Effect of substitution on novel tricyclic HIV-1 integrase inhibitors.

  title={Effect of substitution on novel tricyclic HIV-1 integrase inhibitors.},
  author={Maria Fardis and Haolun Jin and Salman Y Jabri and Ruby Z Cai and Michael R Mish and Manuel Tsiang and Choung U. Kim},
  journal={Bioorganic & medicinal chemistry letters},
  volume={16 15},
A series of novel tricyclic inhibitors of HIV-1 integrase enzyme was prepared. The effect of substitution at C-6 of the 9-hydroxy-6,7-dihydropyrrolo[3,4-g]quinolin-8-one compounds was studied in vitro. Inhibitors with small side chains at C-6 were generally well tolerated by the enzyme, and the physicochemical properties of the inhibitors were improved by substitution of a small alkyl group at this position. A second series of analogs bearing a sulfamate at the C-5 position with various C-6… CONTINUE READING

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