Article ; Online: Indole- and Pyrazole-Glycyrrhetinic Acid Derivatives as PTP1B Inhibitors: Synthesis, In Vitro and In Silico Studies.
Molecules (Basel, Switzerland)
2021 Volume 26, Issue 14
Abstract: Regulating insulin and leptin levels using a protein tyrosine phosphatase 1B (PTP1B) inhibitor is an attractive strategy to treat diabetes and obesity. Glycyrrhetinic acid (GA), a triterpenoid, may weakly inhibit this enzyme. Nonetheless, semisynthetic ... ...
| Abstract | Regulating insulin and leptin levels using a protein tyrosine phosphatase 1B (PTP1B) inhibitor is an attractive strategy to treat diabetes and obesity. Glycyrrhetinic acid (GA), a triterpenoid, may weakly inhibit this enzyme. Nonetheless, semisynthetic derivatives of GA have not been developed as PTP1B inhibitors to date. Herein we describe the synthesis and evaluation of two series of indole- and |
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| MeSH term(s) | Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Glycyrrhetinic Acid/analogs & derivatives ; Glycyrrhetinic Acid/chemical synthesis ; Glycyrrhetinic Acid/chemistry ; Humans ; Indoles/chemical synthesis ; Indoles/chemistry ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Protein Tyrosine Phosphatase, Non-Receptor Type 1/antagonists & inhibitors ; Protein Tyrosine Phosphatase, Non-Receptor Type 1/chemistry ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Structure-Activity Relationship | |||||
| Chemical Substances | Enzyme Inhibitors ; Indoles ; Pyrazoles ; PTPN1 protein, human (EC 3.1.3.48) ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 (EC 3.1.3.48) ; Glycyrrhetinic Acid (P540XA09DR) | |||||
| Language | English | |||||
| Publishing date | 2021-07-20 | |||||
| Publishing country | Switzerland | |||||
| Document type | Journal Article | |||||
| ZDB-ID | 1413402-0 | |||||
| ISSN | 1420-3049 ; 1431-5165 ; 1420-3049 | |||||
| ISSN (online) | 1420-3049 | |||||
| ISSN | 1431-5165 ; 1420-3049 | |||||
| DOI | 10.3390/molecules26144375 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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