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Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors |
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| Authors: | Cai Jiaqiang Robinson John Belshaw Simone Everett Kathryn Fradera Xavier van Zeeland Mario van Berkom Leon van Rijnsbergen Peter Popplestone Lucy Baugh Mark Dempster Maureen Bruin John Hamilton William Kinghorn Emma Westwood Paul Kerr Jennifer Rankovic Zoran Arbuckle Wullie Bennett D Jonathan Jones Philip S Long Clive Martin Iain Uitdehaag Joost C M Meulemans Tommi |
| Institution: | Merck Research Laboratories, MSD, Newhouse, Lanarkshire, United Kingdom. jiaqiang.cai@merck.com |
| 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. |
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