Nitrobenzofuroxane derivatives as dual action HIV-1 inhibitors

Korolev S.P.1 , Pustovarova M.A.1, Starosotnikov A.M.2, Bastrakov M.A.2, Agapkina Yu.Yu.1, Shevelev S.A.2, Gottikh M.B.1

1. Belozeksky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia
2. Zelinsky Institute of Organic Chemistry, Moscow, Russia
Section: Short Communication
DOI: 10.18097/PBMC20166206725      PubMed Id: 28026819
Year: 2016  Volume: 62  Issue: 6  Pages: 725-728
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.
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Keywords: HIV-1, inhibitor, integrase, reverse transcriptase, RNase H

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.
This paper is also available as the English translation: 10.1134/S1990750817030064
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