Design, synthesis, and evaluation of novel oxyacanthine derivatives for anti-SARS-CoV-2 activity
文献类型：期刊论文
| 作者 | Lu, Jie1,2,3; Cheng, Yan1,3; Zhang, Yumin4; Wang, Yi3; Xia, Bingqing1,3; Zhang, Leike4; Odilov, Abdullajon1,3; He, Yang1,3; Jiang, Xiangrui1,3 ; Yang, Feipu3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2024-11-15 |
| 卷号 | 113页码:5 |
| 关键词 | Bisbenzylisoquinoline alkaloid Oxyacanthine derivatives SARS-CoV-2 |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2024.129951 |
| 通讯作者 | Yang, Feipu(yangfeipu@simm.ac.cn) |
| 英文摘要 | Here, we report the synthesis of a series of oxyacanthine derivatives and evaluation for their anti-SARS-CoV-2 activity in Vero E6 cells. In order to eliminate the potential metabolic activation caused by para-methylene phenol moiety in oxyacanthine, totally 29 derivatives were designed and synthesized, resulting in 23 compounds with antivirus IC50 below 5.00 mu M and 9 compounds with antivirus IC50 below 1.00 mu M. Among them, amides compound 4a and 4d exhibited potent anti-SARS-CoV-2 activity and the most favorable selectivity index (SI) in vitro with the SI values of 115 and 70, respectively. The pharmacokinetic properties of 4a and 4d were also assessed. Much more improved exposure in mice, longer half-life (T1/2), and increased oral bioavailability were observed for both compounds 4a and 4d compared with oxyacanthine. |
| 资助项目 | National Natural Science Foundation of China[U22A20379] ; National Natural Science Foundation of China[82341058] ; National Natural Science Foundation of China[92169202] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001386525800001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/315309]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Yang, Feipu |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Henan Univ, Sch Pharm, Kaifeng 475004, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, State Key Lab Virol, Wuhan Inst Virol, Ctr Biosafety Mega Sci, Wuhan 430071, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lu, Jie,Cheng, Yan,Zhang, Yumin,et al. Design, synthesis, and evaluation of novel oxyacanthine derivatives for anti-SARS-CoV-2 activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2024,113:5. |
| APA | Lu, Jie.,Cheng, Yan.,Zhang, Yumin.,Wang, Yi.,Xia, Bingqing.,...&Shen, Jingshan.(2024).Design, synthesis, and evaluation of novel oxyacanthine derivatives for anti-SARS-CoV-2 activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,113,5. |
| MLA | Lu, Jie,et al."Design, synthesis, and evaluation of novel oxyacanthine derivatives for anti-SARS-CoV-2 activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 113(2024):5. |
入库方式： OAI收割
来源：上海药物研究所
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