title: Amino acid derived sulfonamide hydroxamates as inhibitors of procollagen C-proteinase. Part 2: Solid-phase optimization of side chains.
abstract: 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.
authors.affiliation: Roche Bioscience, Inflammatory and Viral Diseases Unit, 3401 Hillview Avenue, Palo Alto, CA 94304, USA. sharon.dankwardt@roche.com
authors.forename: Sharon M
authors.initials: SM
authors.lastname: Dankwardt
authors.forename: Sarah C
authors.initials: SC
authors.lastname: Abbot
authors.forename: Chris A
authors.initials: CA
authors.lastname: Broka
authors.forename: Robert L
authors.initials: RL
authors.lastname: Martin
authors.forename: Christine S
authors.initials: CS
authors.lastname: Chan
authors.forename: Eric B
authors.initials: EB
authors.lastname: Springman
authors.forename: Harold E
authors.initials: HE
authors.lastname: Van Wart
authors.forename: Keith A M
authors.initials: KA
authors.lastname: Walker
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D055395:Bone Morphogenetic Protein 1; D019485:Bone Morphogenetic Proteins / Q000037:antagonists & inhibitors*; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry*
chemical_list: D000596:Amino Acids; D019485:Bone Morphogenetic Proteins; D006877:Hydroxamic Acids; D011480:Protease Inhibitors; D013449:Sulfonamides; D008666:Metalloendopeptidases; D055395:Bone Morphogenetic Protein 1