Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S. A. S. Nagar, Punjab 160 062, India.
Eur J Med Chem. 2012 Jun;52:230-41. doi: 10.1016/j.ejmech.2012.03.019. Epub 2012 Mar 21.
Three new series of 8-aminoquinolines with modifications in the side-chain by conjugation with amino acids, dipeptides and pseudodipeptides have been synthesized. The synthesized compounds were tested for in vitro antimalarial activity against chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains, in vitro cytotoxicity in mammalian kidney cells (Vero), in vitro antileishmanial activity against Leishmania donovani, in vitro antimicrobial activity and in vitro inhibition of β-haematin formation. The promising compounds were also evaluated for in vivo blood-schizontocidal antimalarial activity against Plasmodium berghei infected mice. The analogues 55 and 101 produced highest antimalarial activities, in vitro. Analogues 52 and 59 exhibited promising antileishmanial and broad spectrum of antifungal activities, respectively.
已经合成了三个新系列的 8-氨基喹啉，这些化合物通过与氨基酸、二肽和假二肽的侧链连接进行修饰。合成的化合物进行了以下测试：在体外对氯喹敏感和氯喹耐药的恶性疟原虫菌株的抗疟活性、在哺乳动物肾细胞（Vero）中的体外细胞毒性、对利什曼原虫的体外抗利什曼原虫活性、体外抗菌活性和体外抑制β-血红素形成。有前途的化合物还针对感染伯氏疟原虫的小鼠进行了体内血裂殖体杀灭抗疟活性评估。类似物 55 和 101 在体外产生了最高的抗疟活性。类似物 52 和 59 分别表现出有希望的抗利什曼原虫活性和广谱抗真菌活性。
