Synthesis and biological evaluation of (±)-3-(2-(2-fluorobenzyloxy) naphthalen-6-yl)-2-aminopropanoic acid derivatives as novel PTP1B inhibitors
| Autor: | Wei-Ping Ma, Li-Xin Gao, Fajun Nan, Jia Li, Liang-Peng Sun, Hu-Ri Piao, Hong-Hua Piao, Qiang Shen, Wei Zhang |
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| Rok vydání: | 2011 |
| Předmět: |
Protein Tyrosine Phosphatase
Non-Receptor Type 1 Pharmacology Magnetic Resonance Spectroscopy Chemistry Stereochemistry Organic Chemistry General Medicine Nuclear magnetic resonance spectroscopy Protein Tyrosine Phosphatase 1B In vitro Inhibitory Concentration 50 Drug Discovery Inhibitory concentration 50 Enzyme Inhibitors Propionates Selectivity hormones hormone substitutes and hormone antagonists Biological evaluation |
| Zdroj: | European Journal of Medicinal Chemistry. 46:3630-3638 |
| ISSN: | 0223-5234 |
| Popis: | A series of novel nonphosphonate-based pTyr mimetics comprised (±)-3-(2-(2-fluorobenzyloxy)naphthalen-6-yl)-2-aminopropanoic acid derivatives were identified as reversible and competitive PTP1B inhibitors via a structure-based design approach. Among the compounds studied, 12h was found to have the best in vitro inhibition activity against PTP1B (IC(50) = 1.25 ± 0.24 μM) and the best selectivity (3-fold) between PTP1B and TCPTP. These results should provide suitable druglike lead compounds for the design of inhibitors of PTP1B as well as other PTPs. |
| Databáze: | OpenAIRE |
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