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Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

  作者 DING DAZHONG; ZHAO YAXUE; MENG QINGQING; XIE DONGSHENG; NARE BAKELA; CHEN DAITAO; BACCHI CYRUS J; YARLETT NIGEL; ZHANG YONGKANG; HERNANDEZ VINCENT; XIA YI; FREUND YVONNE; ABDULLA MAHA; ANG KEANHOOI; RATNAM JOSELINE; MCKERROW JAMES H; JACOBS ROBERT T; ZHOU HUCHEN; PLATTNER JACOB J  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2010年1-4;  页码  165-169  
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[摘要]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 mu g/mL and in vivo efficacy in acute murine infection models against nryapnosoma brucei.

 
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