1. Novel pyrrolobenzoxaboroles: Design, synthesis, and biological evaluation against Trypanosoma brucei.
- Author
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Wu, Puhua, Zhang, Jiong, Meng, Qingqing, Nare, Bakela, Jacobs, Robert T., and Zhou, Huchen
- Subjects
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TRYPANOSOMIASIS , *CHEMICAL synthesis , *TRYPANOSOMA brucei , *PARASITIC diseases , *STRUCTURE-activity relationships , *CELL-mediated cytotoxicity - Abstract
Abstract: Human African trypanosomiasis is a fatal parasitic infection caused by the protozoan Trypanosoma brucei. The development of novel antitrypanosomal agents is urgently needed. Here we report the synthesis and structure–activity relationship of a new class of benzoxaboroles as antitrypanosomal agents. These compounds showed antiparasitic IC50 values ranging from 4.02 to 0.03 μg/mL and satisfactory cytotoxicity profile. Three of the lead compounds were demonstrated to cure the parasitic infection in a murine acute infection model. The structure–activity relationship of the pyrrolobenzoxaboroles are also discussed. [Copyright &y& Elsevier]
- Published
- 2014
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