Therapeutic potential of synthetic pyrazolotriazinones for the hyperuricemia treatment

MARÍA LOURDES SCIU; DANIELA SANTI; CARLOS ROCA; NURIA CAMPILLO; ANA MARTINEZ; GABRIELA ORTEGA; ELIZABETH MOYANO

BUENOS AIRES

Otro; Reunion Conjunta de Biociencias; 2017

Xanthine oxidase (XO) is a widely distributed enzyme involve in the later stages of purine catabolism, catalyzing the oxidation of hypoxanthine to xanthine and of xanthine to uric acid. A high level of this acid in the blood stream produced hyperuricemia, which could develop to gout, nephrolithiasis, cardiovascular disease, hypertension and diabetes, among others. Allopurinol is a well-known XO inhibitor, a purine analogue, currently used for the treatment of hyperuricemia. However, numerous side effects have been reported due to Allopurinol administration.In this study, pyrazolotriazinone compounds structurally related to purine bases were synthesized and evaluated for their ability to inhibit XO in vitro. Molecular docking studies has been performed to explain the binding modes of XO with the selected compounds.