2-Arylquinazolin-4(3H)-ones: Inhibitory Activities Against Xanthine Oxidase

Title:2-Arylquinazolin-4(3H)-ones: Inhibitory Activities Against Xanthine Oxidase

Volume: 12 Issue: 1

Author(s): Humaira Zafar, Syed M. Saad, Shahnaz Perveen, Arshia, Rizwana Malik, Ajmal Khan, Khalid M. Khan and Muhammad I. Choudhary

Affiliation:

Keywords: 2-Arylquinazolin-4(3H)-ones, xanthine oxidase inhibition, uric acid, gout, allopurinol.

Abstract: 2-Arylquinazolin-4(3H)-ones (1-25) were synthesized, and evaluated for their xanthine oxidase inhibitory activity. Significant to moderate activities were exhibited by the compounds 1-3, 7, 9, 13-15, 19-21, and 23 with IC₅₀ between 2.80 - 28.13 µM as compared to the standard allopurinol (IC₅₀ (IC50 = 2.01 ± 0.01 µM). Compounds 4-6, 8, 11-12, 16-18, 22, and 24 demonstrated a weak activity with IC₅₀ values 44.60 - 112.60 µM. Nonetheless, compounds 10 and 25 did not show any activity. Amongst all derivatives, compound 2, containing a C-4´ dimethylamino group, was the most potent inhibitor of the enzyme with an IC₅₀ value comparable to the standard. Kinetics studies on the most active compounds (2, 7, 9, 14, 15, 19, and 20) were conducted in order to determine their modes of inhibition and dissociation constants Ki. Some of the compounds of 2-arylquinazolin-4(3H)-one series were thus identified as potential leads for further studies towards the treatment of hyperuricemia and gout.

Cite this article as:

Zafar Humaira, M. Saad Syed, Perveen Shahnaz, Arshia , Malik Rizwana, Khan Ajmal, M. Khan Khalid and I. Choudhary Muhammad, 2-Arylquinazolin-4(3H)-ones: Inhibitory Activities Against Xanthine Oxidase, Medicinal Chemistry 2016; 12 (1) . https://dx.doi.org/10.2174/1573406410666150807111336