Chalcone–Benzoxaborole hybrid molecules as potent antitrypanosomal agents

…, Q Wang, F Zhang, Z Wang, T Bowling…

文献索引：Qiao, Zhitao; Wang, Qi; Zhang, Fenglong; Wang, Zhongli; Bowling, Tana; Nare, Bakela; Jacobs, Robert T.; Zhang, Jiong; Ding, Dazhong; Liu, Yangang; Zhou, Huchen Journal of Medicinal Chemistry, 2012 , vol. 55, # 7 p. 3553 - 3557

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被引用次数: 42

摘要

We report the novel chalcone–benzoxaborole hybrids and their structure–activity relationship against Trypanosoma brucei parasites. The 4-NH2 derivative 29 and 3-OMe derivative 43 were found to have excellent potency. The synergistic 4-NH2-3-OMe compound 49 showed an IC50 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 ...