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1, 2, 3-Triazolo [1, 5-a][1, 4]-and 1, 2, 3-triazolo [1, 5-a][1, 5] benzodiazepine derivatives: synthesis and benzodiazepine receptor binding

L Bertelli, G Biagi, I Giorgi, O Livi, C Manera, V Scartoni…

Index: Bertelli, Lucia; Biagi, Giuliana; Giorgi, Irene; Livi, Oreste; Manera, Clementina; Scartoni, Valerio; Martini, Claudia; Giannaccini, Gino; Trincavelli, Letizia; Barili, Pier Luigi Farmaco, 1998 , vol. 53, # 4 p. 305 - 311

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Citation Number: 29

Abstract

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 (Ki= 150 nM). N-methylation of the diazepine ring (7a) lowers receptorial ...