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. 2010 Jul 15;20(14):4027-31.
doi: 10.1016/j.bmcl.2010.05.095. Epub 2010 Jun 2.

Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials

Xianming Deng  1 , Advait Nagle, Tao Wu, Tomoyo Sakata, Kerstin Henson, Zhong Chen, Kelli Kuhen, David Plouffe, Elizabeth Winzeler, Francisco Adrian, Tove Tuntland, Jonathan Chang, Susan Simerson, Steven Howard, Jared Ek, John Isbell, David C Tully, Arnab K Chatterjee, Nathanael S Gray
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Free article

Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials

Xianming Deng et al. Bioorg Med Chem Lett. .
Free article

Abstract

A novel family of 1H-imidazol-2-yl-pyrimidine-4,6-diamines has been identified with potent activity against the erythrocyte-stage of Plasmodium falciparum (Pf), the most common causative agent of malaria. A systematic SAR study resulted in the identification of compound 40 which exhibits good potency against both wild-type and drug resistant parasites and exhibits good in vivo pharmacokinetic properties.

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