Randolph, John T.; Voight, Eric A.; Greszler, Stephen N.; Uno, Brice E.; Newton, James N.; Gleason, Kenneth M.; Stolarik, DeAnne; Van Handel, Cecilia; Bow, Daniel A. J.; DeGoey, David A. published the artcile< Prodrug Strategies to Improve the Solubility of the HCV NS5A Inhibitor Pibrentasvir (ABT-530)>, Quality Control of 623-50-7 , the main research area is prodrug pibrentasvir solubility.
A research program to discover solubilizing prodrugs of the HCV NS5A inhibitor pibrentasvir (PIB) identified phosphomethyl analog 2 and trimethyl-lock (TML) prodrug 9. The prodrug moiety is attached to a benzimidazole nitrogen atom via an oxymethyl linkage to allow for rapid and complete release of the drug for absorption following phosphate removal by intestinal alk. phosphatase. These prodrugs have good hydrolytic stability properties and improved solubility compared to PIB, both in aqueous buffer (pH 7) and FESSIF (pH 5). TML prodrug 9 provided superior in vivo performance, delivering high plasma concentrations of PIB in PK studies conducted in mice, dogs, and monkeys. The improved dissolution properties of these phosphate prodrugs provide them the potential to simplify drug dosage forms for PIB-containing HCV therapy.
Journal of Medicinal Chemistry published new progress about Antiviral agents. 623-50-7 belongs to class esters-buliding-blocks, and the molecular formula is C4H8O3, Quality Control of 623-50-7 .
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics