Discovery of novel benzoxaborole-based potent antitrypanosomal agents

Abstract

We report the discovery of benzoxaborole antitrypanosomal agents and their structure?activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC50 values as low as 0.02 μg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei. © 2010 American Chemical Society.