Divergent synthesis of a thiolate-based alpha-hydroxytropolone library with a dynamic bioactivity profile

摘要

Here we describe a rapid and divergent synthetic route toward structurally novel alpha HTs functionalized with either one or two thioether or sulfonyl appendages. Evaluation of this library against hepatitis B and herpes simplex virus, as well as the pathogenic fungus Cryptococcus neoformans, revealed complementary biological profiles and new lead compounds with sub-micromolar activities against each pathogen and high selectivities when compared to mammalian cell lines.