- 2,6-Di(arylamino)-3-fluoropyridine Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors
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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.
- Sergeyev, Sergey,Yadav, Ashok Kumar,Franck, Philippe,Michiels, Johan,Lewi, Paul,Heeres, Jan,Vanham, Guido,Ari?n, Kevin K.,Vande Velde, Christophe M. L.,De Winter, Hans,Maes, Bert U. W.
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p. 1854 - 1868
(2016/03/22)
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- NOVEL ANTI-HIV COMPOUNDS
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The present invention relates to the field of HIV-1 infections, and in particular provides novel compounds containing fluorine on the Central ring. The compounds according to this invention are very suitable for the prevention and/or treatment of HIV-1 infection and in particular show higher activity against NNRTI-resistant strains of HIV-1.
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