(S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements, Structural and Biological Investigation.
Research output: Contribution to journal › Journal article › Research › peer-review
Starting from 1-4 and 7 structural templates, analogues based on bioisosteric replacements (5a-c vs 1, 2 and 6 vs 7) were synthesized for completing the SAR analysis. Interesting binding properties at GluA2, GluK1 and GluK3 receptors were discovered. The requirements for GluK3 interaction were elucidated determining the X-ray structures of the GluK3-LBD with 2 and 5c and by computational studies. Antinociceptive potential was demonstrated for GluK1 partial agonist 3 and antagonist 7 (2 mg/kg ip).
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 61 |
Issue number | 5 |
Pages (from-to) | 2124-2130 |
Number of pages | 7 |
ISSN | 0022-2623 |
DOIs | |
Publication status | Published - 8 Mar 2018 |
ID: 189836867