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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.

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

06/10/1998

Volume

8

Pages

2623 - 2628

Keywords

Anti-HIV Agents, Carboxylic Acids, HIV Reverse Transcriptase, Hydrocarbons, Aromatic, RNA-Directed DNA Polymerase, Reverse Transcriptase Inhibitors, Structure-Activity Relationship