Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo [d] thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors

G Navarrete-Vazquez, M Ramírez-Martínez…

Index: Navarrete-Vazquez, Gabriel; Ramirez-Martinez, Marleth; Estrada-Soto, Samuel; Nava-Zuazo, Carlos; Paoli, Paolo; Camici, Guido; Escalante-Garcia, Jaime; Medina-Franco, Jose L.; Lopez-Vallejo, Fabian; Ortiz-Andrade, Rolffy European Journal of Medicinal Chemistry, 2012 , vol. 53, p. 346 - 355

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Citation Number: 11

Abstract

The ethyl 2-(6-substituted benzo [d] thiazol-2-ylamino)-2-oxoacetate derivatives (OX 1–9) were prepared using a one-step reaction. The in vitro inhibitory activity of the compounds against protein tyrosine phosphatase 1B (PTP-1B) was evaluated. Compounds OX-(1, 6 and 7) were rapid reversible (mixed-type) inhibitors of PTP-1B with IC50 values in the low micro- molar range. The most active compounds OX-(1, 6 and 7) were docked into the crystal ...