Bioorganic and Medicinal Chemistry Letters 2005-Jul
Synthesis of functionalized acetophenones as protein tyrosine phosphatase 1B inhibitors.
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Abstrakts
Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that plays a critical role in down-regulating insulin signaling through dephosphorylation of the insulin receptor. Studies have shown that PTP1B knock-out mice showed increased insulin sensitivity in muscle and liver as well as resistance to obesity. A series of functionalized acetophenones were synthesized and evaluated for their PTP1B inhibitory activity. Some of the screened compounds displayed good inhibitory activity.