Department of Chemistry and Biochemistry, 1306 E. University Boulevard, University of Arizona , Tucson, Arizona 85721, United States.
J Med Chem. 2014 Dec 11;57(23):9764-73. doi: 10.1021/jm501105n. Epub 2014 Oct 6.
The diversity of elements among U.S. Food and Drug Administration (FDA) approved pharmaceuticals is analyzed and reported, with a focus on atoms other than carbon, hydrogen, oxygen, and nitrogen. Our analysis reveals that sulfur, chlorine, fluorine, and phosphorous represent about 90% of elemental substitutions, with sulfur being the fifth most used element followed closely by chlorine, then fluorine and finally phosphorous in the eighth place. The remaining 10% of substitutions are represented by 16 other elements of which bromine, iodine, and iron occur most frequently. The most detailed parts of our analysis are focused on chlorinated drugs as a function of approval date, disease condition, chlorine attachment, and structure. To better aid our chlorine drug analyses, a new poster showcasing the structures of chlorinated pharmaceuticals was created specifically for this study. Phosphorus, bromine, and iodine containing drugs are analyzed closely as well, followed by a discussion about other elements.
对美国食品和药物管理局 (FDA) 批准的药物中的元素多样性进行了分析和报告,重点关注碳、氢、氧和氮以外的原子。我们的分析表明,硫、氯、氟和磷约占元素取代的 90%,其中硫是第五大常用元素,紧随其后的是氯,然后是氟,最后是第八位的磷。其余 10%的取代由其他 16 种元素表示,其中溴、碘和铁最常见。我们分析的最详细部分集中在作为批准日期、疾病状况、氯附着和结构函数的氯化药物上。为了更好地帮助我们进行氯药物分析,专门为此研究创建了一个新的海报,展示了氯化药物的结构。还对含磷、溴和碘的药物进行了密切分析,然后讨论了其他元素。