کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1378200 981996 2005 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol
چکیده انگلیسی

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.

A coumarin-based esterase-sensitive prodrug (3) of meptazinol (1) was designed and synthesized to minimize the first-pass effect of meptazinol. Biological evaluation results in rats indicated that there was a 4-fold increase in oral bioavailability of this prodrug compared to the parent drug meptazinol.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 22, 15 November 2005, Pages 4953–4956
نویسندگان
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