Benedetto Tiz Davide, Bagnoli Luana, Rosati Ornelio, Marini Francesca, Sancineto Luca, Santi Claudio
Group of Catalysis, Synthesis and Organic Green Chemistry, Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06100 Perugia, Italy.
Molecules. 2022 Mar 2;27(5):1643. doi: 10.3390/molecules27051643.
This review describes the recent Food and Drug Administration (FDA)-approved drugs (in the year 2021) containing at least one halogen atom (covalently bound). The structures proposed throughout this work are grouped according to their therapeutical use. Their synthesis is presented as well. The number of halogenated molecules that are reaching the market is regularly preserved, and 14 of the 50 molecules approved by the FDA in the last year contain halogens. This underlines the emergent role of halogens and, in particular, of fluorine and chlorine in the preparation of drugs for the treatment of several diseases such as viral infections, several types of cancer, cardiovascular disease, multiple sclerosis, migraine and inflammatory diseases such as vasculitis.
本综述描述了近期（2021年）美国食品药品监督管理局（FDA）批准的含有至少一个（共价结合的）卤原子的药物。贯穿本研究提出的结构根据其治疗用途进行了分类。还介绍了它们的合成方法。进入市场的卤化分子数量一直保持稳定，去年FDA批准的50种分子中有14种含有卤素。这突出了卤素，特别是氟和氯在制备用于治疗多种疾病（如病毒感染、多种癌症、心血管疾病、多发性硬化症、偏头痛以及血管炎等炎症性疾病）的药物中的重要作用。
