This paper reports the synthesis of 1,2,3-triazolo[1,5-a][1,3] benzodiazepines, which represent a new heterocyclic system obtained by 1,3-dipolar cycloaddition reaction of ethyl 2-azidophenylacetate to methylenic compounds activated by a cyano group. The new derivatives were submitted to benzodiazepine receptor binding assays; only the 3-carboethoxy derivative 3c showed moderate receptorial affinity. However, on the basis of biological results, theoretical calculations were made, which suggested useful structural modifications.
Autori interni: | |
Autori: | Biagi G; Giorgi I; Livi O; Scartoni V; Velo S; DeSantis B; Martinelli A; Martini C; Senatore G |
Titolo: | 1,2,3-Triazolo[1,5-a][1,3]benzodiazepine a new heterocyclic system: Synthesis, benzodiazepine receptor binding and theoretical calculations |
Anno del prodotto: | 1996 |
Appare nelle tipologie: | 1.1 Articolo in rivista |
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