Preparation and prodrug studies of quercetin pentabenzensulfonate.
Pentabenzensulfonate (QPBS), a potential prodrug for quercetin, was designed and synthesized in high yield. It possesses better physical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kinetics than its original form. The LogP value (2.04) and the half-life of the hydrolysis value (3.85 h) show that oral bioavailability is improved evidently compared with that of quercetin. These results indicate that QPBS can be considered as a potential prodrug for quercetin.
Peng
You
Y
State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang, China.
Deng
Zeyuan
Z
Wang
Chunfeng
C
D001557:Benzenesulfonates / Q000138:chemical synthesis* / Q000737:chemistry; D001682:Biological Availability; D006207:Half-Life; D006868:Hydrolysis; D008055:Lipids; D008968:Molecular Conformation; D011355:Prodrugs; D011794:Quercetin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D012995:Solubility; D014867:Water
D001557:Benzenesulfonates; D008055:Lipids; D011355:Prodrugs; C535103:quercetin pentabenzenesulfonate; D014867:Water; D011794:Quercetin