Antihyperuricemic effects of thiadiazolopyrimidin-5-one analogues in oxonate treated rats

Sathisha, Kadanuru R. and Shubha Gopal and Rangappa, K. S. (2016) Antihyperuricemic effects of thiadiazolopyrimidin-5-one analogues in oxonate treated rats. European Journal of Pharmacology, 776. 99 - 105.

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Hyperuricemia is a risk factor for not only gout, but also to a variety of disorders that affect the vital organ systems of the human body. The xanthine oxidase (XO) is the key enzyme in the production of uric acid and its inhibition can inhibit hyperuricemia. Although, XO inhibitor allopurinol is widely prescribed antigout agent but its use is not without any side effects. Previously, we described the synthesis of four novel thiadiazolopyrimidin-5-one analogues as effective XO inhibitors and molecular docking studies also confirmed this. When these analogues were tested in potassium oxonate treated rats, their serum uric acid and creatinine levels were dropped significantly from 4.85±0.03mg/dl to 1.21±0.01mg/dl and 0.92±0.02mg/dl to 0.40±0.02mg/dl respectively. Among the pyrimidine analogues tested, 6a was most potent. Histological examinations of both liver and kidney tissues exhibited severe necrosis in oxonate treated rats and pyrimidine analogues could significantly attenuate this with a correlative inhibitory profile of hepatic XO from the same rats. Our results demonstrate antihyperuricemic effect of novel thiadiazolopyrimidin-5-one analogues in oxonate treated rats, which can be further explored not only as antigout therapeutics but also in other systems where hyperuricemia is the driving cause of the disease.

Item Type: Article
Uncontrolled Keywords: Thiadiazolopyrimidin-5-one analogues, Potassium oxonate, Hyperuricemia, Xanthine oxidase, Gout
Subjects: B Life Science > Microbiology
Divisions: Department of > Microbiology
Depositing User: Manjula P Library Assistant
Date Deposited: 07 Jun 2019 07:48
Last Modified: 07 Jun 2019 07:48

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