Synthesis of benzofuran scaffold-based potential PTP-1B inhibitors.
Protein tyrosine phosphatase 1B (PTP-1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Studies have shown that PTP-1B knockout mice showed increased insulin sensitivity in muscle and liver as well as resistance to obesity. A series of hydroxy benzofuran methyl ketones and their naturally mimicking dimers and linear and angular furanochalcones and flavones have been evaluated as PTP-1B inhibitors. Screened compounds displayed good inhibitory activity.
Dixit
Manish
M
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. agoel13@yahoo.com
Tripathi
Brajendra K
BK
Tamrakar
Akhilesh K
AK
Srivastava
Arvind K
AK
Kumar
Brijesh
B
Goel
Atul
A
D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D003500:Cyclization; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D014638:Vanadates / Q000494:pharmacology
D001572:Benzofurans; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D014638:Vanadates; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases