877201-35-9Relevant articles and documents
4-Amino-2-cyanopyrimidines: Novel scaffold for nonpeptidic cathepsin S inhibitors
Irie, Osamu,Yokokawa, Fumiaki,Ehara, Takeru,Iwasaki, Atsuko,Iwaki, Yuki,Hitomi, Yuko,Konishi, Kazuhide,Kishida, Masashi,Toyao, Atsushi,Masuya, Keiichi,Gunji, Hiroki,Sakaki, Junichi,Iwasaki, Genji,Hirao, Hajime,Kanazawa, Takanori,Tanabe, Keiko,Kosaka, Takatoshi,Hart, Terance W.,Hallett, Allan
scheme or table, p. 4642 - 4646 (2009/04/06)
We describe here a novel 4-amino-2-cyanopyrimidine scaffold for nonpeptidomimetic cathepsin S selective inhibitors. Some of the synthesized compounds have sub-nanomolar potency and high selectivity toward cathepsin S along with promising pharmacokinetic a
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-Cyanopyrimidines. Part 2
Irie, Osamu,Kosaka, Takatoshi,Kishida, Masashi,Sakaki, Junichi,Masuya, Keiichi,Konishi, Kazuhide,Yokokawa, Fumiaki,Ehara, Takeru,Iwasaki, Atsuko,Iwaki, Yuki,Hitomi, Yuko,Toyao, Atsushi,Gunji, Hiroki,Teno, Naoki,Iwasaki, Genji,Hirao, Hajime,Kanazawa, Takanori,Tanabe, Keiko,Hiestand, Peter C.,Malcangio, Marzia,Fox, Alyson J.,Bevan, Stuart J.,Yaqoob, Mohammed,Culshaw, Andrew J.,Hart, Terance W.,Hallett, Allan
scheme or table, p. 5280 - 5284 (2009/05/07)
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