Title of article
4-Amino-2-cyanopyrimidines: Novel scaffold for nonpeptidic cathepsin S inhibitors
Author/Authors
Osamu Irie، نويسنده , , Fumiaki Yokokawa، نويسنده , , Takeru Ehara، نويسنده , , Atsuko Iwasaki، نويسنده , , Yuki Iwaki، نويسنده , , Yuko Hitomi، نويسنده , , Kazuhide Konishi، نويسنده , , Masashi Kishida، نويسنده , , Atsushi Toyao، نويسنده , , Keiichi Masuya، نويسنده , , Hiroki Gunji، نويسنده , , Junichi Sakaki، نويسنده , , Genji Iwasaki، نويسنده , , Hajime Hirao، نويسنده , , Takanori Kanazawa، نويسنده , , Keiko Tanabe، نويسنده , , Takatoshi Kosaka، نويسنده , , Terance W. Hart، نويسنده , , Allan Hallett، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
4642
To page
4646
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.
Keywords
Cathepsin S inhibitors , Pyrimidine , nitrile , cysteine protease
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799849
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