2. Academic Validation
  3. Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase

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.
Vinay V Thakur 1,  Joseph T Kim,  Andrew D Hamilton,  Christopher M Bailey,  Robert A Domaoal,  Ligong Wang,  Karen S Anderson,  William L Jorgensen
Affiliations

Affiliation

  • 1 Department of Chemistry, Yale University, New Haven, CT 06520-8107, USA.
PMID: 16931015 DOI: 10.1016/j.bmcl.2006.08.037
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.

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