Two series of sulfonylureas derivatives including 24 compounds (4, 7, 5a–5o, 8a–8h), among them 17 new derivatives, have been synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 5c, 5h and 8e showed significant in vitro α-glucosidase inhibition with IC50 values of 5.58, 79.85 and 213.36 µm, respectively, comparing with the standard compounds acarbose (IC50 = 268.29 µm) and glipizide (IC50 = 300.47 µm). The preliminary structure-activity relationships (SARs) of the synthesized compounds were also investigated.
Glipizide is a second generation of sulfonylurea with promising hypoglycemic activity. It acts by stimulating the release of insulin from β-cells of pancreas. Glipizide is absorbed rapidly, uniformly with good mean oral bioavailability. It offers several advantages such as swift and short action, high potency and also does not accumulate in plasma on repeated oral administration. In this paper we report the acute and subacute toxicity of glipizide on BALB/c albino mice. The results showed the safety of our synthesized products.
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