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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2010-06-17 , DOI: 10.1016/j.bmcl.2010.06.072 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 , Zoran Rankovic , John Robinson , Paul Scullion , Joost C.M. Uitdehaag , Paul Vink , Paul Westwood , Mario van Zeeland , Leon van Berkom , Martijn Bastiani , Tommi Meulemans
中文翻译：
6-苯基-1 H-咪唑并[4,5 - c ]吡啶-4-腈作为组织蛋白酶S抑制剂
更新日期：2010-06-17
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2010-06-17 , DOI: 10.1016/j.bmcl.2010.06.072 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 , Zoran Rankovic , John Robinson , Paul Scullion , Joost C.M. Uitdehaag , Paul Vink , Paul Westwood , Mario van Zeeland , Leon van Berkom , Martijn Bastiani , Tommi Meulemans
6-Phenyl-1H-imidazo[4,5-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.
中文翻译：
6-苯基-1 H-咪唑并[4,5 - c ]吡啶-4-腈作为组织蛋白酶S抑制剂
6-苯基-1 H-咪唑并[4，5 - c ]吡啶-4-甲腈类似物被鉴定为针对纯化的酶和基于人JY细胞的细胞分析的有效的和选择性的组织蛋白酶S抑制剂。与已广泛报道的嘧啶-2-甲腈半胱氨酸组织蛋白酶抑制剂相比，该核具有非常稳定的硫捕获腈腈战斗部。化合物47在体内小鼠脾脏Lip10积累测定中也非常有效。
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