Potent small molecule mouse CD22-inhibitors: Exploring the interaction of the residue at C-2 of sialic acid scaffold
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- 作者：Hajjaj H.M. Abdu-Allah ; Kozo Watanabe ; Koji Hayashizaki ; Chiaki Takaku ; Taichi Tamanaka ; Hiromu Takematsu ; Yasunori Kozutsumi ; Takeshi Tsubata ; Hideharu Ishida ; Makoto Kiso
- 关键词：CD22 ; Sialoside ; Hanessian reaction ; Inhibitor ; ELISA
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 October 2009
- 年：2009
- 卷：19
- 期：19
- 页码：5573-5575
- 全文大小：305 K
文摘
Our previous study revealed that compound 1 (9-(4′-hydroxy-4-biphenyl)acetamido-9-deoxy-Neu5Gcα2-6GalOMP) 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.