2. Academic Validation
  3. Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors

Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors

  • J Med Chem. 2002 May 9;45(10):2101-11. doi: 10.1021/jm0105474.
Timothy A Shepherd 1,  James A Aikins,  David Bleakman,  Buddy E Cantrell,  John P Rearick,  Richard L Simon,  Edward C R Smith,  Gregory A Stephenson,  Dennis M Zimmerman,  Allan Mandelzys,  Keith R Jarvie,  Ken Ho,  Michelle Deverill,  Rajender K Kamboj
Affiliations

Affiliation

  • 1 NPS Allelix Corporation, 6850 Goreway Drive, Mississaugua, Ontario L4V 1V7, Canada. Shepherd_Timothy@Lilly.com
PMID: 11985477 DOI: 10.1021/jm0105474
Abstract

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).

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