Applied Biological Chemistry

The Korean Society for Applied Biological Chemistry (한국응용생명화학회)
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Biological activity of quinoline derivatives as inhibitors of NADH-ubiquinone oxidoreductase in the respiratory chain

NADH-ubiquinone oxidoreductase 저해제인 quinoline 유도체들의 생리활성

  • Chung, Kun-Hoe (Organic Div. I, Korea Research Institute of Chemical Technology (KRICT)) ;
  • Cho, Kwang-Yun (Organic Div. I, Korea Research Institute of Chemical Technology (KRICT)) ;
  • Takahashi, Nobutaka (Department of Agricultural Chemistry, The University Tokyo) ;
  • Yoshida, Shigeo (Chemical Regulation of Biomechanisms Lab., The Institute of Chemical and Physical Research)
  • Published : 1991.03.30
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Abstract

New quinoline compounds were designed, synthesized, and examined with submitochondria. Most compounds showed high activity against NADH-ubiquinone oxidoreductase. Inhibition activity was mainly affected by the length of the lipophilic part, regardless of bulkiness or location of a phenyl group in the side chain. The $\beta-methyl$ group was demons)rated to be the optimal functionality on the nuclei of the quinoline derivatives so 4hat either deletion or insertion of a methylene on the group eliminated its activity.

Menaquinone과 비슷한 구조로써 새로운 quinoline 화합물들은 design하고 합성하여 submitochondria를 이용하여 생리활성을 검정하였다. NADH-ubiquinone oxidoreductase를 저해하는 생리활성은 주로 친유성 부분인 측쇄의 길이에 의존되었다. Quinoline핵의 3위치는 methyl group일 때가 가장 높은 저해활성을 나타냈다.

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