| Autor: |
Vogensen, S. B., Clausen, R. P., Greenwood, J. R., Johansen, T. N., Pickering, D. S., Nielsen, B., Ebert, B., Krogsgaard-Larsen, P. |
| Zdroj: |
Journal of Medicinal Chemistry; May 2005, Vol. 48 Issue: 9 p3438-3442, 5p |
| Abstrakt: |
The synthesis and pharmacological characterization of 1- and 2-alkyltetrazolyl analogues of (RS)-2-amino-3-[3-hydroxy-5-(2-methyl-2H-5-tetrazolyl)-4-isoxazolyl]propionic acid (2-Me-Tet-AMPA), a highly potent and selective agonist at AMPA receptors, are presented. A shorter and more convergent synthetic route than previously described, employing a new method for introducing the amino acid moiety, was developed for these derivatives. The 2-substituted isomers were selective agonists, and their activity correlated inversely with the size of the substituent. Structural explanations of the structure−activity relationship are provided. |
| Databáze: |
Supplemental Index |
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