Synthesis and Biological Activity of a 1α, 25-Dihydroxyvitamin D2 Analog Bearing an Amide Group in the Side-Chain

Katsuhiro KONNO; Katsuji OJIMA; Takaaki HAYASHI; Miyuki TANABE; Hiroaki TAKAYAMA

doi:10.1248/cpb.45.185

Synthesis and Biological Activity of a 1α, 25-Dihydroxyvitamin D₂ Analog Bearing an Amide Group in the Side-Chain

Katsuhiro KONNO, Katsuji OJIMA, Takaaki HAYASHI, Miyuki TANABE, Hiroaki TAKAYAMA

著者情報

キーワード: 1α, 25-dihydroxyvitamin D₂ analog, isosteric replacement, synthesis, vitamin D receptor binding

ジャーナルフリー

1997 年 45 巻 1 号 p. 185-188

DOI https://doi.org/10.1248/cpb.45.185

詳細

抄録

Synthesis of a 1α, 25-dihydroxyvitamin D₂ analog (3), in which the double bond in the side-chain in replaced by an amide group, is described. Condensation of a carboxylic acid (8) with an amine (6) gave an amide (9), which in turn led to 3 via several steps. The analog (3) could not bind to the chick cytosol vitamin D receptor, which indicated the importance of the hydrophobic interaction of the C(22)-C(23) double bond in 1α, 25-dihydroxyvitamin D₂ (2) with the vitamin D receptor.

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