Bioorganic and Medicinal Chemistry Letters p. 4350 - 4354 (2010)
Update date:2022-07-29
Cai, Jiaqiang
Baugh, Mark
Black, Darcey
Long, Clive
Jonathan Bennett
Dempster, Maureen
Fradera, Xavier
Gillespie, Jonathan
Andrews, Fiona
Boucharens, Sylviane
Bruin, John
Cameron, Kenneth S.
Cumming, Iain
Hamilton, William
Jones, Philip S.
Kaptein, Allard
Kinghorn, Emma
Maidment, Maurice
Martin, Iain
Mitchell, Ann
Rankovic, Zoran
Robinson, John
Scullion, Paul
Uitdehaag, Joost C.M.
Vink, Paul
Westwood, Paul
Van Zeeland, Mario
Van Berkom, Leon
Bastiani, Martijn
Meulemans, Tommi
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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