Document Report Card

ID: ALA2203078

Journal: ACS Med Chem Lett

Title: Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.

Authors: Kuduk SD, Chang RK, Greshock TJ, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Abstract: Selective activation of the M1 muscarinic receptor via positive allosteric modulation represents an approach to treat the cognitive decline in patients with Alzheimer's disease. A series of amides were examined as a replacement for the carboxylic acid moiety in a class of quinolizidinone carboxylic acid M1 muscarinic receptor positive allosteric modulators, and leading pyran 4o and cyclohexane 5c were found to possess good potency and in vivo efficacy.

CiteXplore: 24900430

DOI: 10.1021/ml300280g