Abstract
Several novel amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines were synthesized which had potent activity against HIV-1. The synthetic approaches adopted allowed for variation of the substitution pattern and resulting changes in antiviral activity are highlighted. This led to the identification of compounds with low and sub-nanomolar anti-HIV-1 activity.
MeSH terms
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Acquired Immunodeficiency Syndrome / drug therapy
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Amines / chemical synthesis
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Amines / chemistry*
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Amines / pharmacology
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Aminoquinolines
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / chemistry*
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Anti-HIV Agents / pharmacology
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Benzimidazoles / chemical synthesis
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Benzimidazoles / chemistry*
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Benzimidazoles / pharmacology
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Butylamines
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Cell Line, Tumor
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HIV-1 / drug effects*
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Heterocyclic Compounds, 1-Ring / chemistry
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Humans
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Receptors, CXCR4 / antagonists & inhibitors*
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Receptors, CXCR4 / metabolism
Substances
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Amines
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Aminoquinolines
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Anti-HIV Agents
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Benzimidazoles
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Butylamines
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Heterocyclic Compounds, 1-Ring
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Receptors, CXCR4
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