Molecules (Oct 2008)

Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors

  • Nouri Neamati,
  • Nicolino Pala,
  • Alessia Cosseddu,
  • Alessandro Dessì,
  • Roberto Dallocchio,
  • Maria Paola Delussu,
  • Ugo Azzena,
  • Mario Sechi

Journal volume & issue
Vol. 13, no. 10
pp. 2442 – 2461

Abstract

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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.

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