4.4 Article

Synthesis of New Pyridazine Derivatives as Potential Anti-HIV-1 Agents

期刊

JOURNAL OF HETEROCYCLIC CHEMISTRY
卷 46, 期 6, 页码 1420-1424

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WILEY-BLACKWELL PUBLISHING, INC
DOI: 10.1002/jhet.230

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  1. European Commission [HEALTH-F3-2008-201032]

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We herein report conventional and microwave-assisted methods for the synthesis of a series of compounds containing some bivalent ion chelating requirements useful to exert potential HIV-1 integrase (IN) enzyme inhibition activity. The biological screening highlighted that only derivative 5 proved to be a strand-transfer step inhibitor of the virus integration process at micromolar concentration.

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