Inoue Munenori, Sumii Yuji, Shibata Norio
Sagami Chemical Research Institute, 2743-1 Hayakawa, Ayase, Kanagawa 252-1193, Japan.
Department of Life Science and Applied Chemistry, Department of Nanopharmaceutical Sciences, Nagoya Institute of Technology, Gokiso, Showa-ku, Nagoya 466-5888, Japan.
ACS Omega. 2020 Apr 22;5(19):10633-10640. doi: 10.1021/acsomega.0c00830. eCollection 2020 May 19.
Inspired by the success of fluorinated corticosteroids in the 1950s and fluoroquinolones in the 1980s, fluorine-containing pharmaceuticals, which are also known as fluoro-pharmaceuticals, have been attracting attention for more than half of a century. Presently, about 20% of the commercial pharmaceuticals are fluoro-pharmaceuticals. In this mini-review, we analyze the prevalence of fluoro-pharmaceuticals in the market and categorize them into several groups based on the chemotype of the fluoro-functional groups, their therapeutic purpose, and the presence of heterocycles and/or chirality to highlight the structural motifs, patterns, and promising trends in fluorine-based drug design. Our database contains 340 fluoro-pharmaceuticals, from the first fluoro-pharmaceutical, Florinef, to the latest fluoro-pharmaceuticals registered in 2019 and drugs that have been withdrawn. The names and chemical structures of all the 340 fluorinated drugs discussed are provided in the Supporting Information.
受20世纪50年代氟化皮质类固醇和80年代氟喹诺酮类药物成功的启发，含氟药物（也称为氟药物）已经吸引了半个多世纪的关注。目前，约20%的商业药物是氟药物。在这篇小型综述中，我们分析了氟药物在市场上的流行情况，并根据氟官能团的化学类型、治疗目的以及杂环和/或手性的存在将它们分为几个类别，以突出基于氟的药物设计中的结构基序、模式和有前景的趋势。我们的数据库包含340种氟药物，从第一种氟药物氟氢可的松到2019年注册的最新氟药物以及已撤市的药物。所讨论的所有340种氟化药物的名称和化学结构在支持信息中提供。
