摘要
N-l-alkyl-5-halogeno-6-alkylamino uracils, which are novel l-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) analogues, were synthesized as the selective and potent non-nucleoside human immunodeficiency virus (HIV)-I reverse transcriptase inhibitors. Some of the compounds showed potent inhibitory activity against HIV-1 reverse transcriptase. For instance, compounds ld, lm and In exhibited potent anti-HIV-1 activity with the ICso values of 13.3, 11.7 and 3.15 μM, respectively, which are comparable to that of nevirapine (IC50 8.38 μM).
基金
Foundation items: National Natural Science Foundation of China (Grant No. 20672008 and 20972011).