新しく設計したキノン誘導体の合成と生物評価 : 5-リポキシゲナーゼ阻害剤とトロンボキサンA2受容体拮抗剤

概要

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As part of our ongoing research efforts into the synthesis and biological evaluation of quinone derivatives, we have established synthetic methodologies for preparing unique quinone compounds possessing multiprenyl groups, chemically modified multiprenyl groups, ethylenic and acetylenic bonds, and sterically hindered groups. Biological effects of the quinone derivatives on the enzymes 5-lipoxygenase and thromboxane A2 synthase, and on thromboxane A2 receptor and other spasmogenic prostanoid receptors, have been evaluated and discussed. Enzyme inhibitors and receptor antagonists involved in the arachidonic acid cascade system represent a new class of drugs that could potentially treat certain sequelae of asthma, septic shock, thrombosis, stroke, and various other human disorders. It was found that the quinone derivative 2- (12- hydroxy-dodeca-5, 10-diynyl) -3, 5, 6-trimethy1-1, 4-benzoquinone (AA-861) proved to be a potent and specific inhibitor of 5-lipoxygenase and that 7- (3, 5, 6-trimethy1-1, 4-benzoquinon-2-yl) -7-phenylheptanoic acid (AA-2414) was a non-prostanoid thromboxane A2 receptor antagonist.
社団法人有機合成化学協会の論文