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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors |
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| Authors: | Jiaqiang Cai Mark Baugh Darcey Black Clive Long D Jonathan Bennett Maureen Dempster Xavier Fradera Jonathan Gillespie Fiona Andrews Sylviane Boucharens John Bruin Kenneth S Cameron Iain Cumming William Hamilton Philip S Jones Allard Kaptein Emma Kinghorn Maurice Maidment Iain Martin Ann Mitchell Tommi Meulemans |
| Institution: | 1. Merck Research Laboratories, MSD, Newhouse, Lanarkshire ML1 5SH, United Kingdom;2. Merck Research Laboratories, MSD, 5340BH Oss, The Netherlands;3. Mercachem B.V. Kerkenbos 1013, 6546 BB Nijmegen, The Netherlands |
| Abstract: | 6-Phenyl-1H-imidazo4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stable thio-trapping nitrile war-head in comparison with the well reported pyrimidine-2-carbonitrile cysteine cathepsin inhibitors. Compound 47 is also very potent in in vivo mouse spleenic Lip10 accumulation assays. |
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