Title

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

ACS Chemical Neuroscience

Journal ISSN

1948-7193

Volume

8

Issue

5

First Page

658

Last Page

665

Digital Object Identifier (DOI)

10.1021%2Fcn500042t