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

Sechi, Mario and Azzena, Ugo Gavino and Delussu, Maria Paola and Dallocchio, Roberto and Dessì, Alessandro and Cosseddu, Alessia and Pala, Nicolino and Nouri, Neamati (2008) Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors. Molecules, Vol. 13 (10), p. 2442-2461. ISSN 1420-3049. Article.

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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.

Item Type:Article
ID Code:1096
Status:Published
Refereed:Yes
Uncontrolled Keywords:Bis-amides, hydrazides, malonic acid, HIV-1, HIV-1 integrase, docking studies
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Chimica
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
002 Altri enti e centri di ricerca del Nord Sardegna > CNR-Consiglio Nazionale delle Ricerche > Istituto di chimica biomolecolare, Sassari
Publisher:Molecular Diversity Preservation International
ISSN:1420-3049
Deposited On:18 Aug 2009 10:04

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