Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376161 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
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 and physicochemical properties. The key structural features of the inhibitors consist of a combination of a spiro[2.5]oct-6-ylmethylamine P2 group at the 4-position, a small or polar P3 group at the 5-position and/or a polar group at the 6-position of the pyrimidine.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Osamu Irie, Fumiaki Yokokawa, Takeru Ehara, Atsuko Iwasaki, Yuki Iwaki, Yuko Hitomi, Kazuhide Konishi, Masashi Kishida, Atsushi Toyao, Keiichi Masuya, Hiroki Gunji, Junichi Sakaki, Genji Iwasaki, Hajime Hirao, Takanori Kanazawa, Keiko Tanabe,