Histone deacetylase inhibitors for enhancing activity of antifungal agent: a patent evaluation of WO2014041424(A1)

Abstract

Novel histone deacetylase inhibitors have been developed for the antifungal therapy. Molecule 8 exhibited potent antifungal activities with MIC values of 0.25/0.25, 0.12/0.25, 0.12/0.12 µg/ml against Candida albicans, C. parapsilosis and C. glabrata after 24/48 h incubation, respectively. Most of the synthesized compound showed significantly synergistic effects with fluconazole in the biological assay. The discovery of these molecules makes positive contributions to the development of potent and safe antifungal drugs.

Keywords:

• antifungal
• histone deacetylase
• inhibitor
• selectivity

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.