Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 1, Pages 34-39Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00302
Keywords
Class IIa HDAC inhibitors; hydroxamic acid; CNS exposure; tetrasubstituted cyclopropane; cyclopropanation; Huntington's disease
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Potent and selective class Ha 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 Ha HDAC catalytic site inhibition in preclinical disease models.
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