β-N-二芳基醚磺酰胺异羟肟酸酯作为有效的明胶酶抑制剂：第2部分。α-氨基取代基的优化。
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
作者信息
Yang Shyh-Ming, Scannevin Robert H, Wang Bingbing, Burke Sharon L, Huang Zhihong, Karnachi Prabha, Wilson Lawrence J, Rhodes Kenneth J, Lagu Bharat, Murray William V
机构信息
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):1140-5. doi: 10.1016/j.bmcl.2007.11.129. Epub 2007 Dec 5.
The introduction and the optimization of an alpha-amino substituent based on a series of alpha-hydroxy-beta-N-biaryl ether sulfonamide hydroxamates is described. The modification leads to a new series of MMP-2/MMP-9 inhibitors with enhanced inhibitory activities and improved ADME properties. An efficacy study on reducing the ischemia-induced brain edema in the rat transient middle cerebral artery occlusion (tMCAo) model is also demonstrated.
本文描述了基于一系列α-羟基-β-N-二芳基醚磺酰胺异羟肟酸酯引入和优化α-氨基取代基的过程。该修饰产生了一系列具有增强抑制活性和改善的药代动力学性质的新型MMP-2/MMP-9抑制剂。还展示了在大鼠短暂性大脑中动脉闭塞（tMCAo）模型中减少缺血性脑水肿的功效研究。
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