药代动力学与实验治疗学杂志

抽象的

Involvement of Multiple Transporters within the Oral Absorption of Glycoside Analogues

Lewes Zang

Nucleoside analogues square measure 1st line therapy in numerous severe maladies: AIDS (acquired immunological disorder disease syndrome), herpes virus infections, cancer, etc. However, several glycoside analogues exhibit poor oral bioavailability attributable to their high polarity and low viscous porousness. so as to urge around this disadvantage, prodrugs are utilised to enhance lipophility by chemical modification of the parent drug. As an alternative, prodrugs targeting transporters gift within the gut are applied to market the transport of the glycoside analogues [1]. Valacyclovir and valacyclovir square measure 2 classic essential amino acid organic compound prodrugs transported by oligopeptide transporter one. The perfect prodrug achieves delivery of a parent drug by attaching a non-toxic moiety that's stable throughout transport, however is quickly degraded to the parent drug once at the target. This text presents advances of prodrug approaches for enhancing oral absorption of glycoside analogues. Within the gift work, we have a tendency to delineate the synthesis, antiviral profiles and metabolic stability in human plasma of compound half-dozen, a possible carbonate prodrug of HIV-1 NNRTI drug candidate RDEA427. Compound half-dozen was found to inhibit the wild-type (WT) and K103N/Y181C double mutant HIV-1 strains at Nano- and submicromolar concentrations, severally [2].