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

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.

SUBMITTER: Kuduk SD 

PROVIDER: S-EPMC4025801 | biostudies-literature | 2012 Dec

REPOSITORIES: biostudies-literature