Design, synthesis and activity evaluation of novel quinazolinone compounds as TRPC5 inhibitors
文献类型：期刊论文
| 作者 | Bai, Longhui2,4,6; Xiang, Yu3,5; Shen, Meiling2,4,6; Han, Yujun3,5; Li, Penghua2,4,6; Zuo, Zhili2,4,6; Li, Yang1,2,3,5
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| 刊名 | BIOORGANIC CHEMISTRY
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| 出版日期 | 2025-02-01 |
| 卷号 | 155页码:20 |
| 关键词 | TRPC5 Inhibitors Structural modifications and optimizing Synthesis Quinazolinone compounds Activity evaluation |
| ISSN号 | 0045-2068 |
| DOI | 10.1016/j.bioorg.2025.108147 |
| 英文摘要 | The TRPC5 channel plays an important role in regulating various physiological processes, which is related to various human diseases, especially psychiatric and kidney diseases. Although the TRPC5 channel is one of the essential potential target, no drugs against TRPC5 channels have been granted in the market to date. In this study, based on the structure of hit compound ph1, we further synthesied 49 compounds of novel quinazolinone and heterocyclic fusion pyrimidinone derivatives, and their activities were evaluated by electrophysiological assays. After extensive screening, 21 compounds exhibited significant TRPC5 inhibitory activity, and compounds ph8 and ph14 displayed strong inhibitory with IC50 of 1.28 and 2.16 mu M, respectively. These identified potential TRPC5 inhibitor may provide lead compounds and experimental evidence for the development of novel TRPC5 inhibitors with potential treatment for anxiety, depression, and progressive kidney disease. |
| WOS关键词 | POTENT ; IDENTIFICATION ; CHANNELS ; AMYGDALA |
| 资助项目 | General Program of Applied Basic Research of Yunnan Province[202001AS070026] ; Yunnan Science and Technology Major Project[202202AA100012] ; State Key Laboratory of Phyto-chemistry and Plant Resources in West China[CASSIMM0220184017] ; National Natural Science Foundation of China[32371005] ; National Natural Science Foundation of China[31671049] ; Shanghai Municipal Science and Technology Major Project[184319071000] ; Shanghai Municipal Science and Technology Major Project[19140903102] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001399720400001 |
| 出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/315893]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zuo, Zhili; Li, Yang |
| 作者单位 | 1.Fudan Univ, Huashan Hosp, Natl Clin Res Ctr Aging & Med, Shanghai 200040, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 4.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Chi, Kunming 650201, Peoples R China 5.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 6.Univ Chinese Acad Sci, Sch Intelligent Sci & Technol, Hangzhou Inst Adv Study, Hangzhou 310024, Peoples R China |
| 推荐引用方式 GB/T 7714 | Bai, Longhui,Xiang, Yu,Shen, Meiling,et al. Design, synthesis and activity evaluation of novel quinazolinone compounds as TRPC5 inhibitors[J]. BIOORGANIC CHEMISTRY,2025,155:20. |
| APA | Bai, Longhui.,Xiang, Yu.,Shen, Meiling.,Han, Yujun.,Li, Penghua.,...&Li, Yang.(2025).Design, synthesis and activity evaluation of novel quinazolinone compounds as TRPC5 inhibitors.BIOORGANIC CHEMISTRY,155,20. |
| MLA | Bai, Longhui,et al."Design, synthesis and activity evaluation of novel quinazolinone compounds as TRPC5 inhibitors".BIOORGANIC CHEMISTRY 155(2025):20. |
入库方式： OAI收割
来源：上海药物研究所
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