New Potential Antimalarial Agents. Synthesis and Biological Activities of Original Diaza-analogs of Phenanthrene.
作者:Ange Desire YAPI、Mustofa MUSTOFA、Alexis VALENTIN、Olivier CHAVIGNON、Jean-Claude TEULADE、Michele MALLIE、Jean-Pierre CHAPAT、Yves BLACHE
DOI:10.1248/cpb.48.1886
日期:——
Several diaza-analogs of phenanthrene derived from 3-amino, 5-amino, 6-amino, 8-aminoquinolines, and 5-aminoisoquinoline were prepared to evaluate their antiplasmodial activities. All compounds showed mild to good activitiy in vitro, both on a Nigerian chloroquino-sensitive strain and on the chloroquino-resistant FcB1-Columbia and FcM29 strains. The position of the intracyclic nitrogen atom is shown
制备了几个衍生自3-氨基,5-氨基,6-氨基,6-氨基,8-氨基喹啉和5-氨基异喹啉的菲的类似物以评估其抗血浆活性。所有化合物在体外对尼日利亚对氯喹敏感的菌株以及对氯喹抗性的FcB1-Columbia和FcM29菌株均显示出轻度至良好的活性。环内氮原子的位置对活性至关重要(使用1,10-菲咯啉骨架可获得最佳结果)。关于该结构的特殊性质(通过螯合二价金属离子抑制金属蛋白酶的活性),该分子的潜在螯合位点被封闭。在这种情况下,该化合物的生物活性大大提高,