Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino) ethyl]-1, 4-benzodiazepines as κ-opioid receptor agonists endowed with …

M Anzini, L Canullo, C Braile, A Cappelli…

Index: Anzini, Maurizio; Canullo, Laura; Braile, Carlo; Cappelli, Andrea; Gallelli, Andrea; Vomero, Salvatore; Menziani, M. Cristina; De Benedetti, Pier G.; Rizzo, Milena; Collina, Simona; Azzolina, Ornella; Sbacchi, Massimo; Ghelardini, Carla; Galeotti, Nicoletta Journal of Medicinal Chemistry, 2003 , vol. 46, # 18 p. 3853 - 3864

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Citation Number: 30

Abstract

The synthesis and biological evaluation of a series of new derivatives of 2-substituted 5- phenyl-1, 4-benzodiazepines, structurally related to tifluadom (5), are reported. Chemical and pharmacological studies on compounds 6 have been pursued with the aim of expanding the SAR data and validating the previously proposed model of interaction of this class of compounds with the κ-opioid receptor. The synthesis of the previously described ...