Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

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...

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Bibliographic Details
Published in:ACS medicinal chemistry letters 2010-07, Vol.1 (4), p.165-169
Main Authors: Ding, Dazhong, Zhao, Yaxue, Meng, Qingqing, Xie, Dongsheng, Nare, Bakela, Chen, Daitao, Bacchi, Cyrus J, Yarlett, Nigel, Zhang, Yong-Kang, Hernandez, Vincent, Xia, Yi, Freund, Yvonne, Abdulla, Maha, Ang, Kean-Hooi, Ratnam, Joseline, McKerrow, James H, Jacobs, Robert T, Zhou, Huchen, Plattner, Jacob J
Format: Article
Language:English
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Letter
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Summary: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml100013s