Highly water-soluble prodrugs of anthelmintic benzimidazole carbamates: Synthesis, pharmacodynamics, and pharmacokinetics
Highly water-soluble prodrugs of anthelmintic benzimidazole carbamates: Synthesis, pharmacodynamics, and pharmacokinetics
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DOI：
10.1021/jm701456r
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发表时间：
2008-03-13
影响因子：
7.3
通讯作者：
Uphoff, M.
中科院分区：
文献类型：
--
作者：
Chassaing, C.;Berger, M.;Uphoff, M.
本文合成了苯并咪唑氨基甲酸酯2a-g的高水溶性前药1a-g。这些前药结合了联合收割机的高水溶性和稳定性以及碱性磷酸酶存在下的高不稳定性。通过进行的药效学和药代动力学研究显示了1a的兽医效用。猪。用前药Ia或母体芬苯达唑2a观察到相当的驱虫功效。药代动力学结果表明，2a从1a衍生时比原样应用时吸收更好。
Highly water-soluble prodrugs 1a - g of anthelmintic benzimidazole carbamates 2a - g were synthesized. These prodrugs combine high aqueous solubility and stability with high lability in the presence of alkaline phosphatases. The veterinary utility of 1a was shown by a pharmacodynamic and pharmacokinetic study performed. in swine. Comparable anthelmintic efficacy was observed with prodrug la or the parent fenbendazole 2a. The pharmacokinetic results showed that 2a is better absorbed when derived from 1a than when applied as such.