title: Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas.
abstract: A series of lysine sulfonamide analogues bearing a Nepsilon-benzylic ureas was synthesized using both solution-phase and solid-phase approaches. A novel synthetic route of Nalpha-(alkyl)-Nalpha-(sulfonamides)lysinol using alpha-amino-caprolactam was developed. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type HIV virus.
authors.affiliation: Procyon Biopharma Inc., 1650 Trans-Canada Highway, Suite 200, Dorval, Quebec, Canada, H9P 1H7. bstranix@procyonbiopharma.com
authors.forename: Brent R
authors.initials: BR
authors.lastname: Stranix
authors.forename: Gilles
authors.initials: G
authors.lastname: Sauvé
authors.forename: Abderrahim
authors.initials: A
authors.lastname: Bouzide
authors.forename: Alexandre
authors.initials: A
authors.lastname: Coté
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
mesh_terms: D006678:HIV / Q000187:drug effects*; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D007700:Kinetics; D008239:Lysine; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D017320:HIV Protease Inhibitors; D013449:Sulfonamides; D008239:Lysine