title: Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.
abstract: 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.
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Luckhurst
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Perla
authors.initials: P
authors.lastname: Breccia
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Stott
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Omar
authors.initials: O
authors.lastname: Aziz
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Helen L
authors.initials: HL
authors.lastname: Birch
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Roland W
authors.initials: RW
authors.lastname: Bürli
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Samantha J
authors.initials: SJ
authors.lastname: Hughes
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Rebecca E
authors.initials: RE
authors.lastname: Jarvis
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Marieke
authors.initials: M
authors.lastname: Lamers
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Philip M
authors.initials: PM
authors.lastname: Leonard
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Kim L
authors.initials: KL
authors.lastname: Matthews
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: George
authors.initials: G
authors.lastname: McAllister
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Scott
authors.initials: S
authors.lastname: Pollack
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Saville-Stones
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Grant
authors.initials: G
authors.lastname: Wishart
authors.affiliation: BioFocus, Charles River , Chesterford Research Park, Saffron Walden, Essex, CB10 1XL, United Kingdom.
authors.forename: Dawn
authors.initials: D
authors.lastname: Yates
authors.affiliation: CHDI Management/CHDI Foundation Inc. , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
authors.forename: Celia
authors.initials: C
authors.lastname: Dominguez
keywords: CNS exposure; Class IIa HDAC inhibitors; Huntington’s disease; cyclopropanation; hydroxamic acid; tetrasubstituted cyclopropane
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