Abstract:
Various functionalized mono- and diarylanthranilo-1,3-dinitriles were synthesized and evaluated for their in vitro antihyperglycemic activity against the PTP-1B, glucose-6-phosphatase, glycogen phosphorylase and alpha-glucosidase enzymes. Among various screened compounds, 5,6-diaryl substituted anthranilo-1,3-dinitriles 3a, 3b, and 3d showed good inhibitory activity against PTP-1B with IC50 values of 58-72 alphaM. Three of the test compounds showed significant (25-37%) lowering of plasma glucose level at 24 h in sucrose-challenged streptozotocin-induced diabetic Sprangue-Dawley rat model.
