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Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity

文献类型：期刊论文

作者Li, Mengyue8,9; Li, Huiyun5,7; Min, Xiaofeng8,9; Sun, Jinping8,9; Liang, Bingwen8,9; Xu, Lei6; Li, Jia1,5,6; Wang, Shao-Hua2,3,4; Xu, Xuetao8,9
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2024-05-09
卷号67期号:10页码:8406-8419
ISSN号0022-2623
DOI10.1021/acs.jmedchem.4c00676
通讯作者Li, Jia(jli@simm.ac.cn) ; Wang, Shao-Hua(wangshh@lzu.edu.cn) ; Xu, Xuetao(wyuchemxxt@126.com)
英文摘要Forty-one 1,3,4-thiadiazolyl-containing thiazolidine-2,4-dione derivatives (MY1-41) were designed and synthesized as protein tyrosine phosphatase 1B (PTP1B) inhibitors with activity against diabetes mellitus (DM). All synthesized compounds (MY1-41) presented potential PTP1B inhibitory activities, with half-maximal inhibitory concentration (IC50) values ranging from 0.41 +/- 0.05 to 4.68 +/- 0.61 mu M, compared with that of the positive control lithocholic acid (IC50 = 9.62 +/- 0.14 mu M). The most potent compound, MY17 (IC50 = 0.41 +/- 0.05 mu M), was a reversible, noncompetitive inhibitor of PTP1B. Circular dichroism spectroscopy and molecular docking were employed to analyze the binding interaction between MY17 and PTP1B. In HepG2 cells, MY17 treatment could alleviate palmitic acid (PA)-induced insulin resistance by upregulating the expression of phosphorylated insulin receptor substrate and protein kinase B. In vivo, oral administration of MY17 could reduce the fasting blood glucose level and improve glucose tolerance and dyslipidemia in mice suffering from DM.
WOS关键词TYROSINE-PHOSPHATASE 1B ; BIOLOGICAL EVALUATION ; NEGATIVE REGULATOR ; 2,4-THIAZOLIDINEDIONES ; THIAZOLIDINEDIONES ; THIADIAZOLE ; INSULIN ; POTENT
资助项目Department of Education of Guangdong Province[2023YFA1506404] ; National Key R&D Program of China[2021KCXTD044] ; Department of Education of Guangdong Province[2021B1212040016] ; Science and Technology Planning Project of Guangdong Province[2021WGALH08] ; Joint Research Fund for Wuyi University and Hong Kong and Macao[23ZDFA003] ; Joint Research Fund for Wuyi University and Hong Kong and Macao[23JRRA1144] ; Joint Research Fund for Wuyi University and Hong Kong and Macao[23JRRA1028] ; Joint Research Fund for Wuyi University and Hong Kong and Macao[23CXGA0043] ; Science and Technology Program of Gansu Province[2024-1-17] ; Science and Technology Program of Gansu Province[2023-QN-18] ; Lanzhou science and technology planning project[2021030103150006664] ; Key Project of Jiangmen Basic and Applied Basic Research
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001225426500001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/311276]  
专题新药研究国家重点实验室
通讯作者Li, Jia; Wang, Shao-Hua; Xu, Xuetao
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Chem Biol, Shanghai 201203, Peoples R China
2.Lanzhou Univ, Collaborat Innovat Ctr Northwestern Chinese Med, Lanzhou 730000, Peoples R China
3.Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China
4.Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China
5.Zunyi Med Univ, Sch Pharm, Zunyi 563000, Guizhou, Peoples R China
6.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Guangdong, Peoples R China
7.Chinese Acad Sci, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
8.Wuyi Univ, Guangdong Prov Key Lab Large Anim Models Biomed, Jiangmen 529020, Peoples R China
9.Wuyi Univ, Sch Pharm & Food Engn, Jiangmen 529020, Peoples R China
推荐引用方式
GB/T 7714		 Li, Mengyue,Li, Huiyun,Min, Xiaofeng,et al. Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity[J]. JOURNAL OF MEDICINAL CHEMISTRY,2024,67(10):8406-8419.
APA Li, Mengyue.,Li, Huiyun.,Min, Xiaofeng.,Sun, Jinping.,Liang, Bingwen.,...&Xu, Xuetao.(2024).Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity.JOURNAL OF MEDICINAL CHEMISTRY,67(10),8406-8419.
MLA Li, Mengyue,et al."Identification of 1,3,4-Thiadiazolyl-Containing Thiazolidine-2,4-dione Derivatives as Novel PTP1B Inhibitors with Antidiabetic Activity".JOURNAL OF MEDICINAL CHEMISTRY 67.10(2024):8406-8419.

入库方式： OAI收割

来源：上海药物研究所

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