2. Academic Validation
  3. A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives

A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives

  • Bioorg Med Chem Lett. 2006 Oct 1;16(19):5057-61. doi: 10.1016/j.bmcl.2006.07.035.
Maria-Carmen Fernandez 1,  Ana Castaño,  Esteban Dominguez,  Ana Escribano,  Delu Jiang,  Alma Jimenez,  Eric Hong,  William J Hornback,  Eric S Nisenbaum,  Nancy Rankl,  Eric Tromiczak,  Grant Vaught,  Hamideh Zarrinmayeh,  Dennis M Zimmerman
Affiliations

Affiliation

  • 1 Lilly S.A., Avenida de la Industria, 30, 28108 Alcobendas, Madrid, Spain. fernandez_maria-carmen@lilly.com
PMID: 16879964 DOI: 10.1016/j.bmcl.2006.07.035
Abstract

The synthesis and initial SAR studies of novel, highly potent positive allosteric modulators of AMPA receptors based on 3-(4-tert-butylphenyl)-4-cyano-5-methylsulfanyl-thiophene-2-carboxylic acid (6a) are described. SAR studies at the thioether moiety indicated that substitution at this position was mandatory and better potency was achieved with small groups.

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