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Chalcone-benzoxaborole hybrid molecules as potent antitrypanosomal agents. 2012
Zhitao Qiao, and
Qi Wang, and
Fenglong Zhang, and
Zhongli Wang, and
Tana Bowling, and
Bakela Nare, and
Robert T Jacobs, and
Jiong Zhang, and
Dazhong Ding, and
Yangang Liu, and
Huchen Zhou
School of Pharmacy, Shanghai Jiao Tong University, 200240, Shanghai, China.
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.
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