Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology

…, P Uhlmann, S Morel, BL Eriksen…

Index: Eriksen, Birgitte Langer; Vedso, Per; Morel, Sandrine; Begtrup, Mikael Journal of Organic Chemistry, 1998 , vol. 63, # 1 p. 12 - 16

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Citation Number: 38

Abstract

A number of 1-hydroxyazole derivatives were synthesized as bioisosteres of (S)-glutamic acid (Glu) and as analogues of the AMPA receptor agonist (R, S)-2-amino-3-(3-hydroxy-5- methyl-4-isoxazolyl) propionic acid (AMPA, 3b). All compounds were subjected to in vitro pharmacological studies, including a series of Glu receptor binding assays, uptake studies on native as well as cloned Glu uptake systems, and the electrophysiological rat cortical ...

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