Nitrobenzofuroxane derivatives as dual action HIV-1 inhibitors

Abstract

Human immunodeficiency virus type 1 (HIV-1) causes one of the most dangerous diseases, HIV infection and AIDS. The search for new inhibitors of the virus still remains an urgent task. One of approaches to suppress the HIV infection is the use of dual action HIV-1 inhibitors, i.e. inhibitors targeting two stages of the viral life cycle. The catalytic domain of HIV-1 integrase shares similar structural organization with the ribonuclease (RNase H) domain of HIV-1 reverse transcriptase, and therefore an approach aimed at creation of dual action inhibitors which would simultaneously inhibit HIV-1 integrase and RNase H seems to be very promising. In this work we have synthesized a series of 6-nitrobenzofuroxane derivatives and studied their inhibitory activity towards two HIV-1 enzymes, integrase and RNase H.