4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Basic Information
ID: ALA1156562
Journal: Bioorg Med Chem Lett
Title: 4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Authors: Irie O, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Konishi K, Kishida M, Toyao A, Masuya K, Gunji H, Sakaki J, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Kosaka T, Hart TW, Hallett A.
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.
CiteXplore: 18662880
DOI: 10.1016/j.bmcl.2008.07.011
Patent ID: ┄