Potent and Orally Efficacious Bisthiazole-Based Histone Deacetylase Inhibitors

ACS Medicinal Chemistry Letters
2014.0

Abstract

Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.

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