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

Discovery of novel benzoxaborole-based potent antitrypanosomal agents.

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School of Pharmacy and E-Institute of Chemical Biology, Shanghai Jiao Tong University, Shanghai, 200240, China.
SCYNEXIS, Inc., P.O. Box 12878, Research Triangle Park, North Carolina 27709.
Haskins Laboratory, Pace University, New York, New York 10038.
Anacor Pharmaceuticals Inc., 1020 East Meadow Circle, Palo Alto, California 94303.
Small Molecule Discovery Center and Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, California 94158.


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.


African trypanosomiasis; Tryapnosoma brucei; benzoxaborole

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