Pyrazole-O-glucosides as novel Na(+)-glucose cotransporter (SGLT) inhibitors.

O-glucuronides and O-glucosides of a series of pyrazoles analogues were synthesized and evaluated for their SGLT inhibitory activity in brush border membrane vehicles (BBMVs) of rat kidney. O-glucosides of certain pyrazole analogues inhibited the transport of [(14)C]-glucose in BBMVs, and induced glucosuria in Wistar rats by intravenous injection.

APC0576, a novel inhibitor of NF-kappaB-dependent gene activation, prevents pro-inflammatory cytokine-induced chemokine production in human endothelial cells.

Endothelial cells participate in the inflammatory and immune reactions. Endothelial cell activation is a recurrent phenomenon linked to the pathogenesis of diverse human diseases, such as acute and chronic inflammation and cardiovascular disorders. Pro-inflammatory cytokines (e.