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.

1,2,3-Triazolo[1,5-a][1,3]benzodiazepine a new heterocyclic system: Synthesis, benzodiazepine receptor binding and theoretical calculations

GIORGI, IRENE;MARTINELLI, ADRIANO;MARTINI, CLAUDIA;
1996

Abstract

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.
Biagi, G; Giorgi, Irene; Livi, O; Scartoni, V; Velo, S; Desantis, B; Martinelli, Adriano; Martini, Claudia; Senatore, G.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/204817
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