Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains
Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains
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DOI：
10.1016/j.bioorg.2016.11.010
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发表时间：
2017-02-01
影响因子：
5.1
通讯作者：
Katti, S. B.
中科院分区：
文献类型：
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作者：
Kondaparla, Srinivasarao;Soni, Awakash;Katti, S. B.
本研究合成了一类新的4-氨基喹啉类化合物，并对其体外抗恶性疟原虫（3D 7敏感株和K1抗性株）和体内抗约氏疟原虫（N-67株）进行了评价。其中，11个化合物（5，6，7，8，9，11，12，13，14，15和21）对K1株显示出比CQ强的上级抗疟活性。此外，当口服给药时，所有这些类似物在体内小鼠模型中对N-67菌株的第4天显示出100%的寄生虫血症抑制。此外，生物物理研究表明，这一系列化合物作用于血红素聚合靶点。(C)2016 Elsevier Inc. All rights reserved.
In the present study we have synthesized a new class of 4-aminoquinolines and evaluated against Plasmodium falciparum in vitro (3D7-sensitive strain & K1-resistant strain) and Plasmodium yoelii in vivo (N-67 strain). Among the series, eleven compounds (5, 6, 7, 8, 9, 11, 12, 13, 14, 15 and 21) showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogues showed 100% suppression of parasitemia on day 4 in the in vivo mouse model against N-67 strain when administered orally. Further, biophysical studies suggest that this series of compounds act on heme polymerization target. (C) 2016 Elsevier Inc. All rights reserved.