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.
Synthesis of new pyridazine derivatives as potential anti-HIV-1 agents
FERRO, Stefania;AGNELLO, STEFANO;DE LUCA, Laura;GITTO, Rosaria
2009-01-01
Abstract
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.File in questo prodotto:
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