N-Heterocyclic Derived M-1 Positive Allosteric Modulators

Scott D. Kuduk,Christina N. Di Marco, Victoria Cofre,Daniel R. Pitts,William J. Ray,Lei Ma,Marion Wittmann,Lone Veng,Matthew A. Seager,Kenneth Koeplinger,Charles D. Thompson,George D. Hartman,Mark T. Bilodeau

Bioorganic & medicinal chemistry letters（2010）

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摘要

Replacement of a phenyl ring with N-linked heterocycles in a series of quinolone carboxylic acid M-1 positive allosteric modulators was investigated. In particular, a pyrazole derivative exhibited improvements in potency, free fraction, and CNS exposure. (C) 2010 Elsevier Ltd. All rights reserved.

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关键词

M-1,Muscarinic,Allosteric,Modulator,GPCR,Alzheimer's,Quinolone

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