| Autor: |
Shepherd TA; NPS Allelix Corporation, 6850 Goreway Drive, Mississaugua, Ontario L4V 1V7, Canada. Shepherd_Timothy@Lilly.com, Aikins JA, Bleakman D, Cantrell BE, Rearick JP, Simon RL, Smith EC, Stephenson GA, Zimmerman DM, Mandelzys A, Jarvie KR, Ho K, Deverill M, Kamboj RK |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2002 May 09; Vol. 45 (10), pp. 2101-11. |
| DOI: |
10.1021/jm0105474 |
| Abstrakt: |
2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) potentiators are ligands that act as positive allosteric modulators at the AMPA receptors. We recently disclosed a novel series of 2-arylpropylsulfonamides that were potent potentiators of responses mediated through AMPA receptors. To further define the structural requirements for activity in this series, new ring-constrained analogues were prepared and a new stereocenter was introduced. The potentiating activity was highly dependent on the stereochemistry at the 2-position of the disubstituted cyclopentane and was independent of the relative stereochemistry at the 1-position. Compound (R,R)-10 represents a potent, novel potentiator of iGluR4 flip receptors (EC(50) = 22.6 nM). |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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