1344109-55-2Relevant articles and documents
Novel pyrrolobenzoxaboroles: Design, synthesis, and biological evaluation against Trypanosoma brucei
Wu, Puhua,Zhang, Jiong,Meng, Qingqing,Nare, Bakela,Jacobs, Robert T.,Zhou, Huchen
, p. 59 - 75 (2014/06/09)
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.
Synthesis of a novel pyrrolo-benzoxaborole scaffold and its derivatization via Friedel-Crafts reaction catalyzed by anhydrous stannic chloride
Wu, Pu Hua,Meng, Qing Qing,Zhou, Hu Chen
, p. 1411 - 1414 (2012/06/16)
A novel pyrrolo-benzoxaborole, 6-(pyrrol-1-yl)-1,3-dihydro-1-hydroxy-2,1- benzoxaborole, was synthesized with 27% overall yield over six steps from 2-bromo-1-methyl-4-nitrobenzene as starting material. Its derivatization was achieved via Friedel-Crafts re