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2,6-Di(arylamino)-3-fluoropyridine derivatives as HIV non-nucleoside reverse transcriptase inhibitors

Journal Contribution - Journal Article

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.
Journal: Journal of medicinal chemistry
ISSN: 0022-2623
Volume: 59
Pages: 1854 - 1868
Publication year:2016
Keywords:A1 Journal article
BOF-keylabel:yes
BOF-publication weight:6
CSS-citation score:1
Authors from:Government
Accessibility:Open