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题名: Synthesis of (5R,8R)-2-(3,8-Dimethyl-2-oxo-1,2,4,5,6,7,8,8 alpha-octahydroazulen-5-yl) Acrylic Acid (Rupestonic Acid) Amide Derivatives and in vitro Inhibitive Activities against Influenza A(3),B and Herpes Simplex Type 1 and 2 Virus
作者: Yong, Jian-ping ; Lv, Qiao-ying ; Aisa, Haji Akber
关键词: Synthesis ; Rupestonic acid amide derivative ; Anti-viral activities
刊名: BULLETIN OF THE KOREAN CHEMICAL SOCIETY
发表日期: 2009
卷: 30, 期:2, 页:435-440
收录类别: SCI
部门归属: [Yong, Jian-ping ; Lv, Qiao-ying ; Aisa, Haji Akber] Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Nat Prod Chem, Urumqi 830011, Peoples R China. [Yong, Jian-ping] Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China.
摘要: 19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a similar to 21, 3a similar to 3g were syntliesized and preliminarily evaluated in vitro against influenza virus A(3),B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus A(3)(TC50 = 120.6 mu mol/L, IC50 = 19.2 mu mol/L, SI = 6.3) and B(TC50 = 120.6 mu mol/L, IC50 = 29.9 mu mol/L, SI = 4.0); 2g was more active against influenza A(3) virus at very low cytotoxicity (TC50 > 2092.1 mu mol/L, IC50 = 143.7 mu mol/L, SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 (TC50 = 200.0 mu mol/L, IC50 = 11.3 mu mol/L, SI = 17.7) and HSV-2 (TC50 = 200.0 mu mol/L, IC50 = 20.7 mu mol/L, SI = 9.7).
英文摘要: 19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a similar to 21, 3a similar to 3g were syntliesized and preliminarily evaluated in vitro against influenza virus A(3),B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus A(3)(TC50 = 120.6 mu mol/L, IC50 = 19.2 mu mol/L, SI = 6.3) and B(TC50 = 120.6 mu mol/L, IC50 = 29.9 mu mol/L, SI = 4.0); 2g was more active against influenza A(3) virus at very low cytotoxicity (TC50 > 2092.1 mu mol/L, IC50 = 143.7 mu mol/L, SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 (TC50 = 200.0 mu mol/L, IC50 = 11.3 mu mol/L, SI = 17.7) and HSV-2 (TC50 = 200.0 mu mol/L, IC50 = 20.7 mu mol/L, SI = 9.7).
语种: 英语
内容类型: 期刊论文
URI标识: http://ir.xjipc.cas.cn/handle/365002/4078
Appears in Collections:中国科学院新疆理化技术研究所(2002年以前数据)_期刊论文

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Yong, Jian-ping;Lv, Qiao-ying;Aisa, Haji Akber.Synthesis of (5R,8R)-2-(3,8-Dimethyl-2-oxo-1,2,4,5,6,7,8,8 alpha-octahydroazulen-5-yl) Acrylic Acid (Rupestonic Acid) Amide Derivatives and in vitro Inhibitive Activities against Influenza A(3),B and Herpes Simplex Type 1 and 2 Virus,BULLETIN OF THE KOREAN CHEMICAL SOCIETY,2009,30(2):435-440
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