Synthesis of a FTO Inhibitor with Anticonvulsant Activity
Department
Chemistry and Biochemistry
Document Type
Article
Publication Date
5-18-2014
Abstract
We describe the rationale for and the synthesis of a new class of compounds utilizing a modular approach that are designed to mimic ascorbic acid and to inhibit 2-oxoglutarate-dependent hydroxylases. Preliminary characterization of one of these compounds indicates in vivo anticonvulsant activity (6 Hz mouse model) at nontoxic doses, inhibition of the 2-oxoglutarate-dependent hydroxylase FTO, and expected increase in cellular N6-methyladenosine. This compound is also able to modulate various microRNA, an interesting result in light of the recent view that modulation of microRNAs may be useful for the treatment of CNS disease.
Journal Title
ACS Chemical Neuroscience
Journal ISSN
1948-7193
Volume
8
Issue
5
First Page
658
Last Page
665
Digital Object Identifier (DOI)
10.1021%2Fcn500042t
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