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Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-Cyanopyrimidines. Part 2
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Oct2008, Vol. 18 Issue 19, p5280-5284. 5p. - Publication Year :
- 2008
-
Abstract
- Abstract: We describe here orally active and brain-penetrant cathepsin S selective inhibitors, which are virtually devoid of hERG K+ channel affinity, yet exhibit nanomolar potency against cathepsin S and over 100-fold selectivity to cathepsin L. The new non-peptidic inhibitors are based on a 2-cyanopyrimidine scaffold bearing a spiro[3.5]non-6-yl-methyl amine at the 4-position. The brain-penetrating cathepsin S inhibitors demonstrate potential clinical utility for the treatment of multiple sclerosis and neuropathic pain. [Copyright &y& Elsevier]
- Subjects :
- *VIRUS diseases
*COMMUNICABLE diseases
*MEDICAL virology
*ADENOVIRUS diseases
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 18
- Issue :
- 19
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 34435373
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.08.067