Sunduru Naresh, Sharma Moni, Srivastava Kumkum, Rajakumar S, Puri S K, Saxena J K, Chauhan Prem M S
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Bioorg Med Chem. 2009 Sep 1;17(17):6451-62. doi: 10.1016/j.bmc.2009.05.075. Epub 2009 Jun 6.
Frequency of malaria and its resistance to chemotherapeutic options are emerging rapidly. To counter this problem, a series of 4-aminoquinolines having oxalamide and triazine functionalities in the side chain were synthesized and screened for their antimalarial activities. Triazine derivative 48 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro assay with an IC(50) of 5.23 ng/mL and oxalamide derivative 13 showed an in vivo suppression of 70.45% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.
疟疾的发病率及其对化疗药物的耐药性正在迅速上升。为应对这一问题,合成了一系列侧链带有草酰胺和三嗪官能团的4-氨基喹啉,并对其抗疟活性进行了筛选。在体外试验中,三嗪衍生物48对恶性疟原虫的氯喹敏感株3D7表现出最强活性,IC(50)为5.23 ng/mL;草酰胺衍生物13在第4天对约氏疟原虫的氯喹耐药株N-67的体内抑制率为70.45%。