66194-29-4Relevant academic research and scientific papers
1,2,3-Triazolo [1,5-a][1,4]- and 1,2,3-triazolo[l,5-a]-[1,5]benzodiazepine derivatives: Synthesis and benzodiazepine receptor binding
Bertelli, Lucia,Biagi, Giuliana,Giorgi, Irene,Livi, Oreste,Manera, Clementina,Scartoni, Valerio,Martini, Claudia,Giannaccini, Gino,Trincavelli, Letizia,Barili, Pier Luigi
, p. 305 - 311 (2007/10/03)
This paper reports the synthesis of new 1,2,3-triazolo[1,4]benzodiazepine and 1,2,3-triazolo[1,5]benzodiazepine derivatives and their evaluation toward benzodiazepine receptors. Receptor affinity gradually and remarkably increases by moving the nitrogen atom of the central ring from position 3 through 4 to position 5, to give the most effective compound 6a (K(i) = 150 nM). N-methylation of the diazepine ring (7a) lowers receptorial binding. Introduction of a chlorine atom on the benzene ring doubles the K(i) value (6b) which remains unaltered by the N-methylation (7b).
