An article Prodrug Strategies to Improve the Solubility of the HCV NS5A Inhibitor Pibrentasvir (ABT-530) WOS:000580558700022 published article about PROTEASE INHIBITORS; PHARMACOKINETICS; GLECAPREVIR; NUCLEOSIDE; DESIGN; SAFETY; SINGLE in [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.] Abbvie Inc, Global Pharmaceut Res & Dev, N Chicago, IL 60064 USA in 2020, Cited 26. Application In Synthesis of Isobenzofuran-1(3H)-one. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2
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 alkaline 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.
Application In Synthesis of Isobenzofuran-1(3H)-one. About Isobenzofuran-1(3H)-one, If you have any questions, you can contact Randolph, JT; Voight, EA; Greszler, SN; Uno, BE; Newton, JN; Gleason, KM; Stolarik, D; Van Handel, C; Bow, DAJ; DeGoey, DA or concate me.
Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem