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Design, synthesis and evaluation of phenoxyacetic acid-based PTP1B inhibitors
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Jin-ying TIAN, Jun-zheng LIU, Shu-en ZHANG, Xiao-lin ZHANG, Fei YE, Zhi-yan XIAO*
Acta Pharmaceutica Sinica | 2023, 58(12) : 3684 - 3690
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Acta Pharmaceutica Sinica | 2023, 58(12): 3684-3690
Design, synthesis and evaluation of phenoxyacetic acid-based PTP1B inhibitors
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Jin-ying TIAN, Jun-zheng LIU, Shu-en ZHANG, Xiao-lin ZHANG, Fei YE, Zhi-yan XIAO*
Affiliations
  • Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Diabetes Research Center of Chinese Academy of Medical Sciences, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2023-12-12 doi: 10.16438/j.0513-4870.2023-1195
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Protein tyrosine phosphatase (PTP) 1B is a potential therapeutic target for type 2 diabetes. Phosphotyrosine (pTyr) mimetics still dominate the currently available PTP1B inhibitors. The phenoxyacetic acid moiety was taken as a pTyr mimetic herein and phenoxyacetic acid-based compounds 2a-2g and 3a-3c were designed. Among them, compounds 2a-2g exhibited potent inhibition against PTP1B, and compound 2g showed an IC50 of 0.42 μmol·L-1 against PTP1B. Compound 2f exhibited pharmacological profiles similar to that of rosiglitazone, and could improve the insulin sensitivity and the serum total cholesterol level. The results suggest that PTP1B inhibitors might be effective in treating type 2 diabetes as well as associated metabolic syndromes.

PTP1B inhibitor  /  pTyr mimetic  /  phenoxyacetic acid  /  insulin sensitizer
Jin-ying TIAN, Jun-zheng LIU, Shu-en ZHANG, Xiao-lin ZHANG, Fei YE, Zhi-yan XIAO. Design, synthesis and evaluation of phenoxyacetic acid-based PTP1B inhibitors[J]. Acta Pharmaceutica Sinica, 2023 , 58 (12) : 3684 -3690 . DOI: 10.16438/j.0513-4870.2023-1195
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Year 2023 volume 58 Issue 12
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doi: 10.16438/j.0513-4870.2023-1195
  • Receive Date：2023-10-23
  • Online Date：2025-11-21
  • Published：2023-12-12
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  • Received：2023-10-23
  • Revised：2023-10-31
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    Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Diabetes Research Center of Chinese Academy of Medical Sciences, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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