Discovery of novel benzoxaborole-based potent antitrypanosomal agents.
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ABSTRACT:
SUBMITTER: Ding D
PROVIDER: S-EPMC4007846 | biostudies-other | 2010 Jul
REPOSITORIES: biostudies-other
Publications
Discovery of novel benzoxaborole-based potent antitrypanosomal agents.
Ding Dazhong D Zhao Yaxue Y Meng Qingqing Q Xie Dongsheng D Nare Bakela B Chen Daitao D Bacchi Cyrus J CJ Yarlett Nigel N Zhang Yong-Kang YK Hernandez Vincent V Xia Yi Y Freund Yvonne Y Abdulla Maha M Ang Kean-Hooi KH Ratnam Joseline J McKerrow James H JH Jacobs Robert T RT Zhou Huchen H Plattner Jacob J JJ
ACS medicinal chemistry letters 20100406 4
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]
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