4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors

The synthesis and SAR of 4-aminophenoxyacetic acids as cathepsin K inhibitors are reported. 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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-03, Vol.16 (6), p.1502-1505
Hauptverfasser:	Shinozuka, Tsuyoshi, Shimada, Kousei, Matsui, Satoshi, Yamane, Takahiro, Ama, Mayumi, Fukuda, Takeshi, Taki, Motohiko, Naito, Satoru
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Biphenylamino acid amides 4-Aminophenoxyacetic acids Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cathepsin K Cathepsin K inhibitors Cathepsins - antagonists & inhibitors Cathepsins - metabolism Cysteine Proteinase Inhibitors - chemical synthesis Cysteine Proteinase Inhibitors - pharmacology Humans Medical sciences Osteoporosis Pharmacology. Drug treatments Phenoxyacetates - chemical synthesis Phenoxyacetates - pharmacology Recombinant Proteins - antagonists & inhibitors Recombinant Proteins - metabolism Structure-Activity Relationship
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Zusammenfassung:	The synthesis and SAR of 4-aminophenoxyacetic acids as cathepsin K inhibitors are reported. 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 IC50 values, although lipophilic groups are favorable for the hydrophobic S1′ pocket.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.12.053