Pierre L. Beaulieu

TL;DR: In this paper, the authors present compounds of formula (I) wherein X is a terminal group, for exemple, an aryloxycarbonyl, an alka-noyl or an optionally mono- or disubstituted carbamoyl; B is absent or an amino acid residue,for example, Val or Asn; R 1 is hy-drogen or a ring substituent, for example, fluoro or methyl; R 2 is alkyl; and Y is a ring substitute, for instance, phenoxy,

TL;DR: This work describes an example where a ligand's "structural hinge" influences potency by inducing an "L-shape" bioactive conformation, and due to its solvent exposure in the complex, reasonable conformation-activity-relationships can be qualitatively attributed.

TL;DR: Structural-activity studies reveal beneficial modifications that result in improved antiviral potency in cell culture in a murine ocular model of HSV-induced keratitis and provide BILD 1357, a significantly more potent antiviral compound than the previously published best compound, BILD 1263.

TL;DR: A structure activity investigation based on the pentapeptide H-Val- Val-Asn-Asp-Leu-OH finds smaller, more potent inhibitors in the hunt for inhibitor potency increases.

TL;DR: This report details the structure--activity studies that lead to the indentification of BILD 1263, a potent inhibitor of HSV RR subunit association that also inhibits the replication ofHSV types 1 and 2 in cell culture and reduces the severity of HSv-1-induced keratitis in a murine ocular model.