular modelling study indicated that the presence of a proton donor group in the N6-H region of adenosine and the 7-NH region of xanthine, respectively and occupancy of the A2 lipophilic area by a moiety endowed with an electrostatic effect are essential for receptor affinity and A2-selectivity.
Colotta, V; Cecchi, L; Catarzi, D; Melani, F; Filacchioni, G; Martini, Claudia; Tacchi, P; Lucacchini, Antonio
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/206167
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