Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor.

Christopher A Luckhurst,Omar Aziz,Vahri Beaumont,Roland W Bürli,Perla Breccia,Michel C Maillard,Alan F Haughan,Marieke Lamers,Phil Leonard,Kim L Matthews, Gilles Raphy,Andrew J Stott,Ignacio Munoz-Sanjuan, Beth Thomas,Michael Wall,Grant Wishart,Dawn Yates,Celia Dominguez

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

•Twenty hydroxamic acid inhibitors of class IIa histone deacetylases were synthesized.•Inhibitor 22 (CHDI-390576) was selective over class I and IIb histone deacetylases.•Inhibitor 22 can reach high exposure levels in mouse plasma, muscle and brain.

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关键词

CHDI-390576,Hydroxamic acid,CNS-penetrant,HDAC4 inhibition,Class IIa HDAC inhibitor

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