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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 22, 15 November 2005, Pages 4953–4956
نویسندگان
Qiong Xie, Xiaolin Wang, Xinghai Wang, Zhiqiang Jiang, Zhuibai Qiu,