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

鉴定酰胺类化合物作为喹诺里酮类m1正向变构调节剂的羧酸替代物

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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.

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