Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents | |
Li, G (Li, Gen)[ 1 ]; Obul, M (Obul, Mamateli)[ 1,2 ]; Zhao, JY (Zhao, Jiang-yu)[ 1 ]; Liu, GY (Liu, Ge-yu)[ 1 ]; Lu, W (Lu, Wei)[ 3 ]; Aisa, HA (Aisa, Haji Akber)[ 1 ] | |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
2019 | |
卷号 | 29期号:19页码:1-3 |
关键词 | Amide Rupestonic acid Anti-influenza virus X-ray crystallographic analysis |
ISSN号 | 0960-894X |
DOI | 10.1016/j.bmcl.2019.08.009 |
英文摘要 | In spired by the important role of amide groups of anti-influenza drugs oseltamivir, zanamivir and peramivir in bioactivity, a series of novel amides modified rupestonic acid derivatives were designed and synthesized. The absolute configuration of critical intermediate bearing chloride with newly formed stereocenter was confirmed by X-ray crystallographic analysis. And all new compounds were evaluated for their in vitro inhibitory activities against influenza A (H1N1 and H3N2) and influenza B viruses. The bioassay results showed that 5h with 4-fluorbenzylsulfonyl modified to 2 position of methyl rupestonate displayed the highest activity against influenza A (H1N1 and H3N2) viruses, even stronger than reference drugs oseltamivir and ribavirin (RVB), and might be recommended as a lead compound to further develop the new anti-influenza reagent. |
WOS记录号 | WOS:000485100200007 |
内容类型 | 期刊论文 |
源URL | [http://ir.xjipc.cas.cn/handle/365002/7157] |
专题 | 新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室 新疆理化技术研究所_资源化学研究室 |
通讯作者 | Aisa, HA (Aisa, Haji Akber)[ 1 ] |
作者单位 | 1.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China 2.Univ Chinese Acad Sci, Yuquan Rd 19 A, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Bath Xinjiang Indigenous Med Plants, Key Lab Plant Resources & Chem Arid Zone, Urumqi 830011, Peoples R China |
推荐引用方式 GB/T 7714 | Li, G ,Obul, M ,Zhao, JY ,et al. Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(19):1-3. |
APA | Li, G ,Obul, M ,Zhao, JY ,Liu, GY ,Lu, W ,&Aisa, HA .(2019).Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(19),1-3. |
MLA | Li, G ,et al."Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.19(2019):1-3. |
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