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Tricyclic Heteroaromatic Systems. 1,2,4-Triazolo[4,3-a]quinoxalines and 1,2,4-Triazino[4,3-a]quinoxalines: Synthesis and Central Benzodiazepine Receptor Activity

✍ Scribed by Vittoria Colotta; Daniela Catarzi; Flavia Varano; Lucia Cecchi; Guido Filacchioni; Alessandro Galli; Chiara Costagli

Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 416 KB
Volume: 330
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19973301206

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✦ Synopsis

Abstract

Some 1,2,4‐triazolo[4,3‐a]quinoxalines 1–10, and 1,2,4‐triazino[4,3‐a]quinoxalines 11–12 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The BZR affinity of 1–10 demonstrates that the presence of a proton acceptor at position‐1 is important for the potency of a BZR ligand. On the other hand, the BZR inactivity of the 1,2,5‐trione derivatives 11–12 shows that the right collocation of the essential L~2~ lipophilic substituent is of paramount importance for receptor‐ligand interaction.

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