期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 14, 页码 3959-3962出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.009
关键词
cathepsin S inhibitor; pyrrolopyrimidine; nitrile; nonpeptidic; cysteine protease
Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an in-house pyrrolopyrimidine cathepsin K inhibitor by modi. cation 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. (c) 2008 Elsevier Ltd. All rights reserved.
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