基于点击化学的三氮唑并噻二唑 ΔF508-CFTR 校正剂的合成用于囊性纤维化。
Click-based synthesis of triazolobithiazole ΔF508-CFTR correctors for cystic fibrosis.
机构信息
Department of Chemistry, University of California, Davis, CA 95616, USA.
出版信息
Bioorg Med Chem. 2012 Sep 1;20(17):5247-53. doi: 10.1016/j.bmc.2012.06.046. Epub 2012 Jul 6.
Abstract
Copper catalyzed azide-alkyne cycloaddition (CuAAC) chemistry is reported for the construction of previously unknown 5-(1H-1,2,3-triazol-1-yl)-4,5'-bithiazoles from 2-bromo-1-(thiazol-5-yl)ethanones. These novel triazolobithiazoles are shown to have cystic fibrosis (CF) corrector activity and, compared to the benchmark bithiazole CF corrector corr-4a, improved logP values (4.5 vs 5.96).
摘要
铜催化的叠氮-炔环加成（CuAAC）反应被用于构建先前未知的 5-(1H-1,2,3-三唑-1-基)-4,5'-联噻唑，其原料为 2-溴-1-(噻唑-5-基)乙酮。这些新型的三唑并联噻唑具有囊性纤维化（CF）校正活性，与基准的联噻唑 CF 校正剂 corr-4a 相比，改善了 logP 值（4.5 对 5.96）。
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