title: [Nitrobenzofuroxane derivatives as dual action hiv-1 inhibitors].
abstract: 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.
authors.affiliation: Belozeksky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: S P
authors.initials: SP
authors.lastname: Korolev
authors.affiliation: Belozeksky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: M A
authors.initials: MA
authors.lastname: Pustovarova
authors.affiliation: Zelinsky Institute of Organic Chemistry, Moscow, Russia.
authors.forename: A M
authors.initials: AM
authors.lastname: Starosotnikov
authors.affiliation: Zelinsky Institute of Organic Chemistry, Moscow, Russia.
authors.forename: M A
authors.initials: MA
authors.lastname: Bastrakov
authors.affiliation: Belozeksky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: Yu Yu
authors.initials: YY
authors.lastname: Agapkina
authors.affiliation: Zelinsky Institute of Organic Chemistry, Moscow, Russia.
authors.forename: S A
authors.initials: SA
authors.lastname: Shevelev
authors.affiliation: Belozeksky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russia.
authors.forename: M B
authors.initials: MB
authors.lastname: Gottikh
mesh_terms: D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D015497:HIV-1 / Q000201:enzymology*; D006801:Humans; D010069:Oxadiazoles / Q000737:chemistry*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry*
chemical_list: D010069:Oxadiazoles; D018894:Reverse Transcriptase Inhibitors; C014701:nitrobenzofuroxan; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase
keywords: HIV-1; RNase H; inhibitor; integrase; reverse transcriptase