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Bioorganic & medicinal chemistry letters

Synthesis and relative bioavailability of meptazinol benzoyl esters as prodrugs.


PMID 15863326

Abstract

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.

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M2824
Meptazinol hydrochloride
C15H23NO· HCl