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Citation: Yuan Feng Tong, Pei Zhang, Feng Chen, Ling Hua Hao, Fei Ye, Jin Ying Tian, Song Wu. Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors[J]. Chinese Chemical Letters, ;2010, 21(12): 1415-1418. doi: 10.1016/j.cclet.2010.07.005 shu

Synthesis and biological evaluation of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives as PTP1B inhibitors

a Department of New Drug Research and Development(Key Laboratory of Biosynthesis of Natural Products, Ministry of Health of PRC), Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China;
b Department of Pharmacology, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, China

Received Date: 8 April 2010

Fund Project: Financial support was provided by the National Natural Science Funds for Young Scholar (No.30901841),the Research Fund for the Doctoral Program of Higher Education of China (No.200800231145),and the Major Scientific and Technological Special Project for "Significant New Drugs Innovation" (No.2009ZX09301-003).

Based on the fact that petroselinic acid showed good inhibitory activity (IC₅₀=6.99 μmol/L) against protein tyrosine phophatase 1B (PTP1B) in vitro, a series of novel N-(alkoxyphenyl)-aminocarbonylbenzoic acid derivatives were designed and synthesized. The results indicated that most of the derivatives showed more potent activities against PTP1B. Especially, compound 13 had obvious activity with an IC₅₀ of 106 nmol/L in vitro.
- Petroselinic acid,
- PTP1B,
- N-(Alkoxyphenyl)-aminoearbonylbenzoic acid derivatives,
- Synthesis,
- Diabetes
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