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Discovery of selective and nonpeptidic cathepsin S inhibitors.

Irie, Osamu and Ehara, Takeru and Iwasaki, Atsuko and Yokokawa, Fumiaki and Sakaki, Junichi and Hirao, Hajime and Kanazawa, Takanori and Teno, Naoki and Horiuchi, Miyuki and Umemura, Ichiro and Gunji, Hiroki and Masuya, Keiichi and Hitomi, Yuko and Iwasaki, Genji and Nonomura, Kazuhiko and Tanabe, Keiko and Fukaya, Hiroaki and Kosaka, Takatoshi and Snell, Chris and Hallett, Allan (2008) Discovery of selective and nonpeptidic cathepsin S inhibitors. Bioorganic & Medicinal Chemistry Letters, 18 (14). pp. 3959-3962. ISSN 1464-3405


Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an in-house pyrrolopyrimidine cathepsin K inhibitor by modification of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanomolar inhibition of cathepsin S with over 100-fold selectivity against other cysteine proteases, including cathepsin K and L. Some of the inhibitors showed cellular activities in mouse splenocytes as well as oral bioavailabilities in rats.

Item Type: Article
Related URLs:
Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Cathepsin S inhibitor; Pyrrolopyrimidine; Nitrile; Nonpeptidic; Cysteine protease
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Date Deposited: 14 Dec 2009 13:53
Last Modified: 31 Jan 2013 01:06


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