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Synthesis, Antiplasmodial Activity And Mechanistic Studies Of Pyrimidine-5-carbonitrile And Quinoline Hybrids.

H. Kaur, J. Balzarini, Carmen de Kock, P. Smith, K. Chibale, K. Singh
Published 2015 · Chemistry, Medicine

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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.
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