近日，湖南大学邱仁华团队研究了机制驱动的生物活性吲唑框架：光引发脱甲基芳构化合成和生物传感应用。相关论文发表在2025年5月21日出版的《德国应用化学》杂志上。

吲哚唑框架是药物化学和荧光偶联设计的关键。研究组报道了一种光化学策略，通过紫外线诱导的亚硝基中间体实现N-甲基胺的高效N-去甲基化和芳香环化，为结构多样的2H-茚唑支架提供了一种环境友好的途径。

与传统方法不同，该方法显示出与各种烷基/芳基胺的特殊底物相容性，促进了功能化2H-茚唑模块的流线型组装。该方法已成功地应用于合成靶向G-四聚物的修饰药物和肿瘤特异性荧光探针。生理毒性和细胞荧光成像的初步评估突出了其生物医学潜力，将这些策略建立为药理学开发和生物成像研究的潜在工具。

附：英文原文

Title: Mechanism-Driven Bioactive Indazole Frameworks: Photoinitiated Demethylation-Aromatization Synthesis and Biosensing Applications

Author: Yi-Feng Ou, Songhua Chen, Qian Lei, Yang Shen, Niu Tang, Yongbo Zhou, Shuang-Feng Yin, Nobuaki Kambe, Lin Yuan, Renhua Qiu

Issue&Volume: 2025-05-21

Abstract: Indazole frameworks are pivotal in medicinal chemistry and fluorescent conjugate design. Herein, we reported a photochemical strategy enabling efficient N-demethylation and aromatic cyclization of N-methyl amines via UV-induced nitroso intermediates, offering an environmentally benign route to structurally diverse 2H-indazole scaffolds. Diverging from conventional methods, this protocol demonstrates exceptional substrate compatibility with various alkyl/aryl amines, facilitating streamlined assembly of functionalized 2H-indazole modules. The methodology has been successfully applied to synthesize modified drugs and tumour-specific fluorescent probes targeting G-quadruplexes. Preliminary evaluations of physiological toxicity and cellular fluorescence imaging highlight their biomedical potential, establishing these strategies as potential tools for pharmacological development and bioimaging research.

DOI: 10.1002/anie.202507163

Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202507163