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ChemInform Abstract: 1-Substituted 4-[Chloropyrazolyl][1,2,4]triazolo[4,3-a]quinoxalines: Synthesis and Structure—Activity Relationships of a New Class of Benzodiazepine and Adenosine Receptor Ligands.

✍ Scribed by B. MATUSZCZAK; E. PEKALA; C. E. MUELLER

Publisher
John Wiley and Sons
Year
2010
Weight
38 KB
Volume
29
Category
Article
ISSN
0931-7597

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✦ Synopsis

Substituted 4-[Chloropyrazolyl][1,2,4]triazolo[4,3-a]quinoxalines: Synthesis and Structure-Activity Relationships of a New Class of Benzodiazepine and Adenosine Receptor Ligands. -A series of substituted triazoloquinoxaline derivatives (VI) (6 examples) is synthesized starting from quinoxalinone (I) and evaluated for their affinities for benzodiazepine as well as for adenosine A 1 -and A 2A -receptors by radioligand binding assays. Compound (VIa) exhibits submicromolar affinity for the benzodiazepine binding site of GABA A receptors. The 2-thienylmethyl derivative (VId) is the most potent and selective A 1 -AR ligand of the present series. -(MATUSZCZAK,

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## 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