Laboratorio Síntesis Orgánica, Instituto de Química de Recursos Naturales, Universidad de Talca, Casilla 747, Talca 3460000, Chile.
Molecules. 2012 Oct 15;17(10):12072-85. doi: 10.3390/molecules171012072.
(E)-2-(benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles are described as a new class of selective inhibitors of acetylcholinesterase (AChE). The most potent compound in the series exhibited good AChE inhibitory activity (IC₅₀ = 64 µM). Compound 7f was found to be more selective than galanthamine in inhibiting AChE and it showed a moderate selectivity index. Kinetic studies on AChE indicated that a competitive type of inhibition pattern exist for these acrylonitrile derivates. Molecular docking models of the ligand-AChE complexes suggest that compound 7 g is located on the periphery of the AChE active site.
(E)-2-(苯并[d]噻唑-2-基)-3-杂芳基丙烯腈被描述为一类新型的乙酰胆碱酯酶 (AChE) 选择性抑制剂。该系列中最有效的化合物表现出良好的 AChE 抑制活性（IC₅₀ = 64 µM）。研究发现化合物 7f 在抑制 AChE 方面比加兰他敏更具选择性，并且具有适度的选择性指数。对 AChE 的动力学研究表明，这些丙烯腈衍生物存在竞争性抑制模式。配体-AChE 复合物的分子对接模型表明，化合物 7 g 位于 AChE 活性部位的外围。
