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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

By Simon Ward, M Harries, L Aldegheri, D Andreotti and et al

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

Topics: Q
Year: 2010
DOI identifier: 10.1021/jm1005429
OAI identifier: oai:sro.sussex.ac.uk:16563
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