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

Yang, Zhi-Qiang; Shu, Youheng; Ma, Lei; Wittmann, Marion; Ray, William
J.; Seager, Matthew A.; Koeplinger, Kenneth A.; Thompson, Charles D.; Hartman, George
D.; Bilodeau, Mark T.; Kuduk, Scott D.

doi:10.1021/ml500055h.s001

ml500055h_si_001.pdf (233 kB)

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

journal contribution

posted on 08.05.2014, 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.

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

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

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