A Structure–Activity Relationship Study of the Antimalarial and Antileishmanial Activities of Nonpeptide Macrocyclic Histone Deacetylase Inhibitors

Histone deacetylase inhibitors (HDACi) induce diverse biological responses that include antiparasitic, antiproliferative, anti-inflammatory, and cognition-enhancing activities. In fact, inhibition of HDAC activity is now a clinically proven strategy for cancer treatment.[1] Several mechanisms have been proposed to account for the molecular basis of the biological activities of HDACi. The most widely accepted mechanism is the perturbation of chromatin remodeling as well as the acetylation status of a subset of nonhistone proteins.[2]