Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K.
The diastereoselective synthesis of a novel class of cathepsin K inhibitors together with their cathepsin K affinity and stability towards aqueous buffer is reported.
Fenwick
A E
AE
Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Gribble
A D
AD
Ife
R J
RJ
Stevens
N
N
Witherington
J
J
D002021:Buffers; 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*; D007700:Kinetics; D013329:Structure-Activity Relationship
D002021:Buffers; 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