Pierre L. Beaulieu

TL;DR: SAR studies at the N(1)-position of allosteric indole-based HCV NS5B inhibitors has led to the discovery of acetamide derivatives with good cellular potency in subgenomic replicons.

TL;DR: This new series of phosphotyrosine-containing dipeptides binds to the Lck SH2 domain with potencies comparable to that of tetrapeptide 1.

TL;DR: A novel series of non-nucleoside thumb pocket 2 HCV NS 5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis.

TL;DR: The most successful strategy involved modification of the parent drug carboxylic acid moiety to glycolic amide esters which improved solubility in lipid-based self-emulsifying drug delivery systems (SEDDS) and correlated with in vitro stability in liver microsomes.

TL;DR: A new series of compounds that contain an extra nitrogen at the inhibitor N-terminus improves inhibitor binding potency 50-fold over the first published inhibitor series, and provides evidence for the bioactive conformation around two important amino acid residues contained in the authors' inhibitors.