Amino acid derived sulfonamide hydroxamates as inhibitors of procollagen C-proteinase. Part 2: Solid-phase optimization of side chains

Optimization of the amino acid side chain and the N-alkyl group of the sulfonamide of amino acid derived sulfonamide hydroxamates is discussed. The solid-phase synthesis of these potent inhibitors of procollagen C-proteinase (PCP) is presented. In addition, novel carboxylic acid sulfonamides were di...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-04, Vol.12 (8), p.1233-1235
Hauptverfasser:	DANKWARDT, Sharon M, ABBOT, Sarah C, BROKA, Chris A, MARTIN, Robert L, CHAN, Christine S, SPRINGMAN, Eric B, VAN WART, Harold E, WALKER, Keith A. M
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acids - chemistry Biological and medical sciences Bone Morphogenetic Protein 1 Bone Morphogenetic Proteins - antagonists & inhibitors Bones, joints and connective tissue. Antiinflammatory agents Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Medical sciences Metalloendopeptidases - antagonists & inhibitors Pharmacology. Drug treatments Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Structure-Activity Relationship Sulfonamides - chemistry
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Zusammenfassung:	Optimization of the amino acid side chain and the N-alkyl group of the sulfonamide of amino acid derived sulfonamide hydroxamates is discussed. The solid-phase synthesis of these potent inhibitors of procollagen C-proteinase (PCP) is presented. In addition, novel carboxylic acid sulfonamides were discovered to be PCP inhibitors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(02)00117-8