Anacor Pharmaceuticals Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA.
Bioorg Med Chem Lett. 2013 Mar 15;23(6):1680-3. doi: 10.1016/j.bmcl.2013.01.072. Epub 2013 Jan 29.
A series of novel 6-(aminomethylphenoxy)benzoxaborole analogs was synthesized for the investigation of the structure-activity relationship of the inhibition of TNF-alpha, IL-1beta, and IL-6, from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compounds 9d and 9e showed potent activity against all three cytokines with IC50 values between 33 and 83nM. Chloro substituted analog 9e (AN3485) is considered to be a promising lead for novel anti-inflammatory agent with a favorable pharmacokinetic profile.
为了研究 6-（氨甲基苯氧基）苯并硼杂环戊烷类似物抑制脂多糖刺激的外周血单个核细胞产生 TNF-α、IL-1β 和 IL-6 的构效关系，我们合成了一系列新型的 6-（氨甲基苯氧基）苯并硼杂环戊烷类似物。化合物 9d 和 9e 对三种细胞因子均具有较强的抑制活性，IC50 值在 33 到 83nM 之间。氯取代的类似物 9e（AN3485）被认为是一种具有良好药代动力学特性的新型抗炎药的有前途的先导化合物。
