Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5664-7. doi: 10.1016/j.bmcl.2006.08.037. Epub 2006 Aug 22.

Abstract

Non-nucleoside inhibitors of HIV-1 reverse transcriptase are being pursued through synthesis and assaying for anti-viral activity. Following computational analyses, the focus has been on the motif Het-NH-Ph-U, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Previous investigations with Het=2-thiazoyl and 2-pyrimidinyl are extended here to triazinyl derivatives. The result is several NNRTIs in the 2-20 nM range with negligible cytotoxicity and auspicious predicted pharmacological properties.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amines / chemistry
  • Amines / pharmacology*
  • HIV Reverse Transcriptase / antagonists & inhibitors*
  • HIV-1 / enzymology*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Triazines / chemistry
  • Triazines / pharmacology*

Substances

  • Amines
  • Pyrimidines
  • Triazines
  • HIV Reverse Transcriptase