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, M, Aldegheri, L, Andreotti, D and et al, (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. ISSN 0022-2623

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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
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science
Depositing User: Simon Ward
Date Deposited: 06 Feb 2012 18:28
Last Modified: 03 Oct 2012 12:38
URI: http://sro.sussex.ac.uk/id/eprint/16563
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