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
  • 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.