Synthesis and anti-HIV activity evaluation of 1-[(alkenyl or alkynyl or alkyloxy)methyl]-5-alkyl-6-(1-naphthoyl)-2,4-pyrimidinediones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

The synthesis and anti-HIV activity evaluation of a new series of 2,4-pyrimidinediones bearing a 6-(1-naphthoyl) group are described. In general, it was found that most of the title compounds showed good activities against human immunodeficiency virus type-1 (HIV-1). In particular, compound 26 displayed the most potent anti-HIV-1 activity (IC50 = 0.11 ± 0.05 μM), inhibiting HIV-1 replication in MT-4 cells more effectively than HEPT (by 45-fold) and DDI (by 50-fold).

Graphical abstractThe synthesis and anti-HIV activities of a new series of 2,4-pyrimidinediones bearing a 6-(1-naphthoyl) group are reported. It was found that most of the title compounds showed good anti-HIV-1 activity.Figure optionsDownload full-size imageDownload as PowerPoint slide