Potent small molecule mouse CD22-inhibitors: Exploring the interaction of the residue at C-2 of sialic acid scaffold
Potent small molecule mouse CD22-inhibitors: Exploring the interaction of the residue at C-2 of sialic acid scaffold
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DOI：
10.1016/j.bmcl.2009.08.044
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发表时间：
2009-10-01
影响因子：
2.7
通讯作者：
Kiso, Makoto
中科院分区：
文献类型：
--
作者：
Abdu-Allah, Hajjaj H. M.;Watanabe, Kozo;Kiso, Makoto
我们先前的研究揭示了化合物1（9-（4 '-羟基-4-联苯基）乙酰氨基-9-脱氧-Neu 5Gc α 2- 6 GalOMP）对mCD 22具有最有希望的亲和力。取代亚末端半乳糖残基的1与苄基或联苯甲基作为苷元导致38倍和20倍的效力，分别。这一发现代表了适合药物开发的抑制剂设计的新方向。(C)2009爱思唯尔有限公司保留所有权利。
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.