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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 ?g/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei.

SUBMITTER: Ding D 

PROVIDER: S-EPMC4007846 | biostudies-other | 2010 Jul

REPOSITORIES: biostudies-other

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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. ...[more]