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 inhi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-08, Vol.14 (15), p.3971-3974
Hauptverfasser:	Stranix, Brent R, Sauvé, Gilles, Bouzide, Abderrahim, Coté, Alexandre, Sévigny, Guy, Yelle, Jocelyn, Perron, Valérie
Format:	Artikel
Sprache:	eng
Schlagworte:	HIV - drug effects HIV Protease Inhibitors - chemical synthesis HIV Protease Inhibitors - pharmacology Kinetics Lysine Molecular Structure Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - pharmacology
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Zusammenfassung:	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.
ISSN:	0960-894X