477789-52-9Relevant academic research and scientific papers
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
Shepherd, Timothy A.,Aikins, James A.,Bleakman, David,Cantrell, Buddy E.,Rearick, John P.,Simon, Richard L.,Smith, Edward C. R.,Stephenson, Gregory A.,Zimmerman, Dennis M.,Mandelzys, Allan,Jarvie, Keith R.,Ho, Ken,Deverill, Michelle,Kamboj, Rajender K.
, p. 2101 - 2111 (2007/10/03)
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 (EC50 = 22.6 nM).
