The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore

作者：Johns Brian A^*; Weatherhead Jason G; Allen Scott H; Thompson James B; Garvey Edward P; Foster Scott A; Jeffrey Jerry L; Miller Wayne H

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(6): 1802-1806.

DOI：10.1016/j.bmcl.2009.01.090

• HIV integrase
• Integration
• Two-metal binder
• Metal chelation

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.

• 出版日期2009-3-15