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Identification of novel thiadiazoloacrylamide analogues as inhibitors of dengue-2 virus NS2B/NS3 protease

文献类型：期刊论文

作者Liu, Hailong1,3; Wu, Ruoming2; Sun, Yanyan2; Ye, Yan1; Chen, Jing1; Luo, Xiaomin1; Shen, Xu1; Liu, Hong1
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2014-11-15
卷号22期号:22页码:6344-6352
关键词Thiadiazo Dengue virus NS2B/NS3
ISSN号0968-0896
DOI10.1016/j.bmc.2014.09.057
文献子类Article
英文摘要Dengue virus is endemic throughout tropical and subtropical regions, and cause severe epidemic diseases. The NS2B/NS3 protease is a promising drug target for dengue virus. Herein, we report the discovery and modification of a novel class of thiadiazoloacrylamide derivatives with potent inhibitory activity against the NS2B/NS3 protease. Thiadiazolopyrimidinone 1 was firstly determined as a new chemical structure against NS2B/NS3 from a commercial compound library. Then, we sought to identify similar compounds with the thiadiazoloacrylamide core that would exhibit better activity. A series of analogues were synthesized and fourteen of them were identified with strong inhibitory activities, in which the nitrile group in the linker part was discovered as an essential group for the inhibitory activity. The best of these (8b) demonstrated an IC50 at 2.24 mu M based on in vitro DENV2 NS2B-NS3pro assays. (C) 2014 Published by Elsevier Ltd.
WOS关键词TETRAPEPTIDE ALDEHYDE INHIBITORS ; PEPTIDE INHIBITORS ; NS2B-NS3 PROTEASE ; NS3 PROTEASE ; SERINE-PROTEASE ; DERIVATIVES ; DESIGN ; SAR
资助项目National Natural Science Foundation of China[81220108025] ; National Natural Science Foundation of China[21021063] ; National Natural Science Foundation of China[91229204] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103101-072] ; National S&T Major Projects[2012ZX09301001-005] ; National S&T Major Projects[2013ZX09507-001] ; Program of Shanghai Subject Chief Scientist[12XD1407100] ; Silver Project[260644]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000344472600004
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/276834]  
专题药物安全性评价中心
药物化学研究室
通讯作者Chen, Jing
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China;
2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China
3.China Pharmaceut Univ, Sch Pharm, Nanjing 200237, Jiangsu, Peoples R China;
推荐引用方式
GB/T 7714		 Liu, Hailong,Wu, Ruoming,Sun, Yanyan,et al. Identification of novel thiadiazoloacrylamide analogues as inhibitors of dengue-2 virus NS2B/NS3 protease[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2014,22(22):6344-6352.
APA Liu, Hailong.,Wu, Ruoming.,Sun, Yanyan.,Ye, Yan.,Chen, Jing.,...&Liu, Hong.(2014).Identification of novel thiadiazoloacrylamide analogues as inhibitors of dengue-2 virus NS2B/NS3 protease.BIOORGANIC & MEDICINAL CHEMISTRY,22(22),6344-6352.
MLA Liu, Hailong,et al."Identification of novel thiadiazoloacrylamide analogues as inhibitors of dengue-2 virus NS2B/NS3 protease".BIOORGANIC & MEDICINAL CHEMISTRY 22.22(2014):6344-6352.

入库方式： OAI收割

来源：上海药物研究所

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