Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors

Molecules. 2008 Oct 1;13(10):2442-61. doi: 10.3390/molecules13102442.


HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Azides
  • Catalytic Domain
  • Computer Simulation
  • Drug Design
  • HIV Integrase Inhibitors / chemistry*
  • HIV Integrase Inhibitors / pharmacology
  • Humans
  • Malonates / chemical synthesis*
  • Malonates / chemistry
  • Malonates / pharmacology*
  • Protein Binding
  • Structure-Activity Relationship


  • Amides
  • Anti-HIV Agents
  • Azides
  • HIV Integrase Inhibitors
  • Malonates
  • malonic acid