9 血小板活性化因子(PAF)構造に基づく合成研究 : コンホメーション制限モデルの展開によるアゴニスト及びアンタゴニストの分子設計(口頭発表の部)

概要

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Since the identification of platelet activating factor (PAF) as alkylacetylglycerophosphocholine, PAF have attracted a great deal of attention in the field of biochemistry, and are now recognized as important chemical mediators for the development of potent new therapeutic agents. We established an efficient route to PAF from tartaric acid. Then, molecular design were carried out in such a way as to lock or localize the conformation of PAF by introducing methyl group in the glycerine moiety, bringing a selective agonist, 1S-Me-PAF. The result also indicates that chemical modification is interesting to start with C-I of the glycerine backbone, and bringing a strong agonist, a cis-disubstituted tetrahydrofuran derivative, partially confined in a ring. The unstable conformation of the agonist further suggests to look for 7-oxabicyclo[2.2.1]heptane derivatives. They turns out to be strong antagonists. The conformationally restricted model approach has opened up a new avenue to the antagonists for PAF.
天然有機化合物討論会の論文
1989-09-17