544467-02-9Relevant articles and documents
Azido-containing aryl β-diketo acid HIV-1 integrase inhibitors
Zhang, Xuechun,Pais, Godwin C.G.,Svarovskaia, Evguenia S.,Marchand, Christophe,Johnson, Allison A.,Karki, Rajeshri G.,Nicklaus, Marc C.,Pathak, Vinay K.,Pommier, Yves,Burke Jr., Terrence R.
, p. 1215 - 1219 (2007/10/03)
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.