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A REVIEW ON THE DESIGN AND SYNTHESIS OF PYRIMIDIN-5-ONE DERIVATIVES AS XANTHINE OXIDASE INHIBITORS. Divya Gumber and Rakesh Yadav

A REVIEW ON THE DESIGN AND SYNTHESIS OF PYRIMIDIN-5-ONE DERIVATIVES AS XANTHINE OXIDASE INHIBITORS.

Divya Gumber and Rakesh Yadav

International Journal of Natural Product Science 2012: Spl Issue 1:103.

Abstract(RBIP-103)

Hyperuricemia is the underlying cause of gout and other ailments. Xanthine oxidase is the key enzyme which is involved in the oxidation of hypoxanthine to xanthine and then to uric acid. Allopurinol (1), a widely used xanthine oxidase inhibitor is the most commonly used drug for the treatment of gout. Significant portion of the population suffers from adverse effects of allopurinol that includes gastrointestinal upset, skin rashes and hypersensitivity reactions. Moreover, an elevated level of uric acid is considered as an independent risk factor for cardiovascular diseases.

(1) (2)
R = Electron withdrawings groups

Therefore use of allopurinol-like drugs with minimum side effects is the ideal drug of choice against gout. In this review, synthesis and design of a series of pyrimidin-5-one analogues (2) as effective xanthine oxidase inhibitors has been reported.
Molecular modeling and docking studies revealed that the one of the synthesized molecule has very good interactions with the Molybdenum–Oxygen–Sulfur (MOS) complex, a key component in xanthine oxidase. The outcome highlights the identification of a new class of xanthine oxidase inhibitors that have potential to be more efficacious, than allopurinol, to treat gout and possibly against cardiovascular diseases.
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