4.7 Article

Arylamine based cathepsin K inhibitors: Investigating P3 heterocyclic substituents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 20, Pages 6807-6819

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.06.031

Keywords

cathepsin K; inhibitor; SAR study; heterocyclic substituent

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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. (c) 2006 Elsevier Ltd. All rights reserved.

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