Title
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2,6-Di(arylamino)-3-fluoropyridine derivatives as HIV non-nucleoside reverse transcriptase inhibitors
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Author
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Abstract
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New non-nucleoside reverse transcriptase inhibitors (NNRTI), which are similar in structure to earlier described di(arylamino)pyrimidines but featuring a 2,6-di(arylamino)-3-fluoropyridine , 2,4-di(arylamino)-5-fluoropyrimidine or 1,3-di(arylamino)-4-fluorobenzene moiety instead of a 2,4-disubstituted pyrimidine moiety, are reported. The short and practical synthesis of novel NNRTI relies on two sequential Pd-catalyzed aminations as the key steps. It is demonstrated through direct comparison with reference compounds, that the presence of a fluorine atom increases the in vitro anti-HIV activity, both against the wild type virus and drug-resistant mutant strains. |
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Language
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English
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Source (journal)
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Journal of medicinal chemistry. - Washington, D.C., 1963, currens
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Publication
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Washington, D.C.
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2016
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ISSN
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0022-2623
[print]
1520-4804
[online]
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DOI
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10.1021/ACS.JMEDCHEM.5B01336
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Volume/pages
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59
:5
(2016)
, p. 1854-1868
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ISI
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000372043400014
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Pubmed ID
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26785139
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Full text (Publisher's DOI)
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Full text (open access)
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