title: Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
abstract: Using solid-phase synthesis, a library of novel cyclic alkoxyketones has been constructed which show strong inhibitory activity against the cysteine protease, cathepsin K (EC 3.4.22.38).
authors.affiliation: Department of Medicinal Chemistry, Smith Kline Beecham Pharmaceuticals, Essex, UK.
authors.forename: A E
authors.initials: AE
authors.lastname: Fenwick
authors.forename: B
authors.initials: B
authors.lastname: Garnier
authors.forename: A D
authors.initials: AD
authors.lastname: Gribble
authors.forename: R J
authors.initials: RJ
authors.lastname: Ife
authors.forename: A D
authors.initials: AD
authors.lastname: Rawlings
authors.forename: J
authors.initials: J
authors.lastname: Witherington
mesh_terms: D001665:Binding Sites; D056657:Cathepsin K; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D020650:Combinatorial Chemistry Techniques; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D005663:Furans / Q000737:chemistry; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D015853:Cysteine Proteinase Inhibitors; D004791:Enzyme Inhibitors; D005663:Furans; D006571:Heterocyclic Compounds; D007659:Ketones; C018674:tetrahydrofuran; D002403:Cathepsins; C534130:CTSK protein, human; D056657:Cathepsin K