Synthesis and Antiplatelet, Antiinflammatory and Antiallergic Activities of 2,3-Disubstituted 1,4-Naphthoquinones.
作者:Jin-Cherng LIEN、Li-Jiau HUANG、Jih-Pyang WANG、Che-Ming TENG、Kuo-Hsiung LEE、Sheng-Chu KUO
DOI:10.1248/cpb.44.1181
日期:——
Modification of 2-acetamido-3-chloro-1,4-naphthoquinone, which has potent antiplatelet, antiallergic and antiinflammatory activities, led to a series of 2,3-disubstituted 1,4-naphthoquinones. Some of these compounds showed significant antiplatelet, antiallergic and antiinflammatory activities. Among them, 2-methoxy-3-chloro-1,4-naphthoquinone (15) and 2-ethoxy-3-chloro-1,4-naphthoquinone (17) exhibited
具有有效的抗血小板,抗过敏和抗炎活性的2-乙酰氨基-3-氯-1,4-萘醌的修饰导致了一系列的2,3-二取代的1,4-萘醌。这些化合物中的一些显示出显着的抗血小板,抗过敏和抗炎活性。其中,2-甲氧基-3-氯-1,4-萘醌(15)和2-乙氧基-3-氯-1,4-萘醌(17)对嗜中性粒细胞和肥大细胞脱粒表现出有效的抑制作用。2-甲氧基-1,4-萘醌(20)和2-乙氧基-1,4-萘醌(21)对中性粒细胞超氧化物的形成具有有效的抑制作用。因此,选择了这四种化合物进行进一步评估。