Total synthesis of bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane as potent PTP1B inhibitor

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Protein tyrosine phosphatase 1B (PTPI B) plays an important role as a negative regulator and has been proved to be an effective target for the treatment of type 2 diabetes mellitus.Bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane 7 was first reported as a natural bromopbenol with significant inhibition against PTP1B which was isolated from red algae Rhodomela confervoides.Intrigued by its astonishing activity (IC50=2.4 μmol/L),compound 7 was synthesized with the overall yield of 24% and evaluated for its PTP1B inhibitory activity compared with natural compound.
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