期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 5, 页码 700-706出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.01.031
关键词
HCV; NS5A inhibitor; Tetracycle; Tetrahydro-2H-pyran; THP; Pan-genotype
A series of novel tetracyclic core-containing HCV NS5A inhibitors has been discovered. Incorporation of tetrahydropyran-substituted amino acid moiety improved their potency and yielded HCV NS5A inhibitors with a minimum potency shift from the GT1a strain compared to other genotypes and mutants. Compounds 53 and 54 showed the best potency profile and had reasonable half-times in rat PK studies. However, further optimization of their oral bioavailability is still needed in order to advance them for further development. (C) 2000 Elsevier Science Ltd. All rights reserved.
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