期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 12, 页码 3845-3854出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.04.041
关键词
Envelope-protein; Flaviviruses; Phenylthiazoles; Dengue virus; Yellow fever virus
资金
- NIH/NIAID Regional Center of Excellence for Biodefense and Emerging Infectious Diseases Research (RCE)
- Region V Great Lakes RCE (NIH) [1-U54-AI-057153]
- NIAID [P01AI055672]
- Egyptian government
Flaviviruses are one of the most clinically important pathogens and their infection rates are increasing steadily. The phenylthiazole ring system has provided a template for the design and synthesis of antiviral agents that inhibit the flaviviruses by targeting their E-protein. Unfortunately, there is a correlation between phenylthiazole antiflaviviral activity and the presence of the reactive and therefore potentially toxic mono-or dibromomethyl moieties at thiazole-C4. Adding a linear hydrophobic tail para to the phenyl ring led to a new class of phenylthiazole antiflaviviral compounds that lack the toxic dibromomethyl moiety. This led to development of a drug-like phenylthiazole 12 that had high antiflaviviral selectivity (TI = 147). (C) 2011 Elsevier Ltd. All rights reserved.
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