Synthetic studies of vitamin D analogs. XXIV. Synthesis of active vitamin D3 analogs substituted at the 2 beta-position and their preventive effects on bone mineral loss in ovariectomized rats.
Synthetic studies of vitamin D analogs. XXIV. Synthesis of active vitamin D3 analogs substituted at the 2 beta-position and their preventive effects on bone mineral loss in ovariectomized rats.
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维生素 D 类似物的合成研究。
DOI：
10.1248/cpb.45.1626
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发表时间：
1997
影响因子：
1.7
通讯作者：
N. Kubodera
中科院分区：
文献类型：
--
作者：
Y. Ono;H. Watanabe;A. Shiraishi;S. Takeda;Y. Higuchi;K. Sato;N. Tsugawa;T. Okano;T. Kobayashi;N. Kubodera
与1 α，25-二羟基-2 β-（3-羟基丙氧基）维生素D3（艾德-71）（4）相关的类似物，在1 α，25-二羟基维生素D3（1）的2 β-位上带有取代基的维生素D3的氧杂型和卡巴型类似物，是从α-环氧化物（6和13）合成的。三种类似物，艾德-71（4）和两种卡巴型类似物（16和26），对骨质疏松症模型大鼠的骨矿物质丢失显示出有效的预防作用。结论艾德-71（4）是一种优化的类似物，是治疗骨质疏松症的有希望的候选物。
Analogs related to 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitamin D3 (ED-71) (4), oxa-type and carba-type analogs of vitamin D3 bearing substituents at the 2 beta-position of 1 alpha,25-dihydroxyvitamin D3 (1), were synthesized from the alpha-epoxides (6 and 13). Three analogs, ED-71 (4) and two carba-type analogs (16 and 26), showed potent preventive effects on bone mineral loss in pre-osteoporosis model rats. ED-71 (4) was concluded to be an optimized analog and a promising candidate for the treatment of osteoporosis.