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…

Index: 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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Citation Number: 26

Abstract

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.