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

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

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

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

Vinay V Thakur et al. Bioorg Med Chem Lett. .

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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