Permeation in artifical membrane of allopurinol derivatives with potential anti-t cruzi activity

S. GUALDESI; M. LONGHI; M. RAVIOLO

Cordoba

Congreso; 3a Reunión Internacional de Ciencias Farmacéuticas; 2014

Universidad Nacional de Córdoba

Chagas disease is caused by Trypanosoma cruzi (T. cruzi), and is a major health problem in Central and South America that affects nearly 8-10 million people. Allopurinol (Allop) is a hypoxantine analog used by the T. cruzi as an alternative purine substrate. Although Allop presents trypanocidal activity, its failure avoiding Chagas progression may be due in part to inadequate blood levels caused by unfavorable physicochemical properties, thus leading to versatile responses in humans. In an attempt to improve its performance, we have developed twelve derivatives of Allop by chemical modification, resulting in active anti-T cruzi agents per se or prodrugs compounds.1 The present study deals with the permeability of Allop and its derivatives by using artificial membranes as an in vitro technique that represent an interesting alternative to the use of animal tissues or cells because of its simplicity, in addition to showing comparable results to Caco-2 permeability.