349621-50-7Relevant academic research and scientific papers
Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides
Moreno-Diaz, Hermenegilda,Villalobos-Molina, Rafael,Ortiz-Andrade, Rolffy,Diaz-Coutino, Daniel,Medina-Franco, Jose Luis,Webster, Scott P.,Binnie, Margaret,Estrada-Soto, Samuel,Ibarra-Barajas, Maximiliano,Leon-Rivera, Ismael,Navarrete-Vazquez, Gabriel
, p. 2871 - 2877 (2008)
N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives 1-8 were synthesized and evaluated for their in vivo antidiabetic activity in a non-insulin-dependent diabetes mellitus rat model. Several compounds synthesized showed significant lower
Synthesis, in vitro and computational studies of protein tyrosine phosphatase 1B inhibition of a small library of 2-arylsulfonylaminobenzothiazoles with antihyperglycemic activity
Navarrete-Vazquez, Gabriel,Paoli, Paolo,Leon-Rivera, Ismael,Villalobos-Molina, Rafael,Medina-Franco, Jose Luis,Ortiz-Andrade, Rolffy,Estrada-Soto, Samuel,Camici, Guido,Diaz-Coutino, Daniel,Gallardo-Ortiz, Itzell,Martinez-Mayorga, Karina,Moreno-Diaz, Hermenegilda
experimental part, p. 3332 - 3341 (2009/09/08)
The 2-arylsulfonylaminobenzothiazole derivatives 1-27 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 4 and 16 are rapid reversible (mixed-type) inhibitors of PTP-1B with IC50 values in the low micromolar range. The most active compounds (4 and 16) were docked into the crystal structure of PTP-1B. Docking results indicate potential hydrogen bond interactions between the nitro group in both compounds and the catalytic amino acid residues Arg 221 and Ser 216. Both compounds were evaluated for their in vivo antihyperglycemic activity in a type 2 diabetes mellitus rat model, showing significant lowering of plasma glucose concentration, during the 7 h post-intragastric administration.
