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Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.
Deng, Xianming; Nagle, Advait; Wu, Tao; Sakata, Tomoyo; Henson, Kerstin; Chen, Zhong; Kuhen, Kelli; Plouffe, David; Winzeler, Elizabeth; Adrian, Francisco; Tuntland, Tove; Chang, Jonathan; Simerson, Susan; Howard, Steven; Ek, Jared; Isbell, John; Tully, David C; Chatterjee, Arnab K; Gray, Nathanael S.
Affiliation
  • Deng X; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Ave., SGM 628, Boston, MA 02115, USA.
Bioorg Med Chem Lett ; 20(14): 4027-31, 2010 Jul 15.
Article in En | MEDLINE | ID: mdl-20610151
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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Plasmodium falciparum / Pyrimidines / Antimalarials Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Type: Article Affiliation country: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Plasmodium falciparum / Pyrimidines / Antimalarials Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Type: Article Affiliation country: United States