中文关键词:1α,25-二羟基维生素D₂ 类似物度骨化醇 帕立骨化醇化学合成 生物活性 英文关键词:1α,25-dihydroxyvitamin D₂analoguesdoxercalciferolparicalcitolchemical synthesisbiological activities 基金项目:

作者	单位	E-mail
胡代花	陕西理工大学 维生素D生理与应用研究所 汉中 723000	hudaihua007@163.com
陈旺	陕西理工大学

摘要点击次数:1800 全文下载次数:0 中文摘要: 1α,25-二羟基维生素D₂(1α, 25-(OH) ₂-D₂,125D2)是维生素D₂的活性代谢产物。125D2与活性维生素D₃(1α,25-二羟基维生素D₃,125D)的活性很相似,125D因高钙血症副反应而限制其临床应用,而维生素D₂及其类似物一般比相应维生素D₃类化合物副作用较小。本文综述了两种临床应用效果较好的维生素D₂类似物度骨化醇及帕立骨化醇的合成新进展,以及侧链修饰、19-去亚甲基、A环C3位修饰和九重氢同位素标记的维生素D₂类似物的合成及生物活性研究新进展,旨在为新型活性维生素D₂类似物的合成及临床开发提供参考。 英文摘要: 1α,25-Dihydroxyvitamin D₂(1α,25-(OH)₂-D₂; 125D2)is the active metabolite form of vitamin D₂, and 1α,25-dihydroxyvitamin D₃(1α,25-(OH)₂-D₃; 125D)is the most active metabolite of vitamin D₃. The biological activity of 125D2 and 125D is similar, but the therapeutic application of 125D is limited by induction of hypercalcemia. Vitamin D₂ and analogues are thought to be generally less toxic than the respective vitamin D₃compounds. This article reviews the recent development of two 125D2 analogues (doxercalciferol and paricalcitol) showed good clinical effect in organic syntheses, and new research in the design and syntheses of the structural modifications in the side chain, 19-nor, C3-substituted in A ring, and nonadeuterated isotope labeling 125D2 analogues, and the relation between the structure and the biological activities, aimed at guiding significance to the syntheses and clinical development of new selective biological vitamin D₂ analogues. 查看全文查看/发表评论下载PDF阅读器 相关附件：版权转让声明书相关参考文献 -->