HCVNS5b RNA-dependent RNA polymerase inhibitors:: From α,γ-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids.: Design and synthesis

被引：94
|
作者：
Summa, V
Petrocchi, A
Matassa, VG
Taliani, M
Laufer, R
De Francesco, R
Altamura, S
Pace, P
机构：
[1] IRBM, Dept Med Chem, MRL Rome, I-00040 Pomezia, RM, Italy
[2] IRBM, Dept Biochem, MRL Rome, I-00040 Pomezia, RM, Italy
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 22期
关键词：
D O I：
10.1021/jm0494669
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new class of the HCV NS5b RNA-dependent RNA polymerase inhibitors, the dihyroxypyrimidinecarboxylic acid derivative, was designed from a diketoacid and meconic acid derivative discovered by screening. Mechanism of action and essential moieties required for activity were identified. The corresponding N-methylpyrimidinone was also prepared; both classes are novel, reversible, and selective inhibitors of the HCV NS5b polymerase with improved druglike characteristics.
引用
收藏
页码：5336 / 5339
页数：4
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