Design and Synthesis of Biologically Active Substituted Indole Compounds Using Enamide-ene Metathesis

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  • Arisawa Mitsuhiro
    Graduate School of Pharmaceutical Sciences, Hokkaido Univerisity Graduate School of Pharmaceutical Sciences and Graduated School of Pharmaceutical Sciences, Osaka University
  • Nishida Atsushi
    Graduate School of Pharmaceutical Sciences, Chiba Univerisity
  • Shuto Satoshi
    Graduate School of Pharmaceutical Sciences, Hokkaido Univerisity

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  • 芳香族エナミドメタセシス反応の開発：生物活性多置換インドール化合物の設計·合成·機能評価
  • 芳香族エナミドメタセシス反応の開発 : 生物活性多置換インドール化合物の設計・合成・機能評価
  • ホウコウゾク エナミドメタセシス ハンノウ ノ カイハツ : セイブツ カッセイ タチカン インドール カゴウブツ ノ セッケイ ・ ゴウセイ ・ キノウ ヒョウカ

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Abstract

We have established aromatic enamide-ene metathesis to give highly substituted indole derivatives. This is a new method for the preparation of chiral 2-trans-cyclopropyl indoles, which successfully led to our H4 antagonist candidates. Based on this findings, we also designed and synthesized conformationally restricted analogues and regioisomers of the nonsteroidal anti-inflammatory drug indomethacin. Evaluation of the inhibitory effects of these compounds on COX, P-glycoprotein, and multidrug-resistance indicated that NSAIDS modulation of multidrug resistant P-glycoprotein and multidrug-resistant protein-1 is not associated with COX-1 and COX-2 inhibitory activities.

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