2. Academic Validation
  3. 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

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

  • Eur J Med Chem. 2007 Feb;42(2):198-204. doi: 10.1016/j.ejmech.2006.09.018.
Lei Ji 1,  Fen-Er Chen,  Bin Xie,  Erik De Clercq,  Jan Balzarini,  Christophe Pannecouque
Affiliations

Affiliation

  • 1 Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
PMID: 17095124 DOI: 10.1016/j.ejmech.2006.09.018
Abstract

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 (IC(50)=0.11+/-0.05 microM), inhibiting HIV-1 replication in MT-4 cells more effectively than HEPT (by 45-fold) and DDI (by 50-fold).

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