期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 81, 期 -, 页码 59-75出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.04.079
关键词
Human African trypanosomiasis; Antitrypanosomal agent; Indolobenzoxaboroles; Pyrrolobenzoxaboroles; Structure-activity relationship
资金
- National Natural Science Foundation of China [81222042, 81102313]
- Ministry of Science and Technology of China [2009CB918404, 2012CB518001]
- E-Institutes of Shanghai Universities (EISU) Chemical Biology Division
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 mu g/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. (C) 2014 Elsevier Masson SAS. All rights reserved.
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