Discovery ofN-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a Novel Clinical AMPA Receptor Positive Modulator
Journal of Medicinal Chemistry2010Vol. 53(15), pp. 5801–5812
Citations Over TimeTop 12% of 2010 papers
Simon E. Ward, Mark H Harries, Laura Aldegheri, Daniele Andreotti, Stuart P. Ballantine, B.D. Bax, A. I. Harris, A.J. Harker, Jesper Lund, Rosemary A. Melarange, Anna Mingardi, Claudette Mookherjee, J. Mosley, M. Neve, Beatrice Oliosi, Roberto Profeta, Kathrine J. Smith, Paul W. Smith, Simone Spada, Kevin M. Thewlis, Shahnaz P. Yusaf
Abstract
A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i, a potent, efficacious CNS penetrant molecule with an excellent pharmacokinetic profile across preclinical species, which is well tolerated and is also orally bioavailable in humans.
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