| Literature DB >> 21507639 |
Joe B Perales1, Jennifer Freeman, Cyrus J Bacchi, Tana Bowling, Robert Don, Eric Gaukel, Luke Mercer, Joseph A Moore, Bakela Nare, Tien M Nguyen, Robert A Noe, Ryan Randolph, Cindy Rewerts, Stephen A Wring, Nigel Yarlett, Robert T Jacobs.
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.Entities:
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Year: 2011 PMID： 21507639 DOI： 10.1016/j.bmcl.2011.03.097
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823