Potent small molecule mouse CD22-inhibitors: exploring the interaction of the residue at C-2 of sialic acid scaffold.

Autor: Abdu-Allah HH; Department of Applied Bio-organic Chemistry, The United Graduate School of Agricultural Sciences, Gifu University, Gifu 501-1193, Japan. moazhajjaj@yahoo.com, Watanabe K, Hayashizaki K, Takaku C, Tamanaka T, Takematsu H, Kozutsumi Y, Tsubata T, Ishida H, Kiso M
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Oct 01; Vol. 19 (19), pp. 5573-5. Date of Electronic Publication: 2009 Aug 15.
DOI: 10.1016/j.bmcl.2009.08.044
Abstrakt: Our previous study revealed that compound 1 (9-(4'-hydroxy-4-biphenyl)acetamido-9-deoxy-Neu5Gcalpha2-6GalOMP) has the most promising affinity for mCD22. Replacing the subterminal galactose residue of 1 with benzyl or biphenylmethyl as aglycone led to 38- and 20-fold higher potency, respectively. This discovery represents a new direction in inhibitor design suitable for pharmaceutical development.
Databáze: MEDLINE