5-リポキシゲナーゼ阻害剤の研究p-ヒドロキシアリールアルケニルベンゾアゾール類の合成と構造活性相関

概要

論文の詳細を見る
In a previous paper we reported that 2-(p-hydroxyarylbutadienyl) benzoxazoles are highly potent 5-lipoxygenase inhibitors. We synthesized their ethenyl homologues and benzothiazole derivatives, and evaluated their 5-lipoxygenase inhibitory activity in vitro with cell-free rat basophilic leukemia (RBL-1). In most cases the replacement of benzoxazolyl with benzothiazolyl resulted in an enhancement of the activity. All compounds with butadienyl spacers tested herein exhibited strong inhibitory activities. While most of the ethenyl homologues showed weaker activities than their corresponding butadienyl homologues, some ethenyl compounds in the benzothiazole derivatives were found to be as potent as their corresponding butadienyl homologues. The inhibitory activity was also affected by the variation in the p-hydroxyaryl functionality.
社団法人日本薬学会の論文
1997-09-25