Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids.
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.
Stranix
Brent R
BR
Ambrilia Biopharma Inc., 1000 chemin du Golf, Verdun, QC, Canada H3E 1H4. bstranix@ambrilia.com
Lavallée
Jean-François
JF
Sévigny
Guy
G
Yelle
Jocelyn
J
Perron
Valérie
V
LeBerre
Nicholas
N
Herbart
Dominik
D
Wu
Jinzi J
JJ
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*
D000596:Amino Acids; D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D013449:Sulfonamides; D008239:Lysine