Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

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 ORCID: https://orcid.org/0000-0002-8745-8377, Harries, Mark, Aldegheri, Laura, Andreotti, Daniele, Ballantine, Stuart, Bax, Benjamin D. ORCID: https://orcid.org/0000-0003-1940-3785, 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

Full text not available from this repository.

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: 23 Oct 2022 12:59
URI: https://orca.cardiff.ac.uk/id/eprint/109342

Citation Data

Cited 41 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item