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Substituted 1,2,3-Triazolo[1,5-a]quinazolines: Synthesis and Binding to Benzodiazepine and Adenosine Receptors. -Cyclization reactions and nucleophilic displacement are carried out to form new title compounds, e.g. (V), (VIII), and (XI). These compounds show decreased activity compared to triazoloquinazoline derivatives. The most potent compounds within this study are found to be the derivatives (VIII) and (XI). -(BERTELLI,

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This paper reports the synthesis and binding assays toward benzodiazepine and adenosine A(1) 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 (Ki < 100 nM) and selectivity toward the adenosine A(1) receptorial subtype. (C) Elsevier, Paris

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