Abstract
A variety of N-acetyl-beta-aryl-1,2-didehydroethylamines were synthesized by direct reduction-acetylation of beta-aryl-nitroolefins and assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of >13.2 with CC50 value of >0.787 mM in C8166 cells. This structure-activity relationship (SAR) study provided a new lead for design and discovery of more potent and selective analogues act as NNRTIs.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Ethylamines / chemical synthesis*
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Ethylamines / chemistry
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Ethylamines / pharmacology*
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HIV Reverse Transcriptase / antagonists & inhibitors*
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HIV-1 / enzymology*
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Molecular Structure
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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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Ethylamines
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Reverse Transcriptase Inhibitors
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HIV Reverse Transcriptase