Chalcone鈥揃enzoxaborole Hybrid Molecules as Potent Antitrypanosomal Agents

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• 作者：Zhitao Qiao ; Qi Wang ; Fenglong Zhang ; Zhongli Wang ; Tana Bowling ; Bakela Nare ; Robert T. Jacobs ; Jiong Zhang ; Dazhong Ding ; Yangang Liu ; Huchen Zhou
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：April 12, 2012
• 年：2012
• 卷：55
• 期：7
• 页码：3553-3557
• 全文大小：259K
• 年卷期：v.55,no.7(April 12, 2012)
• ISSN：1520-4804

文摘

We report the novel chalcone鈥揵enzoxaborole hybrids and their structure鈥揳ctivity relationship againstTrypanosoma 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 渭g/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.