- Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.
Bioorganic & medicinal chemistry letters (2010-07-09)
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
PMID20610151
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.
MATERIALS