Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid

…, L Brehm, P Krogsgaard-Larsen

Index: Christensen; Ebert; Madsen; Nielsen; Brehm; Krogsgaard-Larsen Journal of Medicinal Chemistry, 1992 , vol. 35, # 19 p. 3512 - 3519

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Citation Number: 33

Abstract

The~-isoxazo~ ol amino acid (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl) propionic acid (AMPA, 2) and the isomeric compound (RS)-2-amino-3-(3-hydroxy-4-methylisoxazol-5- yl) propionic acid (4-methylhomoibotenic acid, 4a) are potent agonists at the AMPA subtype of central excitatory amino acid receptors. Using 4a as a lead structure, the amino acids 4c- e, in which the 4-methyl group of 4a is replaced by substituents of different size and ...