The discovery and characterization of a novel scaffold as a potent hepatitis C virus inhibitor

Na Liu; Shiping Zhu; Xianghua Zhang; Xunkui Yin; Guoqiang Dong; Jianzhong Yao; Zhenyuan Miao; Wannian Zhang; Xiaonan Zhang; Chunquan Sheng

doi:10.1039/c5cc10594c

The discovery and characterization of a novel scaffold as a potent hepatitis C virus inhibitor

Na Liu
, Shiping Zhu
, Xianghua Zhang
, Xunkui Yin
, Guoqiang Dong
, Jianzhong Yao
, Zhenyuan Miao
, Wannian Zhang
, Xiaonan Zhang
, Chunquan Sheng

Research output: Contribution to journal › Review article › peer-review

11 Citations (Scopus)

Abstract

HCV infections are a major global health concern. Although direct acting antiviral agents have significantly improved the response rate of anti-HCV therapy, they also suffer from drug resistance, unfavorable pharmacokinetic profiles and high costs. Thus, it is still highly desirable to develop new anti-HCV therapeutics. Herein a novel anti-HCV benzothiazole scaffold was discovered by phenotypic screening. Further target characterization and structural optimization studies revealed that the benzothiazole-disulfoamide derivatives were potent anti-HCV molecules with good selectivity and acted by targeting NS5A.

Original language	English
Pages (from-to)	3340-3343
Number of pages	4
Journal	Chemical Communications
Volume	52
Issue number	16
DOIs	https://doi.org/10.1039/c5cc10594c
Publication status	Published - 25 Feb 2016
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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10.1039/c5cc10594c

Cite this

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title = "The discovery and characterization of a novel scaffold as a potent hepatitis C virus inhibitor",

abstract = "HCV infections are a major global health concern. Although direct acting antiviral agents have significantly improved the response rate of anti-HCV therapy, they also suffer from drug resistance, unfavorable pharmacokinetic profiles and high costs. Thus, it is still highly desirable to develop new anti-HCV therapeutics. Herein a novel anti-HCV benzothiazole scaffold was discovered by phenotypic screening. Further target characterization and structural optimization studies revealed that the benzothiazole-disulfoamide derivatives were potent anti-HCV molecules with good selectivity and acted by targeting NS5A. ",

keywords = "Antiviral Agents/pharmacology, Drug Discovery, Hepacivirus/drug effects",

author = "Na Liu and Shiping Zhu and Xianghua Zhang and Xunkui Yin and Guoqiang Dong and Jianzhong Yao and Zhenyuan Miao and Wannian Zhang and Xiaonan Zhang and Chunquan Sheng",

note = "Funding Information: Financial support for this research was provided by the 863 Hi-Tech Program of China (Grant 2014AA020525 to C. S.), the National Natural Science Foundation of China (Grant 8122044 to C. S. and 81201278 to X. Z.), the Youth Foundation of Second Military Medical University (grant 2014QN06 to N. L.) and the Shanghai ??ShuGuang?? Project (grant 14SG33 to C. S.). Publisher Copyright: {\textcopyright} The Royal Society of Chemistry 2016. Copyright: Copyright 2020 Elsevier B.V., All rights reserved.",

year = "2016",

month = feb,

day = "25",

doi = "10.1039/c5cc10594c",

language = "English",

volume = "52",

pages = "3340--3343",

journal = "Chemical Communications",

issn = "1359-7345",

publisher = "Royal Society of Chemistry",

number = "16",

}

TY - JOUR

T1 - The discovery and characterization of a novel scaffold as a potent hepatitis C virus inhibitor

AU - Liu, Na

AU - Zhu, Shiping

AU - Zhang, Xianghua

AU - Yin, Xunkui

AU - Dong, Guoqiang

AU - Yao, Jianzhong

AU - Miao, Zhenyuan

AU - Zhang, Wannian

AU - Zhang, Xiaonan

AU - Sheng, Chunquan

N1 - Funding Information: Financial support for this research was provided by the 863 Hi-Tech Program of China (Grant 2014AA020525 to C. S.), the National Natural Science Foundation of China (Grant 8122044 to C. S. and 81201278 to X. Z.), the Youth Foundation of Second Military Medical University (grant 2014QN06 to N. L.) and the Shanghai ??ShuGuang?? Project (grant 14SG33 to C. S.). Publisher Copyright: © The Royal Society of Chemistry 2016. Copyright: Copyright 2020 Elsevier B.V., All rights reserved.

PY - 2016/2/25

Y1 - 2016/2/25

N2 - HCV infections are a major global health concern. Although direct acting antiviral agents have significantly improved the response rate of anti-HCV therapy, they also suffer from drug resistance, unfavorable pharmacokinetic profiles and high costs. Thus, it is still highly desirable to develop new anti-HCV therapeutics. Herein a novel anti-HCV benzothiazole scaffold was discovered by phenotypic screening. Further target characterization and structural optimization studies revealed that the benzothiazole-disulfoamide derivatives were potent anti-HCV molecules with good selectivity and acted by targeting NS5A.

AB - HCV infections are a major global health concern. Although direct acting antiviral agents have significantly improved the response rate of anti-HCV therapy, they also suffer from drug resistance, unfavorable pharmacokinetic profiles and high costs. Thus, it is still highly desirable to develop new anti-HCV therapeutics. Herein a novel anti-HCV benzothiazole scaffold was discovered by phenotypic screening. Further target characterization and structural optimization studies revealed that the benzothiazole-disulfoamide derivatives were potent anti-HCV molecules with good selectivity and acted by targeting NS5A.

KW - Antiviral Agents/pharmacology

KW - Drug Discovery

KW - Hepacivirus/drug effects

UR - https://www.scopus.com/pages/publications/84958794102

U2 - 10.1039/c5cc10594c

DO - 10.1039/c5cc10594c

M3 - Review article

C2 - 26822629

SN - 1359-7345

VL - 52

SP - 3340

EP - 3343

JO - Chemical Communications

JF - Chemical Communications

IS - 16

ER -

The discovery and characterization of a novel scaffold as a potent hepatitis C virus inhibitor

Abstract

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