Discovery of novel 3-hydroxypicolinamides as selective inhibitors of HIV-1 integrase-LEDGF/p75 interaction

A novel class of HIV-1 integrase (IN) allosteric inhibitors targeting both IN-LEDGF/p75 interaction and IN dimerization were discovered bearing 3-hydroxypicolinamide scaffold, with low micromolar IC50 values and therapeutically selective antiviral effect.