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ID: ALA1144971
Journal: Bioorg Med Chem Lett
Title: Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.
Authors: Zhang X, Pais GC, Svarovskaia ES, Marchand C, Johnson AA, Karki RG, Nicklaus MC, Pathak VK, Pommier Y, Burke TR.
Abstract: Aryl beta-diketo acids (ADK) comprise a general class of potent HIV-1 integrase (IN) inhibitors, which can exhibit selective inhibition of strand transfer reactions in extracellular recombinant IN assays and provide potent antiviral effects in HIV-infected cells. Recent studies have shown that polycyclic aryl or aryl rings bearing aryl-containing substituents are components of potent members of this class. Reported herein is the first use of azido functionality as an aryl replacement in beta-diketo acid IN inhibitors. The ability of azido-containing inhibitors to exhibit potent inhibition of IN and antiviral protection in HIV-infected cells, renders the azide group of potential value in the further development of ADK-based IN inhibitors.
CiteXplore: 12643946