2. Academic Validation
  3. Chalcone-benzoxaborole hybrid molecules as potent antitrypanosomal agents

Chalcone-benzoxaborole hybrid molecules as potent antitrypanosomal agents

  • J Med Chem. 2012 Apr 12;55(7):3553-7. doi: 10.1021/jm2012408.
Zhitao Qiao 1,  Qi Wang,  Fenglong Zhang,  Zhongli Wang,  Tana Bowling,  Bakela Nare,  Robert T Jacobs,  Jiong Zhang,  Dazhong Ding,  Yangang Liu,  Huchen Zhou
Affiliations

Affiliation

  • 1 School of Pharmacy, Shanghai Jiao Tong University, 200240, Shanghai, China.
PMID: 22360533 DOI: 10.1021/jm2012408
Abstract

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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