Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas.
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.
Stranix
Brent R
BR
Procyon Biopharma Inc., 1650 Trans-Canada Highway, Suite 200, Dorval, Quebec, Canada, H9P 1H7. bstranix@procyonbiopharma.com
Sauvé
Gilles
G
Bouzide
Abderrahim
A
Coté
Alexandre
A
Sévigny
Guy
G
Yelle
Jocelyn
J
Perron
Valérie
V
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*
D017320:HIV Protease Inhibitors; D013449:Sulfonamides; D008239:Lysine