Discovery of novel benzoxaborole-based potent antitrypanosomal agents

ACS Med Chem Lett. 2010 Apr 6;1(4):165-9. doi: 10.1021/ml100013s. eCollection 2010 Jul 8.


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.

Keywords: African trypanosomiasis; Tryapnosoma brucei; benzoxaborole.