4.5 Article

Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

期刊

ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 4, 页码 165-169

出版社

AMER CHEMICAL SOC
DOI: 10.1021/ml100013s

关键词

Tryapnosoma brucei; African trypanosomiasis; benzoxaborole

资金

  1. Sandler Foundation
  2. Drugs for Neglected Diseases initiative
  3. National Science Foundation of China [20702031]
  4. Ministry of Science and Technology of China [2009CB918404]

向作者/读者索取更多资源

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 IC(50) 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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