Gut Jiri, Rosenthal Philip J, Kumar Vipan
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
Department of Medicine, University of California, San Francisco, CA, USA.
Eur J Med Chem. 2014 Sep 12;84:566-73. doi: 10.1016/j.ejmech.2014.07.064. Epub 2014 Jul 21.
A series of β-amino alcohol tethered 4-aminoquinoline-isatin conjugates were synthesized with the aim of probing their antimalarial structure activity relationship. Two of the most active conjugates (11b and 11f) exhibited antimalarial efficacy comparable to that of chloroquine, with IC50 values of 11.8 and 13.5 nM, respectively against chloroquine resistant W2 strain of Plasmodium falciparum and are devoid of any cytotoxicity.
合成了一系列β-氨基醇连接的4-氨基喹啉-异吲哚酮缀合物，目的是探究它们的抗疟构效关系。两种活性最高的缀合物（11b和11f）表现出与氯喹相当的抗疟效力，对恶性疟原虫氯喹抗性W2株的IC50值分别为11.8和13.5 nM，且无任何细胞毒性。
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