5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
A series of pyrimidine nitrile inhibitors of Cathepsin K with reduced glutathione reactivity has been identified and Molecular Core Matching (MoCoM) has been used to quantify the effect of an amino substituent at C5.
Morley
Andrew D
AD
AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
Kenny
Peter W
PW
Burton
Brenda
B
Heald
Robert A
RA
Macfaul
Philip A
PA
Mullett
Julia
J
Page
Ken
K
Porres
Soraya S
SS
Ribeiro
Lyn Rosenbrier
LR
Smith
Phil
P
Ward
Stuart
S
Wilkinson
Tina J
TJ
D056657:Cathepsin K; D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D008247:Lysosomes / Q000201:enzymology; D008956:Models, Chemical; D015394:Molecular Structure; D009570:Nitriles / Q000138:chemical synthesis*; D010003:Osteoarthritis / Q000188:drug therapy; D010010:Osteoclasts; D010024:Osteoporosis / Q000188:drug therapy; D011743:Pyrimidines / Q000737:chemistry; D013329:Structure-Activity Relationship; D013678:Technology, Pharmaceutical / Q000379:methods
D015853:Cysteine Proteinase Inhibitors; D009570:Nitriles; D011743:Pyrimidines; D002403:Cathepsins; C534130:CTSK protein, human; D056657:Cathepsin K