Design, Synthesis, and Structure-Activity Relationship of Novel Potent and Highly Selective Cysteinyl Leukotriene Receptor 1 (CysLT1R) Antagonists
文献类型：期刊论文
| 作者 | Wang Jingyi2,3; Liu Jinyu1; Chen Dongsheng2; Chen Huayan2; Xie Xin1,2,3 ; Nan Fajun2,3
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| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2024 |
| 卷号 | 44期号:1页码:259-276 |
| 关键词 | cysteinyl leukotriene cysteinyl leukotriene receptor 1 (CysLT1R) selective antagonists |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc202306001 |
| 通讯作者 | Xie Xin(xxie@simm.ac.cn) ; Nan Fajun(fjnan@simm.ac.cn) |
| 英文摘要 | Cysteinyl leukotrienes (CysLTs) are lipid mediators of inflammation, and their receptors (CysLTsR) play an essential role in asthma, allergic rhinitis, cancer, and other diseases. According to earlier studies, 3-substituted 1H-indole-2-car-boxylic acid derivatives displayed selective cysteinyl leukotriene receptor 1 (CysLT1R) antagonistic activity, while their poor water solubility restricted their further evaluation. Hence, structural optimization was continued and multiple series of compounds were designed and synthesized based on existing research foundations. Among them, 3-(2-((E)-3-((3-((E)-2-(7-chloro-quinolin2-yl)vinyl)phenyl)amino)-3-oxoprop-1-en-1-yl)phenyl)propanoic acid (T9) exhibits good selective CysLT(1) receptor antagonistic activity and improved solubility, with IC50 value of (0.0066 +/- 0.0023) mu mol/L and water solubility of 4.16x10(-5) g/mL. |
| WOS关键词 | DERIVATIVES ; DISCOVERY |
| 资助项目 | National Natural Science Foundation of China[82003571] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001195410700006 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/310544]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Xie Xin; Nan Fajun |
| 作者单位 | 1.Nanjing Univ Chinese Med, Nanjing 210023, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Media, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang Jingyi,Liu Jinyu,Chen Dongsheng,et al. Design, Synthesis, and Structure-Activity Relationship of Novel Potent and Highly Selective Cysteinyl Leukotriene Receptor 1 (CysLT1R) Antagonists[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2024,44(1):259-276. |
| APA | Wang Jingyi,Liu Jinyu,Chen Dongsheng,Chen Huayan,Xie Xin,&Nan Fajun.(2024).Design, Synthesis, and Structure-Activity Relationship of Novel Potent and Highly Selective Cysteinyl Leukotriene Receptor 1 (CysLT1R) Antagonists.CHINESE JOURNAL OF ORGANIC CHEMISTRY,44(1),259-276. |
| MLA | Wang Jingyi,et al."Design, Synthesis, and Structure-Activity Relationship of Novel Potent and Highly Selective Cysteinyl Leukotriene Receptor 1 (CysLT1R) Antagonists".CHINESE JOURNAL OF ORGANIC CHEMISTRY 44.1(2024):259-276. |
入库方式： OAI收割
来源：上海药物研究所
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