一种简便的双（异恶唑）方法，有望成为 AMPA 受体的配体。
A Facile Approach to Bis(isoxazoles), Promising Ligands of the AMPA Receptor.
机构信息
Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russia.
Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, 142432 Moscow, Russia.
出版信息
Molecules. 2021 Oct 23;26(21):6411. doi: 10.3390/molecules26216411.
A convenient synthetic approach to novel functionalized bis(isoxazoles), the promising bivalent ligands of the AMPA receptor, was elaborated. It was based on the heterocyclization reactions of readily available electrophilic alkenes with the tetranitromethane-triethylamine complex. The structural diversity of the synthesized compounds was demonstrated. In the electrophysiological experiments using the patch clamp technique on Purkinje neurons, the compound 1,4-phenylenedi(methylene)bis(5-aminoisoxazole-3-carboxylate) was shown to be highly potent positive modulator of the AMPA receptor, potentiating kainate-induced currents up to 70% at 10 M.
一种方便的合成新型功能化双（异恶唑）的方法，即 AMPA 受体有前途的双价配体，被详细阐述。它基于易得的亲电烯烃与四硝甲烷-三乙胺复合物的杂环化反应。合成化合物的结构多样性得到了证明。在使用膜片钳技术在浦肯野神经元上进行的电生理实验中，化合物 1,4-亚苯基二（亚甲基）双（5-氨基异恶唑-3-羧酸酯）被证明是 AMPA 受体的高效正变构调节剂，在 10 μM 时将海人藻酸诱导的电流增强高达 70%。
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