Study of the chemical and enzymatic stability of new zidovudine prodrugs

SCHENFELD, E.M.; RIBONE, S.R.; BRIÑÓN, M.C.; QUEVEDO, M.A.

Rosario - Argentina

Congreso; 2a Reunión Internacional de Ciencias Farmacéuticas; 2012

Comité de la 2a Reunión Internacional de Ciencias Farmacéuticas

Zidovudine (AZT) is a widely used anti HIV drug, which exhibits a vastly demonstrated clinical efficacy. Unfortunately, this drug presents several adverse effects that are consequence of its suboptimal pharmacotherapeutic properties. To improve these properties, several strategies have been applied, among which the design and synthesis of prodrugs has been pursued. Considering that these prodrugs require adequate stability, both in aqueous and physiological conditions, the need to evaluate and rationalize this behavior is critical. In this context, the general objective of this work is to study the chemical and enzymatic stability of three new prodrugs of AZT with essential aminoacids that were previously obtained in our research group,1 namely AZT-l-Leu (l-leucine), AZT-l-Pha (l-phanylalanine) and AZT-d-Pha.