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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 |
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| Authors: | Fernandez Maria-Carmen Castaño Ana Dominguez Esteban Escribano Ana Jiang Delu Jimenez Alma Hong Eric Hornback William J Nisenbaum Eric S Rankl Nancy Tromiczak Eric Vaught Grant Zarrinmayeh Hamideh Zimmerman Dennis M |
| Institution: | Lilly S.A., Avenida de la Industria, 30, 28108 Alcobendas, Madrid, Spain. fernandez_maria-carmen@lilly.com |
| 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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