一系列间位苯胺基LFA-1 ICAM抑制剂的设计与合成。
Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.
作者信息
Guckian Kevin M, Lin Edward Yin-Shiang, Silvian Laura, Friedman Jessica E, Chin Donovan, Scott Daniel M
机构信息
Biogen Idec, 14 Cambridge Center, Cambridge, MA 02142, USA.
出版信息
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5249-51. doi: 10.1016/j.bmcl.2008.08.061. Epub 2008 Aug 22.
A series of meta-substituted anilines were designed and synthesized to inhibit the interaction of LFA-1 with ICAM for the treatment of autoimmune disease. Design of these molecules was performed by utilizing a co-crystal structure for structure-based drug design. The resulting molecules were found to be potent and to possess favorable pharmaceutical properties.
设计并合成了一系列间位取代苯胺，以抑制淋巴细胞功能相关抗原-1（LFA-1）与细胞间黏附分子（ICAM）的相互作用，用于治疗自身免疫性疾病。这些分子的设计是通过利用共晶体结构进行基于结构的药物设计来完成的。结果发现所得分子具有强效性且具备良好的药学性质。
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