Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 6, Pages 1802-1806Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.090
Keywords
HIV integrase; Integration; Two-metal binder; Metal chelation
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A series of HIV-1 integrase inhibitors containing a novel metal binding motif consisting of the 8-hydroxy1,6-naphthyridine core and either an oxadiazole or triazole has been identified. The design of the key structural components was based on a two-metal coordination pharmacophore. This report presents initial structure-activity data that shows the new chelation architecture delivers potent inhibition in both enzymatic and antiviral assays. (C) 2009 Elsevier Ltd. All rights reserved.
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