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Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

2010; American Chemical Society; Volume: 1; Issue: 4 Linguagem: Inglês

10.1021/ml100013s

1948-5875

Dazhong Ding, Yaxue Zhao, Qingqing Meng, Dongsheng Xie, Bakela Nare, Daitao Chen, Cyrus J. Bacchi, Nigel Yarlett, Yong-Kang Zhang, Vincent Hernandez, Yi Xia, Yvonne R. Freund, Maha Abdulla, Kean-Hooi Ang, Joseline Ratnam, James H. McKerrow, Robert T. Jacobs, Huchen Zhou, Jacob J. Plattner,

Parasites and Host Interactions

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.