Biomaterials Center, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5895-9. doi: 10.1016/j.bmcl.2010.07.089. Epub 2010 Jul 25.
Synthesis of novel amides and esters prodrugs of olmesartan is described. Their in vitro stability in rat plasma was tested. The results showed that the ester derivative IIa with n-octyl substituted dioxolone moiety was rapidly converted into olmesartan within 30 min. The pharmacokinetic parameters of IIa were studied and compared with those of olmesartan medoxomil. Compound IIa is proposed to be a promising prodrug of olmesartan.
本文描述了新型奥美沙坦酰胺和酯前药的合成。测试了它们在大鼠血浆中的体外稳定性。结果表明，具有正辛基取代二恶烷部分的酯衍生物 IIa 在 30 分钟内迅速转化为奥美沙坦。研究了 IIa 的药代动力学参数，并与奥美沙坦酯进行了比较。该化合物 IIa 被认为是奥美沙坦有前途的前药。
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