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期刊论文
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol
Bioorg. Med. Chem. Lett. 15(2005)4953-4956,-0001,():
Based on the known coumarin-based prodrug system, a new meptazinol (Z)-3-[2-(propionyloxy) phenyl]-2-propenoic ester (3) was designed and synthesized as prodrug to minimize the first-pass effect of meptazinol (1) and improve the oral bioavailability. The prodrug (3) showed a 4-fold increase in oral bioavailability over the parent drug meptazinol in rats.
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