Zheng Xunan, Ma Zhengning, Zhang Dawei
College of Chemistry, Jilin University, Changchun 130012, China.
College of Plant Science, Jilin University, Changchun 130062, China.
Pharmaceuticals (Basel). 2020 Mar 3;13(3):37. doi: 10.3390/ph13030037.
Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activities, and are widely researched and applied by pharmaceutical companies for drug discovery. The van Leusen reaction based on tosylmethylisocyanides (TosMICs) is one of the most appropriate strategies to synthetize imidazole-based medicinal molecules, which has been increasingly developed on account of its advantages. In this review, we summarize the recent developments of the chemical synthesis and bioactivity of imidazole-containing medicinal small molecules, utilizing the van Leusen imidazole synthesis from 1977.
咪唑及其衍生物是药物化学中最重要且最常见的杂环之一。由于其特殊的结构特征，这些化合物展现出广泛的显著药理或生物活性，并且被制药公司广泛研究和应用于药物研发。基于对甲苯磺酰甲基异腈（TosMICs）的范勒森反应是合成基于咪唑的药用分子的最合适策略之一，因其优势而得到了越来越多的发展。在本综述中，我们总结了含咪唑药用小分子的化学合成及生物活性的最新进展，采用了始于1977年的范勒森咪唑合成法。
