863442-93-7Relevant academic research and scientific papers
HIV INTEGRASE INHIBITORS
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, (2015/09/22)
The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1integrase inhibitors
Johns, Brian A.,Kawasuji, Takashi,Weatherhead, Jason G.,Boros, Eric C.,Thompson, James B.,Garvey, Edward P.,Foster, Scott A.,Jeffrey, Jerry L.,Miller, Wayne H.,Kurose, Noriyuki,Matsumura, Kenichi,Fujiwara, Tamio
scheme or table, p. 6461 - 6464 (2011/12/02)
A series of naphthyridinone HIV-1 integrase strand-transfer inhibitors have been designed based on a psdeudo-C2 symmetry element present in the two-metal chelation pharmacophore. A combination of two distinct inhibitor binding modes resulted in potent inhibition of the integrase strand-transfer reaction in the low nM range. Effects of aryl and N1 substitutions are disclosed including the impact on protein binding adjusted antiviral activity.
Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin- 2(1H)-one HIV integrase inhibitors
Boros, Eric E.,Edwards, Cynthia E.,Foster, Scott A.,Fuji, Masahiro,Fujiwara, Tamio,Garvey, Edward P.,Golden, Pamela L.,Hazen, Richard J.,Jeffrey, Jerry L.,Johns, Brian A.,Kawasuji, Takashi,Kiyama, Ryuichi,Koble, Cecilia S.,Kurose, Noriyuki,Miller, Wayne H.,Mote, Angela L.,Murai, Hitoshi,Sato, Akihiko,Thompson, James B.,Woodward, Mark C.,Yoshinaga, Tomokazu
experimental part, p. 2754 - 2761 (2010/01/16)
The medicinal chemistry and structure-activity relationships for a novel series of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV-integrase inhibitors are disclosed. Substituent effects were evaluated at the N-1, C-3, and 7-benzyl positions of the naph
HIV INTEGRASE INHIBITORS
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Page/Page column 40, (2008/06/13)
The present infention features compounds that are HIV integrase inhibitors and may be useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
