Structure-Activity Relationship of New Anti-Hepatitis C Virus Agents: Heterobicycle-Coumarin Conjugates

被引：221

作者：

Neyts, Johan ^{[1
]}

De Clercq, Erik ^{[1
]}

Singha, Raghunath ^{[2
]}

Chang, Yung Hsiung ^{[2
]}

Das, Asish R. ^{[2
]}

Chakraborty, Subhasish K. ^{[2
]}

Hong, Shih Ching ^{[2
]}

Tsay, Shwu-Chen ^{[2
]}

Hsu, Ming-Hua ^{[2
]}

Hwu, Jih Ru ^{[2
,3
]}

机构：

[1] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

[2] Natl Tsing Hua Univ, Dept Chem, Hsinchu 30013, Taiwan

[3] Natl Cent Univ, Dept Chem, Jhongli 32001, Taiwan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 05期

关键词：

NS5B POLYMERASE; BENZIMIDAZOLE DERIVATIVES; BIOLOGICAL-ACTIVITY; ANTITUMOR-ACTIVITY; INHIBITORS; ANTICANCER; RIBAVIRIN; POTENT;

D O I：

10.1021/jm801240d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

For establishment of the structure-activity relationship, 19 heterobicycle-coumarin conjugated compounds with the -SCH2- linker were synthesized and found to possess significant antiviral activities. Prominent examples included imidazopyridine-coumarin 12c, purine-coumarin 12d, and benzoxazole-coumarin 14c, which inhibited HCV replication at an EC50 of 6.8, 2.0, and 12 mu M, respectively. The heteroatoms in bicycles

引用

页码：1486 / 1490

页数：5

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