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Discovery of Naphthyl-Fused 5‑Membered Lactams as a New Class of M1 Positive Allosteric Modulators

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journal contribution
posted on 2014-05-08, 00:00 authored by Zhi-Qiang Yang, Youheng Shu, Lei Ma, Marion Wittmann, William J. Ray, Matthew A. Seager, Kenneth A. Koeplinger, Charles D. Thompson, George D. Hartman, Mark T. Bilodeau, Scott D. Kuduk
Selective activation of the M1 muscarinic receptor via positive allosteric modulation represents an original approach to treat the cognitive decline in patients with Alzheimer’s disease. A series of naphthyl-fused 5-membered lactams were identified as a new class of M1 positive allosteric modulators and were found to possess good potency and in vivo efficacy.