1. Belozeksky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia 2. Zelinsky Institute of Organic Chemistry, Moscow, Russia
Human immunodeficiency virus first type (HIV-1) is a main cause of one of the most dangerous diseases, AIDS. The search for new inhibitors of the virus still remains an urgent task. One approach to suppress the HIV infection is to use a double-acting inhibitors, i.e. inhibitors directed to two stages of the viral life cycle. The catalytic domain of HIV-1 integrase has a similar spatial organization with ribonuclease (RNase H) domain of HIV-1 reverse transcriptase, and approach aimed to create HIV-1 integrase and RNase H double-acting is very promising. In this work we synthesized a series of 6-nitrobenzofuroxane derivatives and studied their ability to inhibit two viral enzymes – integrase and RNase H HIV-1.
Download PDF:
Keywords: HIV-1, inhibitor, integrase, reverse transcriptase, RNase H
Korolev S.P. et al. Nitrobenzofuroxane derivatives as dual action HIV-1 inhibitors // Biomeditsinskaya Khimiya. - 2016. - V. 62. -N 6. - P. 725-728.
Korolev S.P. et al., "Nitrobenzofuroxane derivatives as dual action HIV-1 inhibitors." Biomeditsinskaya Khimiya 62.6 (2016): 725-728.
Korolev, S. P., Pustovarova, M. A., Starosotnikov, A. M., Bastrakov, M. A., Agapkina, Yu. Yu., Shevelev, S. A., Gottikh, M. B. (2016). Nitrobenzofuroxane derivatives as dual action HIV-1 inhibitors. Biomeditsinskaya Khimiya, 62(6), 725-728.
Billamboz M., Bailly F., Barreca M.L., De Luca L., Mouscadet J.F., Calmels C., Andreola M.L., Witvrouw M., Christ F., Debyser Z., Cotelle P. (2008) J. Med. Chem., 51, 7717-7730. CrossRef Scholar google search
Billamboz M., Bailly F., Lion C., Calmels C., Andréola M.L., Witvrouw M., Christ F., Debyser Z., De Luca L., Chimirri A., Cotelle P. (2011) Eur. J. Med. Chem. 46(2), 535-546. CrossRef Scholar google search
