Discovery of C-3 isoxazole substituted thiochromone S,S-dioxide derivatives as potent and selective inhibitors for monoamine oxidase B (MAO-B)

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成果类型：

期刊论文

作者：

Mi, Pengbing*;Tan, Yan;Ye, Shiying;Lang, Jia-Jia;Lv, You;...

通讯作者：

Mi, Pengbing;Yuan, Zhonghua;Zheng, X;Lin, YW

作者机构：

[Tan, Yan; Yuan, Zhonghua; Mi, Pengbing; Jiang, Jinhuan; Chen, Limei; Luo, Jianxiong; Zheng, Xing; Ye, Shiying; Lin, Yuqing; Zheng, X] Univ South China, Dept Pharm, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.

[Lang, Jia-Jia; Lin, Ying-Wu] Univ South China, Sch Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.

[Lang, Jia-Jia; Lin, Ying-Wu; Mi, Pengbing] Univ South China, Key Lab Prot Struct & Funct Univ Hunan Prov, Hengyang 421001, Hunan, Peoples R China.

[Zheng, Xing] Hunan Vocat Coll Sci & Technol, Dept Pharm, Changsha 410004, Hunan, Peoples R China.

[Lv, You] Shaanxi Univ Sci & Technol, Coll Bioresources Chem & Mat Engn, Xian 710021, Shaanxi, Peoples R China.

通讯机构：

[Yuan, ZH; Mi, PB; Lin, YW ; Zheng, X ] U

Univ South China, Dept Pharm, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.

Univ South China, Sch Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.

语种：

英文

关键词：

Human monoamine oxidase B inhibitor;Thiochromone;Thiochromone S,S-dioxide

期刊：

European Journal of Medicinal Chemistry

ISSN：

0223-5234

年：

2024

卷：

263

页码：

115956

DOI：

10.1016/j.ejmech.2023.115956

基金类别：

Acknowledgments The authors thank Natural Science Foundation of Hunan Province (2021JJ40451), The Research Foundation of Education Department of Hunan Province (21C0283, 21C0290), The Research Foundation of Health Commission of Hunan Province (202113050308), and The initial funding of University of South China (190XQD142) for financial support.

机构署名：

本校为第一且通讯机构

院系归属：

化学化工学院

药学与生物科学学院

摘要：

Developing new scaffolds for highly potent and selective inhibitors of human Monoamine Oxidase B (hMAO-B) is a crucial objective in enhancing the efficacy and safety in the clinical treatment of neurodegenerative diseases. In this study, we have identified a series of C-3 isoxazole-substituted thiochromone S,S-dioxide derivatives that exhibit strong inhibitory activity against hMAO-B. The strategy of oxidizing thiochromone to thiochromone S,S-dioxide solves the key defect of extreme insolubility observed for thiochromone analogues. In addition, the sulfone group contributes extra hydrogen(H)-b...

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Discovery of C-3 isoxazole substituted thiochromone S,S-dioxide derivatives as potent and selective inhibitors for monoamine oxidase B (MAO-B)

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