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Difluoromethylbenzoxazole Pyrimidine Thioether Derivatives: A Novel Class of Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

  • Jeremie Boyer
  • Eric Arnoult
  • Maurice Medebielle
  • Jerome Guillemont
  • Johan Unge
  • Dirk Jochmans
Publiceringsår: 2011
Språk: Engelska
Sidor: 7974-7985
Publikation/Tidskrift/Serie: Journal of Medicinal Chemistry
Volym: 54
Nummer: 23
Dokumenttyp: Artikel
Förlag: American Chemical Society


This paper reports the synthesis and antiviral properties of new difluoromethylbenzoxazole (DFMB) pyrimidine thioether derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. By use of a combination of structural biology study and traditional medicinal chemistry, several members of this novel class were synthesized using a single electron transfer chain process (radical nucleophilic substitution, Si) and were found to be potent against wild-type HIV-1 reverse transcriptase, with low cytotoxicity but with moderate activity against drug-resistant strains. The most promising compound 2,4 showed a significant EC(50) value close to 6.4 nM against HIV-1 IIIB, a moderate EC(50) value close to 54 mu M against an NNRTI resistant double mutant (K103N + Y181C), but an excellent selectivity index >15477 (CC(50) > 100 mu M).



  • Medicinal Chemistry


  • ISSN: 0022-2623

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