Bioorganic & Medicinal Chemistry Letters 2005-05-16

Synthesis and relative bioavailability of meptazinol benzoyl esters as prodrugs.

Meiyan Lu, Chengji Zhang, Jinglai Hao, Zhuibai Qiu

文献索引：Bioorg. Med. Chem. Lett. 15(10) , 2607-9, (2005)

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摘要

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.