Molecules 2008, 13(10), 2442-2461; doi:10.3390/molecules13102442
Article

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

Mario Sechi 1,* email, Ugo Azzena 2 , Maria Paola Delussu 1 , Roberto Dallocchio 3 , Alessandro Dessì 3 , Alessia Cosseddu 4 , Nicolino Pala 1  and Nouri Neamati 5,* email
1 Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via Muroni 23/A, 07100 Sassari, Italy 2 Dipartimento di Chimica, Università di Sassari, Via Vienna 2, 07100 Sassari, Italy 3 CNR-Istituto di Chimica Biomolecolare, Sassari, 07040 Li Punti, Italy 4 Dipartimento Farmaco Chimico Tecnologico, Università di Siena, Via A. Moro, 53100 Siena, Italy 5 Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, 1985 Zonal Avenue, PSC 304, Los Angeles, California, 90089, USA
* Authors to whom correspondence should be addressed.
Received: 11 April 2008; in revised form: 19 September 2008 / Accepted: 19 September 2008 / Published: 1 October 2008
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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.
Keywords: Bis-amides; Hydrazides; Malonic acid; HIV-1; HIV-1 integrase; Docking studies

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MDPI and ACS Style

Sechi, M.; Azzena, U.; Delussu, M.P.; Dallocchio, R.; Dessì, A.; Cosseddu, A.; Pala, N.; Neamati, N. Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors. Molecules 2008, 13, 2442-2461.

AMA Style

Sechi M, Azzena U, Delussu MP, Dallocchio R, Dessì A, Cosseddu A, Pala N, Neamati N. Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors. Molecules. 2008; 13(10):2442-2461.

Chicago/Turabian Style

Sechi, Mario; Azzena, Ugo; Delussu, Maria Paola; Dallocchio, Roberto; Dessì, Alessandro; Cosseddu, Alessia; Pala, Nicolino; Neamati, Nouri. 2008. "Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors." Molecules 13, no. 10: 2442-2461.

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