Potent and selective class IIa HDAC tetrasubstituted cyclopropane hydroxamic acid inhibitors were identified with high oral bioavailability that exhibited good brain and muscle exposure. Compound 14 displayed suitable properties for assessment of the impact of class IIa HDAC catalytic site inhibition in preclinical disease models.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4716601PMC
http://dx.doi.org/10.1021/acsmedchemlett.5b00302DOI Listing

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