☆ 4.7 Article

Chalcone-Benzoxaborole Hybrid Molecules as Potent Antitrypanosomal Agents

JOURNAL OF MEDICINAL CHEMISTRY (2012)

期刊

JOURNAL OF MEDICINAL CHEMISTRY

卷 55, 期 7, 页码 3553-3557

出版社

AMER CHEMICAL SOC

DOI: 10.1021/jm2012408

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Chemistry, Medicinal

资金

National Science Foundation of China [20702031]
Ministry of Science and Technology of China [2009CB918404]
E-Institutes of Shanghai Universities (EISU) Chemical Biology Division
National Comprehensive Technology Platforms for Innovative Drug RD [2009ZX09301-007]

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摘要

We report the novel chalcone-benzoxaborole hybrids and their structure-activity relationship against Trypanosoma brucei parasites. The 4-NH2 derivative 29 and 3-OMe derivative 43 were found to have excellent potency. The synergistic 4-NH2-3-OMe compound 49 showed an IC50 of 0.010 mu g/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.

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