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Updated: Apr 29, 2026
In Vitro Drug Screening Against All Life Cycle Stages of Trypanosoma cruzi Using Parasites Expressing β-galactosidase
Published on: November 5, 2021
Novel pyrrolobenzoxaboroles: design, synthesis, and biological evaluation against Trypanosoma brucei
Puhua Wu1, Jiong Zhang1, Qingqing Meng1
1State Key Laboratory of Microbial Metabolism, and School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, People's Republic of China.
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.
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