Stock, Nicholas S. published the artcile5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3-tert-Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor, Name: Imidazo[1,2-a]pyridin-2-ylmethanol, the main research area is lipoxygenase activating protein inhibitor AM803 GSK2190915 antiasthmatic; FLAP inhibitor SAR.
The potent 5-lipoxygenase-activating protein (FLAP) inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid 11cc (I) is described (AM803, now GSK2190915). Building upon AM103, SAR studies centering around the pyridine moiety led to the discovery of compounds that exhibit significantly increased potency in a human whole blood assay measuring LTB4 inhibition with longer drug preincubation times (15 min vs 5 h). Further studies identified 11cc with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood (5 h incubation) and excellent preclin. toxicol. and pharmacokinetics in rat and dog. 11Cc also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model. This compound has successfully completed phase 1 clin. studies in healthy volunteers and is currently undergoing phase 2 trials in asthmatic patients.
Journal of Medicinal Chemistry published new progress about Blood serum albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (human serum albumin – FLAP binding equilibrium). 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Name: Imidazo[1,2-a]pyridin-2-ylmethanol.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem