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

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 investig...

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Detalles Bibliográficos
Autores principales: Sechi, Mario, Azzena, Ugo, Delussu, Maria Paola, Dallocchio, Roberto, Dessì, Alessandro, Cosseddu, Alessia, Pala, Nicolino, Neamati, Nouri
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2008
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6245433/
https://www.ncbi.nlm.nih.gov/pubmed/18830166
http://dx.doi.org/10.3390/molecules13102442
Descripción
Sumario: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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