Author/Authors :
Rosanna Maccari، نويسنده , , Paolo Paoli، نويسنده , , Rosaria Ottanà، نويسنده , , Michela Jacomelli، نويسنده , , Rosella Ciurleo، نويسنده , , Giampaolo Manao، نويسنده , , Theodora Steindl، نويسنده , , Thierry Langer، نويسنده , , Maria Gabriella Vigorita، نويسنده , , Guido Camici، نويسنده ,
Abstract :
4-(5-Arylidene-2,4-dioxothiazolidin-3-yl)methylbenzoic acids (2) were synthesized and evaluated in vitro as inhibitors of PTP1B and LMW-PTP, two protein tyrosine phosphatases (PTPs) which act as negative regulators of the metabolic and mitotic signalling of insulin. The synthesis of compounds 2 represents an example of utilizing phosphotyrosine-mimetics to identify effective low molecular weight nonphosphorus inhibitors of PTPs. Several thiazolidinediones 2 exhibited PTP1B inhibitory activity in the low micromolar range with moderate selectivity for human PTP1B and IF1 isoform of human LMW-PTP compared with other related PTPs.
Keywords :
molecular modelling , Protein tyrosine phosphatases , diabetes mellitus , PTP1B and LMW-PTP inhibitors
