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.

Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors / Sechi, Mario; Azzena, Ugo Gavino; MARIA PAOLA, Delussu; Roberto, Dallocchio; Alessandro, Dessì; Alessia, Cosseddu; Nicolino, Pala; Nouri, Neamati. - In: MOLECULES. - ISSN 1420-3049. - 13:(2008), pp. 2442-2461. [10.3390/molecules13102442]

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

SECHI, Mario;AZZENA, Ugo Gavino;
2008-01-01

Abstract

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.
2008
Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors / Sechi, Mario; Azzena, Ugo Gavino; MARIA PAOLA, Delussu; Roberto, Dallocchio; Alessandro, Dessì; Alessia, Cosseddu; Nicolino, Pala; Nouri, Neamati. - In: MOLECULES. - ISSN 1420-3049. - 13:(2008), pp. 2442-2461. [10.3390/molecules13102442]
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11388/44741
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 40
  • ???jsp.display-item.citation.isi??? 35
social impact