脒作为VLA - 4拮抗剂中酰胺键的替代物。
Amidines as amide bond replacements in VLA-4 antagonists.
作者信息
Kamenecka Theodore M, Park You-Jung, Lin Linus S, de Laszlo Stephen, McCauley Ermengilda D, Van Riper Gail, Egger Linda, Kidambi Usha, Mumford Richard A, Tong Sharon, Tang Wei, Colletti Adria, Teffera Yohannes, Stearns Ralph, MacCoss Malcolm, Schmidt John A, Hagmann William K
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2004 May 3;14(9):2323-6. doi: 10.1016/j.bmcl.2004.01.100.
VLA-4 (alpha(4)beta(1), very late activating antigen-4), a key cell surface integrin plays an important role in inflammation by promoting leukocyte attachment and extravasation from the vasculature into the peripheral tissues. As such, VLA-4 antagonists may be useful in the treatment, prevention, and suppression of diseases where cell adhesion and migration are important such as asthma, rheumatoid arthritis, and multiple sclerosis. Herein, we report on the discovery, synthesis, and biological evaluation of amidines as small molecule antagonists of VLA-4.
VLA-4（α(4)β(1)，极迟活化抗原-4）是一种关键的细胞表面整合素，通过促进白细胞黏附以及从血管系统外渗到外周组织，在炎症中发挥重要作用。因此，VLA-4拮抗剂可能在治疗、预防和抑制细胞黏附与迁移起重要作用的疾病（如哮喘、类风湿性关节炎和多发性硬化症）方面具有应用价值。在此，我们报告脒类作为VLA-4小分子拮抗剂的发现、合成及生物学评价。
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