Bonina, Francesco and Puglia, Carmelo and Rimoli, Maria Grazia and Avallone, Lucia and Abignente, Enrico and Boatto, Gianpiero and Nieddu, Maria and Meli, Rosaria and Amorena, Michele and De Caprariis, Paolo (2002) Synthesis and in vitro chemical and enzymatic stability of glycosyl 3′-azido-3′-deoxythymidine derivatives as potential anti-HIV agents. European Journal of Pharmaceutical Sciences, Vol. 16 (3), p. 167-174. ISSN 0928-0987. Article.
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New glycosyl derivatives of 3′-azido-3′-deoxythymidine (AZT) (1 and 2) were synthesized in order to improve AZT retention in the blood and to guarantee its sustained release, overcoming the necessity of multiple drug administrations. The esters synthesized (1 and 2) link AZT, by a succinyl linker, to the C-3 position of glucose and to C-6 of galactose. Furthermore, the chemical and enzymatic stabilities of esters 1 and 2 were evaluated in order to determine both their stability in aqueous medium and their feasibility to undergo enzymatic cleavage by esterase to regenerate the original drug. The pharmacokinetic profiles of esters 1 and 2, obtained after systemic administration, showed an interesting controlled release, in particular for ester 2, compared to the pharmacokinetic profile of AZT.
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