Author/Authors :
Vinay V. Thakur، نويسنده , , Joseph T. Kim، نويسنده , , Andrew D. Hamilton، نويسنده , , Christopher M. Bailey، نويسنده , , Robert A. Domaoal، نويسنده , , Ligong Wang، نويسنده , , Karen S. Anderson، نويسنده , , William L. Jorgensen، نويسنده ,
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.
