| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370911 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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 pka 6–8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen.
Graphical abstractBased on the theoretical understanding of the in vivo lysosomotropism, by manipulating the pka of the cathepsin S inhibitors, a set of compounds with pka 6–8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![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](/preview/png/1370911.png "First Page Preview: 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")
Authors
Wullie Arbuckle, Mark Baugh, Simone Belshaw, D. Jonathan Bennett, John Bruin, Jiaqiang Cai, Kenneth S. Cameron, Chris Claxton, Maureen Dempster, Kathryn Everett, Xavier Fradera, William Hamilton, Philip S. Jones, Emma Kinghorn, Clive Long, Iain Martin,