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  • Title: Arylamine based cathepsin K inhibitors: investigating P3 heterocyclic substituents.
    Author: Shinozuka T, Shimada K, Matsui S, Yamane T, Ama M, Fukuda T, Taki M, Takeda Y, Otsuka E, Yamato M, Naito S.
    Journal: Bioorg Med Chem; 2006 Oct 15; 14(20):6807-19. PubMed ID: 16829073.
    Abstract:
    A modification of novel cathepsin K inhibitors I was carried out. The structural design was aimed at reducing the lipophilic character of compounds I for obtaining better pharmacokinetic profiles. This modification afforded several less lipophilic compounds with good inhibitory activities and pharmacokinetic profiles, although the enzyme selectivity over cathepsin S was left at issue.
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