title: New chemotypes for cathepsin K inhibitors.
abstract: Cyano pyrimidine acetylene and cyano pyrimidine t-amine, which belong to a new chemical class, were prepared and tested for inhibitory activities against cathepsin K and the highly homologous cathepsins L and S. The use of novel chemotypes in the development of cathepsin K inhibitors has been demonstrated by derivatives of compounds 1 and 8.
authors: Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan. naoki.teno@novartis.com
authors: Naoki
authors: N
authors: Teno
authors: Osamu
authors: O
authors: Irie
authors: Takahiro
authors: T
authors: Miyake
authors: Keigo
authors: K
authors: Gohda
authors: Miyuki
authors: M
authors: Horiuchi
authors: Sachiyo
authors: S
authors: Tada
authors: Kazuhiko
authors: K
authors: Nonomura
authors: Motohiko
authors: M
authors: Kometani
authors: Genji
authors: G
authors: Iwasaki
authors: Claudia
authors: C
authors: Betschart
mesh_terms: D001665:Binding Sites; D056657:Cathepsin K; D056668:Cathepsin L; D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D003546:Cysteine Endopeptidases / Q000378:metabolism; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D002403:Cathepsins; D003546:Cysteine Endopeptidases; C534281:CTSL protein, human; D056668:Cathepsin L; C028217:cathepsin S; C534130:CTSK protein, human; D056657:Cathepsin K