期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 2, 页码 457-460出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.114
关键词
HCV polymerase inhibitors; 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran; 3,4-dihydro-1H-pyrano[3,4-b]benzofuran
A novel class of HCV NS513 RNA dependent RNA polymerase inhibitors containing 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran scaffolds were designed and synthesized. Optimization of the alkyl substituent in the pyran ring showed preference for an n-propyl group, while 5,8-disubstitution pattern is preferred for the aromatic region. Analog 19 displayed potent activity with an IC50 of 50 nM against HCV NS513 enzyme and was selective over a panel of polymerases. (c) 2005 Elsevier Ltd. All rights reserved.
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