915774-28-6Relevant articles and documents
Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Thakur, Vinay V.,Kim, Joseph T.,Hamilton, Andrew D.,Bailey, Christopher M.,Domaoal, Robert A.,Wang, Ligong,Anderson, Karen S.,Jorgensen, William L.
, p. 5664 - 5667 (2006)
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.