Synthesis of 6-arylvinyl analogues of the HIV drugs SJ-3366 and Emivirine.

  title={Synthesis of 6-arylvinyl analogues of the HIV drugs SJ-3366 and Emivirine.},
  author={M. Wamberg and E. Pedersen and N. R. El‐Brollosy and C. Nielsen},
  journal={Bioorganic \& medicinal chemistry},
  volume={12 5},
This paper reports the synthesis and the antiviral activities of a series of 6-arylvinyl substituted analogues of SJ-3366, a highly potent agent against HIV. The objective was to investigate whether substitution of the 6-arylketone with a 6-arylvinyl group could lead to an improved antiviral activity against HIV-1. The most active compounds 1-ethoxymethyl, 1-(2-propynyloxymethyl), and 1-(2-methyl-3-phenylallyloxymethyl) substituted 6-[1-(3,5-dimethylphenyl)vinyl]-5-ethyl-1H-pyrimidine-2,4-dione… Expand
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