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

Selective activation of the M-1 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 M-1 positive allosteric modulators and were found to possess good potency and in vivo efficacy.