嘧啶-氯喹啉杂合体的合成与抗疟原虫活性。
Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity.
机构信息
Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India.
Department of Chemistry, South African Medical Research Council Drug Discovery and Development Research Unit, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa.
出版信息
Eur J Med Chem. 2018 Mar 25;148:39-53. doi: 10.1016/j.ejmech.2018.02.021. Epub 2018 Feb 9.
Triazole tethered 7-chloroquinoline-pyrimidine-5-carboxylate hybrids were synthesized and evaluated for antiplasmodial activity against chloroquine sensitive (CQ) NF54 strain of Plasmodium falciparum. The most active hybrids of the series were further screened against the chloroquine resistant (CQ) Dd2 strain of the parasite and for in vitro cytotoxicity against mammalian Vero cell lines. Further, their physico-chemical properties, binding studies with hemin (monomeric &μ-oxo dimeric) and DNA [pUC-18, calf thymus (CT)] led us to plausible proposed binding mode of the most active member of the present series.
三氮唑连接的 7-氯喹啉-嘧啶-5-羧酸杂合体被合成并评估了对氯喹敏感（CQ）恶性疟原虫 NF54 株的抗疟原虫活性。该系列中最活跃的杂种进一步针对寄生虫的氯喹耐药（CQ）Dd2 株进行了筛选，并对哺乳动物 Vero 细胞系进行了体外细胞毒性筛选。此外，它们的物理化学性质、与血红素（单体和μ-氧二聚体）和 DNA [pUC-18、小牛胸腺（CT）]的结合研究使我们能够提出本系列中最活跃成员的可能结合模式。
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