Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents
Chronic hepatitis C virus (HCV) infection has become a major public health burden worldwide. Twenty-two sophocarpinic acid or matrine derivatives were synthesized and their anti-HCV activities were evaluated in vitro. The structure-activity analysis revealed that (i) sophocarpinic acids with a D-sec...
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doaj-58ee6e711779431a862d1796f01f06aa2020-11-24T23:13:27ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432014-08-014430731210.1016/j.apsb.2014.06.002Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agentsYinghong LiZonggen PengLimei GaoDanqing SongChronic hepatitis C virus (HCV) infection has become a major public health burden worldwide. Twenty-two sophocarpinic acid or matrine derivatives were synthesized and their anti-HCV activities were evaluated in vitro. The structure-activity analysis revealed that (i) sophocarpinic acids with a D-seco 3-ring structure scaffold were more favorable than matrines with a 4-ring scaffold; (ii) the introduction of an electron-withdrawing group on the phenyl ring in 12-N-benzenesulfonyl Δβγ sophocarpinic acids was beneficial for the antiviral activity against HCV. Among them, compounds 9h and 9j exhibited the most potent inhibitory activities on HCV replication with selectivity indies of 70.3 and 30.9, respectively. Therefore, both were selected as antiviral candidates for further investigation.http://www.sciencedirect.com/science/article/pii/S2211383514000549Sophocarpinic acidMatrineAnti-HCVAntiviral activityStructure−activity relationship |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Yinghong Li Zonggen Peng Limei Gao Danqing Song |
spellingShingle |
Yinghong Li Zonggen Peng Limei Gao Danqing Song Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents Acta Pharmaceutica Sinica B Sophocarpinic acid Matrine Anti-HCV Antiviral activity Structure−activity relationship |
author_facet |
Yinghong Li Zonggen Peng Limei Gao Danqing Song |
author_sort |
Yinghong Li |
title |
Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents |
title_short |
Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents |
title_full |
Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents |
title_fullStr |
Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents |
title_full_unstemmed |
Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents |
title_sort |
synthesis and biological evaluation of sophocarpinic acid derivatives as anti-hcv agents |
publisher |
Elsevier |
series |
Acta Pharmaceutica Sinica B |
issn |
2211-3835 2211-3843 |
publishDate |
2014-08-01 |
description |
Chronic hepatitis C virus (HCV) infection has become a major public health burden worldwide. Twenty-two sophocarpinic acid or matrine derivatives were synthesized and their anti-HCV activities were evaluated in vitro. The structure-activity analysis revealed that (i) sophocarpinic acids with a D-seco 3-ring structure scaffold were more favorable than matrines with a 4-ring scaffold; (ii) the introduction of an electron-withdrawing group on the phenyl ring in 12-N-benzenesulfonyl Δβγ sophocarpinic acids was beneficial for the antiviral activity against HCV. Among them, compounds 9h and 9j exhibited the most potent inhibitory activities on HCV replication with selectivity indies of 70.3 and 30.9, respectively. Therefore, both were selected as antiviral candidates for further investigation. |
topic |
Sophocarpinic acid Matrine Anti-HCV Antiviral activity Structure−activity relationship |
url |
http://www.sciencedirect.com/science/article/pii/S2211383514000549 |
work_keys_str_mv |
AT yinghongli synthesisandbiologicalevaluationofsophocarpinicacidderivativesasantihcvagents AT zonggenpeng synthesisandbiologicalevaluationofsophocarpinicacidderivativesasantihcvagents AT limeigao synthesisandbiologicalevaluationofsophocarpinicacidderivativesasantihcvagents AT danqingsong synthesisandbiologicalevaluationofsophocarpinicacidderivativesasantihcvagents |
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1725598276899569664 |