嘧啶-5-腈与喹啉杂合物的合成、抗疟活性及作用机制研究
Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids.
作者信息
Kaur Hardeep, Balzarini Jan, de Kock Carmen, Smith Peter J, Chibale Kelly, Singh Kamaljit
机构信息
Department of Chemistry, UGC-Centre of Advance Study-II, Guru Nanak Dev University, Amritsar 143005, India.
Rega Institute for Medical Research, KU Leuven, 10 Minderbroedersstraat, B-3000 Leuven, Belgium.
出版信息
Eur J Med Chem. 2015 Aug 28;101:52-62. doi: 10.1016/j.ejmech.2015.06.024. Epub 2015 Jun 12.
A series of hybrids comprising of 5-cyanopyrimidine and quinoline moiety were synthesized and tested for in vitro antiplasmodial activity against NF54 and Dd2 strains of Plasmodium falciparum. Hybrid bearing m-nitrophenyl substituent at C-4 of pyrimidine displayed the highest antiplasmodial activity [IC50 = 56 nM] against the CQ(R) (Dd2) strain, which is four-fold greater than CQ.
合成了一系列由5-氰基嘧啶和喹啉部分组成的杂化物，并对其针对恶性疟原虫NF54和Dd2菌株的体外抗疟活性进行了测试。在嘧啶的C-4位带有间硝基苯基取代基的杂化物对CQ（R）（Dd2）菌株表现出最高的抗疟活性[IC50 = 56 nM]，比氯喹高四倍。
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