title: Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids.
abstract: A series of lysine sulfonamide analogues bearing Nepsilon-acyl aromatic amino acids were synthesized using an efficient synthetic route. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type and multiple-protease inhibitor-resistant HIV viruses.
authors.affiliation: Ambrilia Biopharma Inc., 1000 chemin du Golf, Verdun, QC, Canada H3E 1H4. bstranix@ambrilia.com
authors.forename: Brent R
authors.initials: BR
authors.lastname: Stranix
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Lavallée
authors.forename: Guy
authors.initials: G
authors.lastname: Sévigny
authors.forename: Jocelyn
authors.initials: J
authors.lastname: Yelle
authors.forename: Valérie
authors.initials: V
authors.lastname: Perron
authors.forename: Nicholas
authors.initials: N
authors.lastname: LeBerre
authors.forename: Dominik
authors.initials: D
authors.lastname: Herbart
authors.forename: Jinzi J
authors.initials: JJ
authors.lastname: Wu
mesh_terms: D000215:Acylation; D000596:Amino Acids / Q000737:chemistry*; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006678:HIV / Q000187:drug effects; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008239:Lysine / Q000031:analogs & derivatives / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000596:Amino Acids; D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D013449:Sulfonamides; D008239:Lysine