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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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
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author Sechi, Mario
Azzena, Ugo
Delussu, Maria Paola
Dallocchio, Roberto
Dessì, Alessandro
Cosseddu, Alessia
Pala, Nicolino
Neamati, Nouri
author_facet Sechi, Mario
Azzena, Ugo
Delussu, Maria Paola
Dallocchio, Roberto
Dessì, Alessandro
Cosseddu, Alessia
Pala, Nicolino
Neamati, Nouri
author_sort Sechi, Mario
collection PubMed
description 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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spelling pubmed-62454332018-11-30 Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors Sechi, Mario Azzena, Ugo Delussu, Maria Paola Dallocchio, Roberto Dessì, Alessandro Cosseddu, Alessia Pala, Nicolino Neamati, Nouri Molecules Article 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. MDPI 2008-10-01 /pmc/articles/PMC6245433/ /pubmed/18830166 http://dx.doi.org/10.3390/molecules13102442 Text en © 2008 by the authors. Licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Sechi, Mario
Azzena, Ugo
Delussu, Maria Paola
Dallocchio, Roberto
Dessì, Alessandro
Cosseddu, Alessia
Pala, Nicolino
Neamati, Nouri
Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
title Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
title_full Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
title_fullStr Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
title_full_unstemmed Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
title_short Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors
title_sort design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential hiv-1 integrase inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6245433/
https://www.ncbi.nlm.nih.gov/pubmed/18830166
http://dx.doi.org/10.3390/molecules13102442
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