title: 4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors.
abstract: We have designed and synthesized a novel series of 3-biphenylamino acid amides as cathepsin K inhibitors based on compound I. In these inhibitors, we have discovered 4-aminophenoxyacetic acids 43 and 47 with good IC(50) values, although lipophilic groups are favorable for the hydrophobic S1' pocket.
authors.affiliation: Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. sinozu@sankyo.co.jp
authors.forename: Tsuyoshi
authors.initials: T
authors.lastname: Shinozuka
authors.forename: Kousei
authors.initials: K
authors.lastname: Shimada
authors.forename: Satoshi
authors.initials: S
authors.lastname: Matsui
authors.forename: Takahiro
authors.initials: T
authors.lastname: Yamane
authors.forename: Mayumi
authors.initials: M
authors.lastname: Ama
authors.forename: Takeshi
authors.initials: T
authors.lastname: Fukuda
authors.forename: Motohiko
authors.initials: M
authors.lastname: Taki
authors.forename: Satoru
authors.initials: S
authors.lastname: Naito
mesh_terms: D056657:Cathepsin K; D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D010642:Phenoxyacetates / Q000138:chemical synthesis* / Q000494:pharmacology; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D015853:Cysteine Proteinase Inhibitors; D010642:Phenoxyacetates; D011994:Recombinant Proteins; D002403:Cathepsins; C534130:CTSK protein, human; D056657:Cathepsin K