Journal of Medicinal Chemistry p. 1854 - 1868 (2016)
Update date:2022-07-29
Topics:
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.
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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