期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 22, 页码 4953-4956出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.016
关键词
meptazinol; coumarin-based prodrug; synthesis; bioavailability
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. (c) 2005 Elsevier Ltd. All rights reserved.
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