NADH-ubiquinone oxidoreductase 저해제인 quinoline 유도체들의 생리활성

Biological activity of quinoline derivatives as inhibitors of NADH-ubiquinone oxidoreductase in the respiratory chain

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.

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.