Author/Authors :
Xuechun Zhang، نويسنده , , Godwin C. G. Pais، نويسنده , , Evguenia S. Svarovskaia، نويسنده , , Christophe Marchand، نويسنده , , Allison A. Johnson، نويسنده , , Rajeshri G. Karki، نويسنده , , Marc C. Nicklaus، نويسنده , , Vinay K. Pathak، نويسنده , , Yves Pommier، نويسنده , , Terrence R. Burke Jr.، نويسنده ,
Abstract :
Aryl β-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 β-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.
