Abstract
HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) are part of the combination therapy currently used to treat HIV infection. The features of a new NNRTI drug for HIV treatment must include selective potent activity against both wild-type virus as well as against mutant virus that have been selected by use of current antiretroviral treatment regimens. Based on analogy with known HIV-1 NNRTI inhibitors and modeling studies utilizing the X-ray crystal structure of inhibitors bound in the HIV-1 RT, a series of substituted 2-quinolones was synthesized and evaluated as HIV-1 inhibitors.
MeSH terms
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Alkynes
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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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Benzoxazines
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Binding Sites
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Cell Line
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Crystallography, X-Ray
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Cyclopropanes
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Drug Design
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Drug Resistance, Viral*
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HIV Reverse Transcriptase / chemistry*
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HIV Reverse Transcriptase / genetics
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HIV Reverse Transcriptase / metabolism
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HIV-1 / drug effects
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HIV-1 / enzymology
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Humans
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Models, Molecular
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Molecular Structure
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Mutation
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Oxazines / chemistry
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Quinolones / chemical synthesis*
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Quinolones / chemistry
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Quinolones / pharmacology
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology
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Structure-Activity Relationship
Substances
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Alkynes
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Anti-HIV Agents
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Benzoxazines
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Cyclopropanes
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Oxazines
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Quinolones
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Reverse Transcriptase Inhibitors
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HIV Reverse Transcriptase
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efavirenz