Replacement of a phenyl ring with N-linked heterocycles in a series of quinolone carboxylic acid M1 positive allosteric modulators was investigated. In particular, a pyrazole derivative exhibited improvements in potency, free fraction, and CNS exposure.
Kuduk, Scott D.,Marco, Christina N. Di,Cofre, Victoria,Pitts, Daniel R.,Ray, William J.,Ma, Lei,Wittmann, Marion,Veng, Lone,Seager, Matthew A.,Koeplinger, Kenneth,Thompson, Charles D.,Hartman, George D.,Bilodeau, Mark T.
scheme or table
p. 1334 - 1337
(2010/07/02)
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