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4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors
Authors: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
Institution:Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan. osamu.irie@novartis.com
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 spiro2.5]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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