期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 6, 页码 263-267出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100095k
关键词
Quinolizidinone; M-1 muscarinic receptor; allosteric modulator; cognition; Alzheimer's
Positive allosteric modulation of the M, muscarinic receptor represents an approach to treat the cognitive decline in patients with Alzheimer's disease. Replacement of a quinolone ring system in a quinolone carboxylic acid series of M, modulators with a quinolizidinone bearing a basic amine linkage led to a series of compounds with higher free fraction, enhanced CNS exposure, and improved efficacy in rodent in vivo models of cognition.
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