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. 2011 May 15;21(10):2816-9.
doi: 10.1016/j.bmcl.2011.03.097. Epub 2011 Apr 1.

SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei

Joe B Perales  1 , Jennifer Freeman, Cyrus J Bacchi, Tana Bowling, Robert Don, Eric Gaukel, Luke Mercer, Joseph A Moore 3rd, Bakela Nare, Tien M Nguyen, Robert A Noe, Ryan Randolph, Cindy Rewerts, Stephen A Wring, Nigel Yarlett, Robert T Jacobs
Affiliations

SAR of 2-amino and 2,4-diamino pyrimidines with in vivo efficacy against Trypanosoma brucei

Joe B Perales et al. Bioorg Med Chem Lett. .

Abstract

A series of 2,4-diaminopyrimidines was investigated and compounds were found to have in vivo efficacy against Trypanosoma brucei in an acute mouse model. However, in vitro permeability data suggested the 2,4-diaminopyrimidenes would have poor permeability through the blood brain barrier. Consequently a series of 4-desamino analogs were synthesized and found to have improved in vitro permeability.

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