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

作者：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; I**ell John; Tully David C; Chatterjee Arnab K; Gray Nathanael S^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(14): 4027-4031.

DOI：10.1016/j.bmcl.2010.05.095

• 1H-Imidazol-2-yl-pyrimidine-4,6-diamines
• Antimalarial

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.

• 出版日期2010-7-15