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

Authors :
Deng X
Nagle A
Wu T
Sakata T
Henson K
Chen Z
Kuhen K
Plouffe D
Winzeler E
Adrian F
Tuntland T
Chang J
Simerson S
Howard S
Ek J
Isbell J
Tully DC
Chatterjee AK
Gray NS
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Jul 15; Vol. 20 (14), pp. 4027-31. Date of Electronic Publication: 2010 Jun 02.
Publication Year :
2010

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.<br /> (2010 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
20
Issue :
14
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
20610151
Full Text :
https://doi.org/10.1016/j.bmcl.2010.05.095