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

NADH-ubiquinone oxidoreductase 저해제인 quinoline 유도체들의 생리활성

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.