J. Milton et al., BIARYL ACIDS - NOVEL NONNUCLEOSIDE INHIBITORS OF HIV REVERSE-TRANSCRIPTASE TYPES 1 AND 2, Bioorganic & medicinal chemistry letters, 8(19), 1998, pp. 2623-2628
A series of biaryl acids has been found to show micromolar inhibition
of the HIV reverse transcriptase (RT) from types 1 and 2 with IC(50)s
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 o
nly. (C) 1998 Elsevier Science Ltd. All rights reserved.