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Title
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From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds
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Author
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Abstract
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| The presence of a structural recognition motif for the nucleoside P2 transporter in a library of pyrimidine and triazine non-nucleoside HIV-1 reverse transcriptase inhibitors, prompted for the evaluation of antitrypanosomal activity. It was demonstrated that the structureactivity relationship for anti-HIV and antitrypanosomal activity was different. Optimization in the diaryl triazine series led to 6-(mesityloxy)-N2-phenyl-1,3,5-triazine-2,4-diamine (69), a compound with potent in vitro and moderate in vivo antitrypanosomal activity. |
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Language
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English
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Source (journal)
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Bioorganic and medicinal chemistry. - Oxford
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Publication
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Oxford
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2014
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ISSN
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0968-0896
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DOI
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10.1016/J.BMC.2014.08.005
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Volume/pages
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22
:19
(2014)
, p. 5241-5248
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ISI
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000341883700010
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Pubmed ID
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25199582
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Full text (Publisher's DOI)
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