Journal of Medicinal Chemistry
Brief Article
compound 51 (20.4%) as a white powder. 1H NMR (400 MHz,
DMSO-d6): δ 9.12 (s, 1H), 7.74 (s, 1H), 7.54 (dd, J = 8.0 and 1.6 Hz,
1H), 7.42−7.29 (m, 5H), 7.26−7.22 (m, 1H), 6.68 (d, J = 15.6 Hz,
1H), 6.37 (dd, J = 16.0 and 6.4 Hz, 1H), 5.61 (d, J = 4.4 Hz, 1H),
5.27−5.25 (m, 1H), 4.96 (s, 2H). 13C NMR (100 MHz, DMSO): δ 153.0,
144.4, 135.3, 133.3, 128.7, 128.1, 128.0, 126.8, 126.0, 121.5, 73.0, 69.7.
HRMS-ESI: [M + Na]+ C16H15BO3Na calcd, 289.1012; found, 289.1010;
mp 178−180 °C; HPLC purity 95.2% (retention time 7.853 min).
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ASSOCIATED CONTENT
■
S
* Supporting Information
Compound characterization data and procedures for biological
assay. This material is available free of charge via the Internet at
AUTHOR INFORMATION
■
Corresponding Author
*Phone: +86(21)34206721. Fax: +86(21)34204457. E-mail:
Author Contributions
§These authors contributed equally to this work.
Notes
The authors declare no competing financial interest.
ACKNOWLEDGMENTS
■
We thank National Science Foundation of China (20702031),
Ministry of Science and Technology of China (2009CB918404),
E-Institutes of Shanghai Universities (EISU) Chemical Biology
Division, and National Comprehensive Technology Platforms for
Innovative Drug R&D (2009ZX09301-007) for financial support
of this work. We thank Prof. Jim McKerrow (UCSF) and
Dr. Geraldine De Muylder (UCSF) for their helpful discussion
and for their generous providing the TBB221 strain.
ABBREVIATIONS USED
■
HAT, human African trypanosomiasis; T. brucei, Trypanosoma
brucei; T. cruzi, Trypanosoma cruzi; NECT, nifurtimox−
eflornithine combination; bid, twice a day; ip, intraperitoneal
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