| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370440 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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.
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Related Topics
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Organic Chemistry
Authors
Brian A. Johns, Takashi Kawasuji, Jason G. Weatherhead, Eric E. Boros, James B. Thompson, Edward P. Garvey, Scott A. Foster, Jerry L. Jeffrey, Wayne H. Miller, Noriyuki Kurose, Kenichi Matsumura, Tamio Fujiwara,