ml500055h_si_001.pdf (233 kB)
Download fileDiscovery of Naphthyl-Fused 5‑Membered Lactams as a New Class of M1 Positive Allosteric Modulators
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. KudukSelective 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.