Ligand-Enabled Pd-Catalyzed sp3 C-H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease
文献类型：期刊论文
| 作者 | Bi, Tongyu6,7; Cui, Yunxia5; Liu, Shuai4; Yu, Haiyue6,7; Qiu, Weirong1,6,7; Hou, Ke-Qiang6,7; Zou, Jiaqi3; Yu, Zhipeng3; Zhang, Feili6,7; Xu, Zhongliang6,7 |
| 刊名 | ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
 |
| 出版日期 | 2024-11-04 |
| 卷号 | 63期号:45页码:11 |
| 关键词 | C-H activation ligand-mediated macrocyclization Pd catalysis SIRT3 PD treatment |
| ISSN号 | 1433-7851 |
| DOI | 10.1002/anie.202412296 |
| 通讯作者 | Zhang, Jian(jian.zhang@sjtu.edu.cn) ; Xu, Xiaojun(xiaojunxu@zju.edu.cn) ; Yang, Weibo(yweibo@simm.ac.cn) |
| 英文摘要 | The development of simplified synthetic strategy to create structurally and functionally diverse pseudo-natural macrocyclic molecules is highly appealing but poses a marked challenge. Inspired by natural scaffolds, herein, we describe a practical and concise ligand-enabled Pd(II)-catalyzed sp3 C-H alkylation, olefination and arylation macrocyclization, which could offer a novel set of pseudo-natural macrocyclic sulfonamides. Interestingly, the potential of ligand acceleration in C-H activation is also demonstrated by an unprecedented enantioselective sp3 C-H alkylation macrocyclization. Moreover, a combination of in silico screening and biological evaluation led to the identification of a novel spiro-grafted macrocyclic sulfonamide 2 a, which showed a promising efficacy for the treatment of Parkinson's disease (PD) in a mouse model through the activation of silent information regulator sirtuin 3 (SIRT3). |
| WOS关键词 | C(SP(3))-H ; ACTIVATION ; PEPTIDES |
| 资助项目 | National Natural Science Foundation of China ; National Key R&D Program of China[2023YFF1205103] ; Program of Shanghai Academic/Technology Research Leader[23XD1424400] ; Program of Shanghai Academic/Technology Research Leader[2023695] ; Postdoctoral Fellowship Program of CPSF[GZC20232843] ; [81925034] ; [82373708] ; [22171275] ; [81973500] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001342232800012 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/314020]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhang, Jian; Xu, Xiaojun; Yang, Weibo |
| 作者单位 | 1.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China 2.Zhejiang Univ, Int Inst Med, Ctr Innovat Tradit Chinese Med Target & New Drug R, Yiwu 322000, Zhejiang, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210000, Peoples R China 4.China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China 5.Shanghai Jiao Tong Univ, Ruijin Hosp, Natl Res Ctr Translat Med Shanghai, State Key Lab Med Genom,Sch Med, Shanghai, Peoples R China 6.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 7.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Bi, Tongyu,Cui, Yunxia,Liu, Shuai,et al. Ligand-Enabled Pd-Catalyzed sp3 C-H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease[J]. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION,2024,63(45):11. |
| APA | Bi, Tongyu.,Cui, Yunxia.,Liu, Shuai.,Yu, Haiyue.,Qiu, Weirong.,...&Yang, Weibo.(2024).Ligand-Enabled Pd-Catalyzed sp3 C-H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease.ANGEWANDTE CHEMIE-INTERNATIONAL EDITION,63(45),11. |
| MLA | Bi, Tongyu,et al."Ligand-Enabled Pd-Catalyzed sp3 C-H Macrocyclization: Synthesis and Evaluation of Macrocyclic Sulfonamide for the Treatment of Parkinson's Disease".ANGEWANDTE CHEMIE-INTERNATIONAL EDITION 63.45(2024):11. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。