Asymmetric Total Synthesis and NaV1.8 Inhibitory Evaluation of Villosin B, 17-Hydroxymandarone B, and Their Derivatives
文献类型：期刊论文
| 作者 | Zeng, Qi-Xiang1,2; Wang, Lin-Lin3; Zheng, Yue-Ming3; Yu, Yue1,2; Gao, Zhao-Bing1,3; Yue, Jian-Min1,2; Zhao, Jin-Xin1,2 |
| 刊名 | ORGANIC LETTERS
 |
| 出版日期 | 2025-08-22 |
| 卷号 | 27期号:33页码:9201-9206 |
| ISSN号 | 1523-7060 |
| DOI | 10.1021/acs.orglett.5c02746 |
| 英文摘要 | Herein, we present two 17(15 -> 16)-abeo-abietane diterpenoids (1 and 2) as the first terpenoid-class NaV1.8 inhibitors, along with their first asymmetric total syntheses to enable in-depth pharmacological studies. Key steps include kinetic resolution of terminal epoxides, bioinspired polyene cyclization, and late-stage photocatalytic benzylic oxidation. Preliminary structural modifications led to 13 derivatives, among which compound 29 exhibited both a 4.3-fold improved potency compared to parent natural product 1 and preserved selectivity across other sodium-gated sodium channels. |
| WOS关键词 | PAIN ; DITERPENES ; MANAGEMENT |
| 资助项目 | National Natural Science Foundation of China[2022YFE0203600] ; National Key R&D Program Strategic Scientific and Technological Innovation Cooperation Key Project[22494691] ; National Key R&D Program Strategic Scientific and Technological Innovation Cooperation Key Project[22237007] ; National Natural Science Foundation of China[2022282] ; Youth Innovation Promotion Association of Chinese Academy of Sciences |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001549279500001 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/321243]  |
| 专题 | 国家级研究中心_原创新药研究全国重点实验室 |
| 通讯作者 | Gao, Zhao-Bing; Yue, Jian-Min; Zhao, Jin-Xin |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ethnomed & Biofunct Mol Res Ctr, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Neurol & Psychiat Res & Drug Discovery, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zeng, Qi-Xiang,Wang, Lin-Lin,Zheng, Yue-Ming,et al. Asymmetric Total Synthesis and NaV1.8 Inhibitory Evaluation of Villosin B, 17-Hydroxymandarone B, and Their Derivatives[J]. ORGANIC LETTERS,2025,27(33):9201-9206. |
| APA | Zeng, Qi-Xiang.,Wang, Lin-Lin.,Zheng, Yue-Ming.,Yu, Yue.,Gao, Zhao-Bing.,...&Zhao, Jin-Xin.(2025).Asymmetric Total Synthesis and NaV1.8 Inhibitory Evaluation of Villosin B, 17-Hydroxymandarone B, and Their Derivatives.ORGANIC LETTERS,27(33),9201-9206. |
| MLA | Zeng, Qi-Xiang,et al."Asymmetric Total Synthesis and NaV1.8 Inhibitory Evaluation of Villosin B, 17-Hydroxymandarone B, and Their Derivatives".ORGANIC LETTERS 27.33(2025):9201-9206. |
入库方式： OAI收割
来源：上海药物研究所
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