（三氟甲基）二氮嗪类 TRPML1 配体的合成、X 射线结构测定和综合光化学特性研究。
Synthesis, X-ray Structure Determination, and Comprehensive Photochemical Characterization of (Trifluoromethyl)diazirine-Containing TRPML1 Ligands.
机构信息
Institute of Pharmaceutical and Biomedical Sciences, Johannes Gutenberg University Mainz, Staudinger Weg 5, 55128 Mainz, Germany.
Department of Chemistry, Biochemistry and Pharmaceutical Sciences, University of Bern, Freiestrasse 3, 3012 Bern, Switzerland.
出版信息
J Org Chem. 2021 May 7;86(9):6169-6183. doi: 10.1021/acs.joc.0c02993. Epub 2021 Apr 9.
Potential (trifluoromethyl)diazirine-based TRPML1 ion channel ligands were designed and synthesized, and their structures were determined by single-crystal X-ray diffraction analysis. Photoactivation studies via F NMR spectroscopy and HPLC-MS analysis revealed distinct kinetical characteristics in selected solvents and favorable photochemical properties in an aqueous buffer. These photoactivatable TRPML activators represent useful and valuable tools for TRPML photoaffinity labeling combined with mass spectrometry.
设计并合成了潜在的（三氟甲基）二氮嗪基 TRPML1 离子通道配体，并通过单晶 X 射线衍射分析确定了它们的结构。通过 19F NMR 光谱和 HPLC-MS 分析的光激活研究揭示了在选定溶剂中的不同动力学特征以及在水性缓冲液中的有利光化学性质。这些光可激活的 TRPML 激活剂是用于与质谱相结合的 TRPML 光亲和标记的有用和有价值的工具。
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