2-Arylquinazolin-4(3H)-ones: A New Class of α-Glucosidase Inhibitors

Publication date: Available online 29 October 2015
Source:Bioorganic & Medicinal Chemistry
Author(s): Kulsoom Javaid, Syed Muhammad Saad, Saima Rasheed, Syed Tarique Moin, Naima Syed, Itrat Fatima, Uzma Salar, Khalid Mohammed Khan, Shahnaz Perveen, M. Iqbal Choudhary
Twenty-five derivatives of 2-arylquinazolin-4(3H)-ones (1-25) were evaluated for their yeast (Saccharomyces cerevisiae) α-glucosidase inhibitory activities. All synthetic compounds, except 1 and 6, were found to be several hundred fold more active (IC50 values in the range of 0.3 ± 0.01 - 117.9 ± 1.76 μM), than the standard drug, acarbose (IC50 = 840 ± 1.73 μM). The enzyme kinetic studies on the most active compounds 12, 4, 19, and 13 were performed for the determination of their modes of inhibition and dissociation constants Ki. Study of the modes of inhibition of compounds 12, and 4 were also performed using molecular modeling techniques. In brief, current study identifies a novel class of α-glucosidase inhibitors which can be further studied for the treatment of hyperglycemia and obesity.

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