Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives

被引：1

作者：

Bao, Beihua ^{[1
]}

Meng, Zheng ^{[1
]}

Li, Nianguang ^{[1
]}

Meng, Zhengjie ^{[2
]}

Zhang, Li ^{[1
]}

Cao, Yudan ^{[1
]}

Yao, Weifeng ^{[1
]}

Shan, Mingqiu ^{[1
]}

Ding, Anwei ^{[1
]}

机构：

[1] Nanjing Univ Chinese Med, Coll Pharm, Jiangsu Key Lab High Technol TCM Formulae Res, Nanjing 210023, Jiangsu, Peoples R China

[2] Nanjing Univ Technol, Coll Biotechnol & Pharmaceut Engn, Nanjing 211816, Jiangsu, Peoples R China

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2013年 / 14卷 / 08期

关键词：

schizonepetin; anti-virus activity; HSV-1; H3N2; HERPES-SIMPLEX-VIRUS; PATIENT; RATS;

D O I：

10.3390/ijms140817193

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE) inhibition assay in vitro. Compounds M2, M4, M5 and M34 showed higher inhibitory activity against HSV-1 virus with the TC50 values being in micromole. Compounds M28, M33, and M35 showed higher inhibitory activity against influenza virus H3N2 with their TC50 values being 96.4, 71.0 and 75.4 M, respectively. Preliminary biological activity evaluation indicated that the anti-H3N2 and anti-HSV-1 activities improved obviously through the introduction of halogen into the structure of schizonepetin.

引用

页码：17193 / 17203

页数：11

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