4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 19, Pages 5573-5575

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.044

Keywords

CD22; Sialoside; Hanessian reaction; Inhibitor; ELISA

Funding

  1. Egyptian Government
  2. ministry of Education, Culture, Sports, Science, and Technology (MEXT) of Japan [17101007]
  3. JST
  4. Grants-in-Aid for Scientific Research [17101007] Funding Source: KAKEN

Ask authors/readers for more resources

Our previous study revealed that compound 1 (9-(4'-hydroxy-4-biphenyl)acetamido-9-deoxy-Neu5Gc alpha 2-6GalOMP) 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. (C) 2009 Elsevier Ltd. All rights reserved.

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