Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.

  title={Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.},
  author={Paola Pace and Maria Emilia Di Francesco and Cristina Gardelli and Steven R. Harper and Ester Muraglia and Emanuela Nizi and Federica Orvieto and Alessia Petrocchi and Marco Poma and Michael Rowley and Rita Scarpelli and Ralph Laufer and Odalys Gonzalez Paz and Edith S. Monteagudo and Fabio Bonelli and Daria Hazuda and Kara A Stillmock and Vincenzo Summa},
  journal={Journal of medicinal chemistry},
  volume={50 9},
Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment of AIDS that has also recently been confirmed in the clinical setting. We report here on the design and synthesis of N-benzyl-5,6-dihydroxypyrimidine-4-carboxamides as a class of agents which exhibits potent inhibition of the HIV-integrase-catalyzed strand transfer process. In the current study… CONTINUE READING

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