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Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials |
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| Authors: | Xianming Deng 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 |
| Institution: | 1. Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Ave., SGM 628, Boston, MA 02115, USA;2. Department of Cancer Biology, Dana-Farber Cancer Institute, 250 Longwood Ave., SGM 628, Boston, MA 02115, USA;3. Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Drive, San Diego, CA 92121, USA |
| 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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