Il Farmaco

Synthesis and pharmacological characterisation of a conformationally restrained series of indole-2-carboxylates as in vivo potent glycine antagonists

…, P Gastaldi, SA Giacobbe, F Micheli, G Pentassuglia

Index: Di Fabio, Romano; Araldi, Gianluca; Baraldi, Davide; Cugola, Alfredo; Donati, Daniele; Gastaldi, Paola; Giacobbe, Simone A; Micheli, Fabrizio; Pentassuglia, Giorgio Farmaco, 2001 , vol. 56, # 10 p. 791 - 798

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Citation Number: 7

Abstract

After the identification of GV150526, the indole-2-carboxylate template was further explored in order to identify novel potential anti-stroke agents. In particular, the SAR of the side chain present at the C-3 position of the indole nucleus was widely studied. In this paper, the synthesis and the pharmacological profile of a further class of conformationally restricted analogues of GV150526 as in vitro and in vivo potent glycine antagonists is reported. In ...