title: Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.
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.
authors.affiliation: Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 250 Longwood Ave., SGM 628, Boston, MA 02115, USA.
authors.forename: Xianming
authors.initials: X
authors.lastname: Deng
authors.forename: Advait
authors.initials: A
authors.lastname: Nagle
authors.forename: Tao
authors.initials: T
authors.lastname: Wu
authors.forename: Tomoyo
authors.initials: T
authors.lastname: Sakata
authors.forename: Kerstin
authors.initials: K
authors.lastname: Henson
authors.forename: Zhong
authors.initials: Z
authors.lastname: Chen
authors.forename: Kelli
authors.initials: K
authors.lastname: Kuhen
authors.forename: David
authors.initials: D
authors.lastname: Plouffe
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Winzeler
authors.forename: Francisco
authors.initials: F
authors.lastname: Adrian
authors.forename: Tove
authors.initials: T
authors.lastname: Tuntland
authors.forename: Jonathan
authors.initials: J
authors.lastname: Chang
authors.forename: Susan
authors.initials: S
authors.lastname: Simerson
authors.forename: Steven
authors.initials: S
authors.lastname: Howard
authors.forename: Jared
authors.initials: J
authors.lastname: Ek
authors.forename: John
authors.initials: J
authors.lastname: Isbell
authors.forename: David C
authors.initials: DC
authors.lastname: Tully
authors.forename: Arnab K
authors.initials: AK
authors.lastname: Chatterjee
authors.forename: Nathanael S
authors.initials: NS
authors.lastname: Gray
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D055808:Drug Discovery; D010963:Plasmodium falciparum / Q000187:drug effects*; D011743:Pyrimidines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011743:Pyrimidines