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Discovery of N-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator

Ward, Simon, Harries, Mark, Aldegheri, Laura, Andreotti, Daniele, Ballantine, Stuart, Bax, Benjamin D., Harris, Andrew J., Harker, Andy J., Lund, Jesper, Melarange, Rosemary, Mingardi, Anna, Mookherjee, Claudette, Mosley, Julie, Neve, Marta, Oliosi, Beatrice, Profeta, Roberto, Smith, Kathrine J., Smith, Paul W., Spada, Simone, Thewlis, Kevin M. and Yusaf, Shahnaz P. 2010. Discovery of N-[(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 Chemistry 53 (15) , pp. 5801-5812. 10.1021/jm1005429

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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.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Medicine
Publisher: ACS Publications
ISSN: 0022-2623
Last Modified: 07 Nov 2019 15:54
URI: http://orca-mwe.cf.ac.uk/id/eprint/109342

Citation Data

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