In vitro and in silico PTP-1B inhibition and in vivo antidiabetic activity of semisynthetic moronic acid derivatives

[Display omitted] Six derivatives (1–6) of moronic acid were semi-synthesized and their in vitro protein tyrosine phosphatase 1B (PTP-1B) inhibition activity assessed. Derivatives 2 (IC50=10.8±0.5μM) and 6 (IC50=7.5±0.1μM) displayed the most potent inhibitory activity. Therefore, they (50mg/Kg) were...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 26; no. 8; pp. 2018 - 2022
Main Authors:	Cerón-Romero, Litzia, Paoli, Paolo, Camici, Guido, Flores-Morales, Virginia, Rios, María Yolanda, Ramírez-Espinosa, Juan J., Hidalgo-Figueroa, Sergio, Navarrete-Vázquez, Gabriel, Estrada-Soto, Samuel
Format:	Journal Article
Language:	English
Published:	England Elsevier Ltd 15-04-2016
Subjects:	Animals Blood Glucose - drug effects Computer Simulation Diabetes Diabetes Mellitus, Experimental - drug therapy Diabetes Mellitus, Experimental - enzymology Dose-Response Relationship, Drug Enzyme inhibition Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Molecular docking Molecular Docking Simulation Molecular Structure Moronic acid derivatives Oleanolic Acid - analogs & derivatives Oleanolic Acid - chemical synthesis Oleanolic Acid - chemistry Oleanolic Acid - pharmacology Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors Protein Tyrosine Phosphatase, Non-Receptor Type 1 - metabolism PTP-1B Rats Structure-Activity Relationship Moronic acid derivatives Enzyme inhibition PTP-1B RGKMKULXFZOUPF-BQSMYOSZSA-N SXYLITRDEAEYTJ-MGPMMZCJSA-N Diabetes Molecular docking
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