Department of Biological, Chemical, and Physical Sciences, Illinois Institute of Technology, Chicago, IL 60616, USA.
Future Med Chem. 2009 Aug;1(5):777-91. doi: 10.4155/fmc.09.65.
This perspective explores the origins of both fluorine and medicinal chemistry a century ago and traces the early history of the intersection of these areas and the subsequent roles that fluorine has played in advancing medicinal innovations and diagnoses during the past 60 years. The overview highlights remarkable breakthroughs in many diverse areas of medicinal chemistry, including inter alia, anesthetics, steroidal and nonsteroidal anti-inflammatory drugs, anticancer and antiviral agents, CNS medications, antibacterials and cholesterol biosynthesis inhibitors. The increasing use of fluorine-18-labeled radiotracers in PET for diagnostic imaging of the brain, heart and in oncology is briefly presented. The signature roles of fluorine in medicinal chemistry are now firmly established. The presence of fluorine in pharmaceuticals has had a major impact on a plethora of important medical applications, such as those cited above. Fluorine will very likely continue to contribute significantly by playing multifaceted roles in enhancing future medical advances.
这篇观点文章探讨了一个世纪前氟化学和药物化学的起源，并追溯了这两个领域交叉的早期历史，以及在过去 60 年中氟在推动药物创新和诊断方面所扮演的后续角色。该综述强调了药物化学许多不同领域的显著突破，包括但不限于麻醉剂、甾体和非甾体抗炎药、抗癌和抗病毒药物、中枢神经系统药物、抗菌药和胆固醇生物合成抑制剂。简要介绍了氟-18 标记放射性示踪剂在正电子发射断层扫描（PET）中用于脑、心脏和肿瘤诊断成像的应用日益增加。氟在药物化学中的标志性作用现在已经确立。氟在药物中的存在对许多重要的医学应用产生了重大影响，如上面引用的那些。氟很可能通过在增强未来医学进展方面发挥多方面的作用继续做出重大贡献。
