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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

1,* , 2, 1, 3, 3, 4, 1 and 5,*
Received: 11 April 2008 / Revised: 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 Bis-amides; Hydrazides; Malonic acid; HIV-1; HIV-1 integrase; Docking studies
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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