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

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.

SUBMITTER: Sechi M

PROVIDER: S-EPMC6245433 | biostudies-literature | 2008 Oct

REPOSITORIES: biostudies-literature

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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 M Azzena Ugo U Delussu Maria Paola MP Dallocchio Roberto R Dessì Alessandro A Cosseddu Alessia A Pala Nicolino N Neamati Nouri N

Molecules (Basel, Switzerland) 20081001 10

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. ...[more]

PMID: 18830166

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Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities.

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