3N4C

6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.

Cai, J., Baugh, M., Black, D., Long, C., Jonathan Bennett, D., Dempster, M., Fradera, X., Gillespie, J., Andrews, F., Boucharens, S., Bruin, J., Cameron, K.S., Cumming, I., Hamilton, W., Jones, P.S., Kaptein, A., Kinghorn, E., Maidment, M., Martin, I., Mitchell, A., Rankovic, Z., Robinson, J., Scullion, P., Uitdehaag, J.C., Vink, P., Westwood, P., van Zeeland, M., van Berkom, L., Bastiani, M., Meulemans, T.

(2010) Bioorg Med Chem Lett 20: 4350-4354

• PubMed: 20598883 Search on PubMed
• DOI: https://doi.org/10.1016/j.bmcl.2010.06.072
• Primary Citation of Related Structures:  
  3N4C


• PubMed Abstract: 
  

  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.

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Organizational Affiliation: 

Merck Research Laboratories, Newhouse, Lanarkshire ML1 5SH, UK. jiaqiang.cai@merck.com