Abstract
A series of biaryl acids has been found to show micromolar inhibition of the HIV reverse transcriptase (RT) from types 1 and 2 with IC50S in the micromolar range. The series was discovered by consideration of the polymerase active site and sub-structure searching of the company compound collection. Synthesis of analogues to investigate the SAR is described. Two of these compounds have shown inhibition of HIV-2 RT only.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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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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Carboxylic Acids / chemical synthesis
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Carboxylic Acids / chemistry*
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Carboxylic Acids / pharmacology*
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HIV Reverse Transcriptase / antagonists & inhibitors*
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Hydrocarbons, Aromatic / chemical synthesis
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Hydrocarbons, Aromatic / chemistry
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Hydrocarbons, Aromatic / pharmacology
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RNA-Directed DNA Polymerase / drug effects*
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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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Anti-HIV Agents
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Carboxylic Acids
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Hydrocarbons, Aromatic
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Reverse Transcriptase Inhibitors
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reverse transcriptase, Human immunodeficiency virus 2
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HIV Reverse Transcriptase
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RNA-Directed DNA Polymerase