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Nitrobenzofuroxane derivatives as dual action HIV-1 inhibitors
Author(s) -
С. П. Королев,
M. A. Pustovarova,
Alexey M. Starosotnikov,
Maxim A. Bastrakov,
Yu. Yu. Agapkina,
С. А. Шевелев,
Marina Gottikh
Publication year - 2016
Publication title -
biomeditsinskaya khimiya
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.192
H-Index - 15
eISSN - 2310-6972
pISSN - 2310-6905
DOI - 10.18097/pbmc20166206725
Subject(s) - integrase , human immunodeficiency virus (hiv) , integrase inhibitor , virology , rnase h , chemistry , enzyme , reverse transcriptase , biology , biochemistry , viral load , rna , antiretroviral therapy , gene
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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