Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 15, Pages 5801-5812Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm1005429
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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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