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Evaluation of novel N'-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors.

Omobolanle Janet JesumorotiFaridoon FaridoonDumisani MnkandhlaMichelle IsaacsHeinrich C HoppeRosalyn Klein
Published in: MedChemComm (2018)
In an attempt to identify potential new agents that are active against HIV-1 IN, a series of novel coumarin-3-carbohydrazide derivatives were designed and synthesised. The toxicity profiles of these compounds showed that they were non-toxic to human cells and they exhibited promising anti-HIV-1 IN activities with IC50 values in nM range. Also, an accompanying molecular modeling study showed that the compounds bind to the active pocket of the enzyme.
Keyphrases
  • antiretroviral therapy
  • hiv positive
  • hiv testing
  • hiv infected
  • human immunodeficiency virus
  • hepatitis c virus
  • hiv aids
  • men who have sex with men
  • south africa
  • photodynamic therapy