1H-Imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: Separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pkₐ
2011
Arbuckle, Wullie | Baugh, Mark | Belshaw, Simone | Bennett, D Jonathan | Bruin, John | Cai, Jiaqiang | Cameron, Kenneth S. | Claxton, Chris | Dempster, Maureen | Everett, Kathryn | Fradera, Xavier | Hamilton, William | Jones, Philip S. | Kinghorn, Emma | Long, Clive | Martin, Iain | Robinson, John | Westwood, Paul
Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pkₐ of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pkₐ6–8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen.
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