Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV.

@article{Nugent1998PyrimidineTA,
  title={Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV.},
  author={Richard A Nugent and Stephen T Schlachter and Mary J Murphy and Gary J Cleek and Toni J Poel and Donn G. Wishka and David R Graber and Yasuo Yagi and B J Keiser and Robert A. Olmsted and Laurice A Kopta and Steven M Swaney and Susan M Poppe and Joel Morris and W. Gary Tarpley and Richard C Thomas},
  journal={Journal of medicinal chemistry},
  year={1998},
  volume={41 20},
  pages={3793-803}
}
A series of pyrimidine thioethers was synthesized and evaluated for inhibitory properties against wild-type HIV-1 reverse transcriptase (RT) and an RT carrying the resistance-conferring mutation P236L. Modifications of both the pyrimidine and the functionality attached through the thioether yielded several analogues, which demonstrated activity against both enzyme types, with IC50 values as low as 190 nM against wild-type and 66 nM against P236L RT. Evaluation of a select number of pyrimidine… CONTINUE READING