title: 5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
abstract: 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.
authors.affiliation: AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Morley
authors.forename: Peter W
authors.initials: PW
authors.lastname: Kenny
authors.forename: Brenda
authors.initials: B
authors.lastname: Burton
authors.forename: Robert A
authors.initials: RA
authors.lastname: Heald
authors.forename: Philip A
authors.initials: PA
authors.lastname: Macfaul
authors.forename: Julia
authors.initials: J
authors.lastname: Mullett
authors.forename: Ken
authors.initials: K
authors.lastname: Page
authors.forename: Soraya S
authors.initials: SS
authors.lastname: Porres
authors.forename: Lyn Rosenbrier
authors.initials: LR
authors.lastname: Ribeiro
authors.forename: Phil
authors.initials: P
authors.lastname: Smith
authors.forename: Stuart
authors.initials: S
authors.lastname: Ward
authors.forename: Tina J
authors.initials: TJ
authors.lastname: Wilkinson
mesh_terms: 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
chemical_list: D015853:Cysteine Proteinase Inhibitors; D009570:Nitriles; D011743:Pyrimidines; D002403:Cathepsins; C534130:CTSK protein, human; D056657:Cathepsin K