Discovery of selective and nonpeptidic cathepsin S inhibitors.
Basic Information
ID: ALA1155066
Journal: Bioorg Med Chem Lett
Title: Discovery of selective and nonpeptidic cathepsin S inhibitors.
Authors: Irie O, Ehara T, Iwasaki A, Yokokawa F, Sakaki J, Hirao H, Kanazawa T, Teno N, Horiuchi M, Umemura I, Gunji H, Masuya K, Hitomi Y, Iwasaki G, Nonomura K, Tanabe K, Fukaya H, Kosaka T, Snell CR, Hallett A.
Abstract: 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.
CiteXplore: 18572405
DOI: 10.1016/j.bmcl.2008.06.009
Patent ID: ┄