Synthesis and relative bioavailability of meptazinol benzoyl esters as prodrugs.
Three meptazinol benzoyl esters (1-3) were synthesized as prodrugs to minimize the first-pass effect of meptazinol and improve the bioavailability. Among these three esters, compound 3 showed better bioavailability than the parent meptazinol. Further, the relative regional bioavailability of prodrug 3 was evaluated using in situ closed loop study in rats, which showed that prodrug 3 has higher absorption efficacy in rat intestine. Thusly, prodrug 3 may be worth for further development.
Lu
Meiyan
M
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 138 Yixueyuan Road, Shanghai 200032, PR China.
Zhang
Chengji
C
Hao
Jinglai
J
Qiu
Zhuibai
Z
D001682:Biological Availability; D004952:Esters; D008621:Meptazinol / Q000737:chemistry / Q000493:pharmacokinetics*; D015394:Molecular Structure; D011355:Prodrugs / Q000493:pharmacokinetics*
D004952:Esters; D011355:Prodrugs; D008621:Meptazinol