1309079-99-9Relevant articles and documents
Identification of amides as carboxylic acid surrogates for quinolizidinone-based M1 positive allosteric modulators
Kuduk, Scott D.,Chang, Ronald K.,Greshock, Thomas J.,Ray, William J.,Ma, Lei,Wittmann, Marion,Seager, Matthew A.,Koeplinger, Kenneth A.,Thompson, Charles D.,Hartman, George D.,Bilodeau, Mark T.
supporting information, p. 1070 - 1074 (2013/02/22)
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.