Department of Chemistry, Guru Nanak Dev University, Amritsar, 143005, India.
Department of Medicine, University of California, San Francisco, CA, USA.
Eur J Med Chem. 2017 Sep 29;138:993-1001. doi: 10.1016/j.ejmech.2017.07.041. Epub 2017 Jul 22.
1H-1,2,3-triazole linked 4-aminoquinoline-chalcone/-N-acetylpyrazoline conjugates were synthesized and evaluated against cultured chloroquine (CQ) resistant strain. Antiplasmodial activities of the synthesized conjugates revealed dependence of activity on the length of the alkyl chain as well as on the presence of methoxy substituents on ring A/ring B of the chalcone. The most potent and non-cytotoxic conjugate showed comparable antiplasmodial activity with that of CQ, with an IC value of 53.7 nM.
1H-1,2,3-三唑连接的 4-氨基喹啉查尔酮/-N-乙酰吡唑啉缀合物被合成并针对培养的氯喹（CQ）抗性株进行了评估。合成缀合物的抗疟活性依赖于烷基链的长度以及查尔酮的 A/环 B 上甲氧基取代基的存在。最有效且非细胞毒性的缀合物显示出与 CQ 相当的抗疟活性，IC 值为 53.7 nM。
