Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
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).
Fenwick
A E
AE
Department of Medicinal Chemistry, Smith Kline Beecham Pharmaceuticals, Essex, UK.
Garnier
B
B
Gribble
A D
AD
Ife
R J
RJ
Rawlings
A D
AD
Witherington
J
J
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
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