Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol |
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| Authors: | Xie Qiong Wang Xiaolin Wang Xinghai Jiang Zhiqiang Qiu Zhuibai |
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| Institution: | Department of Medicinal Chemistry, School of Pharmacy, Fudan University, 138 Yixueyuan Road, Shanghai 200032, PR China. |
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| Abstract: | 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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