School of Pharmacy, Shanghai Jiao Tong University, 200240, Shanghai, China.
J Med Chem. 2012 Apr 12;55(7):3553-7. doi: 10.1021/jm2012408. Epub 2012 Mar 14.
We report the novel chalcone-benzoxaborole hybrids and their structure-activity relationship against Trypanosoma brucei parasites. The 4-NH(2) derivative 29 and 3-OMe derivative 43 were found to have excellent potency. The synergistic 4-NH(2)-3-OMe compound 49 showed an IC(50) of 0.010 μg/mL and resulted in 100% survival and zero parasitemia in a murine infection model, which represents one of the most potent compounds discovered to date from the benzoxaborole class that inhibit T. brucei growth.
我们报告了新型查尔酮-苯并硼氧杂环戊烷杂合体及其对布氏锥虫寄生虫的结构活性关系。发现 4-NH(2)衍生物 29 和 3-OMe 衍生物 43 具有优异的活性。协同的 4-NH(2)-3-OMe 化合物 49 的 IC(50)为 0.010 μg/mL，导致在小鼠感染模型中 100%的存活率和零寄生虫血症，这代表了迄今为止从苯并硼氧杂环戊烷类中发现的最有效的抑制布氏锥虫生长的化合物之一。
