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Molecules

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

M Sechi, U Azzena, MP Delussu, R Dallocchio, A Dessì…

文献索引:Sechi, Mario; Azzena, Ugo; Delussu, Maria Paola; Dallocchio, Roberto; Dessi, Alessandro; Cosseddu, Alessia; Pala, Nicolino; Neamati, Nouri Molecules, 2008 , vol. 13, # 10 p. 2442 - 2461

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被引用次数: 26

摘要

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.