The Second-generation of Highly Potent Hepatitis C Virus (HCV) NS3/4A Protease Inhibitors: Evolutionary Design Based on Tailor-made Amino Acids, Synthesis and Major Features of Bio-activity
Wang, Shuni1,2,3; Wang, Yibing1,2,3; Wang, Jiang1,2,3; Sato, Tatsunori4; Izawa, Kunisuke4; Soloshonok, Vadim A.5,6; Liu, Hong1,2,3
刊名CURRENT PHARMACEUTICAL DESIGN
2017
卷号23期号:30页码:4493-4554
关键词Hepatitis C virus (HCV) pandemic direct-acting antiviral agents (DAAs) NS3/4A protease inhibitor tailor-made amino acids structure-activity relationship (SAR) asymmetric synthesis ring-closing metathesis (RCM)
ISSN号1381-6128
DOI10.2174/1381612823666170522122424
文献子类Review
英文摘要Hepatitis C is a current pandemic liver disease caused by the hepatitis C virus (HCV) with high morbidity and mortality. Recently, the direct-acting antiviral agents (DAAs) targeting HCV NS3/4A, NS5A and NS5B have become the most effective therapies against HCV infection in the clinical treatment. Among them, the second-generation of NS3/4A inhibitors have emerged as the mainstay of the DAA therapies, which are derived from the peptide substrate of NS3/4A protease and modified with various tailor-made amino acids in order to achieve high sustained virologic response (SVR) against HCV. This review summarizes sixteen examples of the second-generation of HCV NS3/4A inhibitors, mainly focusing on the clinical application, structure development, structure-activity relationship (SAR) and their synthesis.
资助项目National Natural Science Foundation of China[81620108027] ; National Natural Science Foundation of China[21632008] ; Major Project of Chinese National Programs for Fundamental Research and Development[2015CB910304] ; IKERBASQUE, the Basque Foundation for Science[00000000]
WOS关键词GENOTYPE 1 INFECTION ; MICHAEL ADDITION-REACTIONS ; TREATMENT-NAIVE PATIENTS ; RING-CLOSING METATHESIS ; NUCLEOPHILIC GLYCINE EQUIVALENTS ; PEPTIDE-BASED INHIBITORS ; DYNAMIC KINETIC RESOLUTION ; CHIRAL NI(II) COMPLEX ; LARGE-SCALE SYNTHESIS ; INTERFERON-ALPHA 2A
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者BENTHAM SCIENCE PUBL LTD
WOS记录号WOS:000416929300008
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/275691]  
专题药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Izawa, Kunisuke; Soloshonok, Vadim A.; Liu, Hong
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China;
3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China;
4.Hamari Chem Ltd, Higashi Yodogawa Ku, 1-4-29 Kunijima, Osaka 5330024, Japan;
5.Univ Basque Country UPV EHU, Dept Organ Chem 1, Fac Chem, Paseo Manuel Lardizabal 3, San Sebastian 20018, Spain;
6.Basque Fdn Sci, IKERBASQUE, Alameda Urquijo 36-5,Plaza Bizkaia, Bilbao 48011, Spain
推荐引用方式
GB/T 7714
Wang, Shuni,Wang, Yibing,Wang, Jiang,et al. The Second-generation of Highly Potent Hepatitis C Virus (HCV) NS3/4A Protease Inhibitors: Evolutionary Design Based on Tailor-made Amino Acids, Synthesis and Major Features of Bio-activity[J]. CURRENT PHARMACEUTICAL DESIGN,2017,23(30):4493-4554.
APA Wang, Shuni.,Wang, Yibing.,Wang, Jiang.,Sato, Tatsunori.,Izawa, Kunisuke.,...&Liu, Hong.(2017).The Second-generation of Highly Potent Hepatitis C Virus (HCV) NS3/4A Protease Inhibitors: Evolutionary Design Based on Tailor-made Amino Acids, Synthesis and Major Features of Bio-activity.CURRENT PHARMACEUTICAL DESIGN,23(30),4493-4554.
MLA Wang, Shuni,et al."The Second-generation of Highly Potent Hepatitis C Virus (HCV) NS3/4A Protease Inhibitors: Evolutionary Design Based on Tailor-made Amino Acids, Synthesis and Major Features of Bio-activity".CURRENT PHARMACEUTICAL DESIGN 23.30(2017):4493-4554.
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