Details

Autor(en) / Beteiligte

• Catarzi, Daniela
• Colotta, Vittoria
• Varano, Flavia
• Filacchioni, Guido
• Martini, Claudia
• Trincavelli, Letizia
• Lucacchini, Antonio

Titel

1,2,4-Triazolo[1,5- a]quinoxaline derivatives: synthesis and biological evaluation as adenosine receptor antagonists

Ist Teil von

• Farmaco (Società chimica italiana : 1989), 2004-02, Vol.59 (2), p.71-81

Ort / Verlag

France: Elsevier SAS

Erscheinungsjahr

2004

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• Since most of the reported adenosine receptor antagonists are 2-(hetero)aryl-substituted tricyclic heteroaromatic derivatives, in the present study we report the synthesis and the biological evaluation of a new set of 4-amino-1,2,4-triazolo[1,5- a]quinoxalines containing at position-2 an ethyl carboxylate group or a hydrogen atom. The structure–activity relationships on these compounds were in accordance with those of a previously reported series of analogous size and shape, thus suggesting a similar A 1-binding mode. In particular, the binding data indicate that alkylation of the 4-amino group of these derivatives lead to potent A 1-receptor antagonists. Moreover, as new results, this study has pointed out that the ethyl 2-carboxylate group can advantageously replace the 2-(hetero)aryl ring of previously reported triazoloquinoxaline derivatives, affording an ameliorated interaction with the A 1-receptor subtype.