863443-84-9Relevant 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
, 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.
