| Literature DB >> 21030256 |
Jiaqiang Cai1, John Robinson, Simone Belshaw, Kathryn Everett, Xavier Fradera, Mario van Zeeland, Leon van Berkom, Peter van Rijnsbergen, Lucy Popplestone, Mark Baugh, Maureen Dempster, John Bruin, William Hamilton, Emma Kinghorn, Paul Westwood, Jennifer Kerr, Zoran Rankovic, Wullie Arbuckle, D Jonathan Bennett, Philip S Jones, Clive Long, Iain Martin, Joost C M Uitdehaag, Tommi Meulemans.
Abstract
The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in this process is the change of the torsion angle between the P2 phenyl ring and the attached secondary amide by adding a small Cl, F, or Me group at the 2-position.Entities:
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Year: 2010 PMID： 21030256 DOI： 10.1016/j.bmcl.2010.10.012
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823