1,3,4-Oxadiazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 2: SAR of the C5 position |
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| Authors: | Brian A. Johns Jason G. Weatherhead Scott H. Allen James B. Thompson Edward P. Garvey Scott A. Foster Jerry L. Jeffrey Wayne H. Miller |
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| Affiliation: | 1. Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709, USA;2. Department of Virology, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709, USA |
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| Abstract: | The use of a 1,3,4-oxadiazole in combination with an 8-hydroxy-1,6-naphthyridine ring system has been shown to deliver potent enzyme and antiviral activity through inhibition of viral DNA integration. This report presents a detailed structure–activity investigation of the C5 position resulting in low nM potency for several analogs with an excellent therapeutic index. |
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