DESIGN, SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF PYRILAMINE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS

For the study on the structure-activity relationship of pyrilamine-based histone deacetylase inhibitor 1, we focused on the structures of its benzyl and dimethylamino groups. Of the synthesized novel pyrilamine derivatives 2-7, compound 2 enhanced potency against hERG inhibition, as well as decreased molecular weight and topological polar surface area.