Imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV-1 |
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| Authors: | Kristjan S Gudmundsson Sharon D Boggs John G Catalano Angilique Svolto Andrew Spaltenstein Michael Thomson Pat Wheelan Stephen Jenkinson |
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| Institution: | 1. Department of Medicinal Chemistry , Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA;2. Department of Virology, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA;3. Department of DMPK, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA;4. Department of Biochemical and Analytical Pharmacology, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA |
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| Abstract: | Synthesis of several novel imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV are described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity and pharmacokinetics are highlighted. Several compounds with low nanomolar anti-HIV activity and oral bioavailability are described. |
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| Keywords: | CXCR4 HIV Antiviral Imidazopyridine Tetrahydroquinoline |
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