1-Amido-1-phenyl-3-piperidinylbutanes – CCR5 antagonists for the treatment of HIV: Part 2
Autor: | Rachel L. Eastwood, Kerry A. Paradowski, Donald Stuart Middleton, Jean-Yves Chiva, Barber Christopher Gordon, David C. Blakemore |
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Rok vydání: | 2009 |
Předmět: |
Receptors
CCR5 Anti-HIV Agents Clinical Biochemistry hERG Triazole Pharmaceutical Science HIV Infections Stereoisomerism CCR5 receptor antagonist Biochemistry Cell Line chemistry.chemical_compound Dogs Piperidines Drug Discovery Animals Humans Molecular Biology Ion channel biology Organic Chemistry Antagonist Triazoles Combinatorial chemistry Rats chemistry CCR5 Receptor Antagonists Butanes biology.protein Molecular Medicine Piperidine Caco-2 Cells Selectivity |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 19:1499-1503 |
ISSN: | 0960-894X |
DOI: | 10.1016/j.bmcl.2009.01.008 |
Popis: | Optimisation of a series of 4-piperidinyltriazoles led to the identification of compound 28a which showed good whole cell antiviral activity, excellent selectivity over the hERG ion channel and complete oral absorption. |
Databáze: | OpenAIRE |
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