{"title":"氟化前列环素的合成及生物学研究。","authors":"W. E. Barnette","doi":"10.3109/10409238409102802","DOIUrl":null,"url":null,"abstract":"Fluorination has been used extensively in the steroid field to alter and/or enhance activity and to increase chemical or biological stability taking advantage of the similarity in size between hydrogen and fluorine and its strong electronegativity. Thus, it is not surprising to find that the same principle has been applied to prostaglandins, more specifically prostacyclin. The specific activity and high instability of Prostacyclin make it an ideal candidate for similar fluorination techniques. The design and preparation of fluorinated analogs with the aim of improving the chemical and metabolic stability of this important molecule will be discussed.","PeriodicalId":75744,"journal":{"name":"CRC critical reviews in biochemistry","volume":"94 1","pages":"201-35"},"PeriodicalIF":0.0000,"publicationDate":"1984-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10409238409102802","citationCount":"27","resultStr":"{\"title\":\"The synthesis and biology of fluorinated prostacyclins.\",\"authors\":\"W. E. Barnette\",\"doi\":\"10.3109/10409238409102802\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Fluorination has been used extensively in the steroid field to alter and/or enhance activity and to increase chemical or biological stability taking advantage of the similarity in size between hydrogen and fluorine and its strong electronegativity. Thus, it is not surprising to find that the same principle has been applied to prostaglandins, more specifically prostacyclin. The specific activity and high instability of Prostacyclin make it an ideal candidate for similar fluorination techniques. The design and preparation of fluorinated analogs with the aim of improving the chemical and metabolic stability of this important molecule will be discussed.\",\"PeriodicalId\":75744,\"journal\":{\"name\":\"CRC critical reviews in biochemistry\",\"volume\":\"94 1\",\"pages\":\"201-35\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1984-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.3109/10409238409102802\",\"citationCount\":\"27\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"CRC critical reviews in biochemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.3109/10409238409102802\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"CRC critical reviews in biochemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3109/10409238409102802","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
The synthesis and biology of fluorinated prostacyclins.
Fluorination has been used extensively in the steroid field to alter and/or enhance activity and to increase chemical or biological stability taking advantage of the similarity in size between hydrogen and fluorine and its strong electronegativity. Thus, it is not surprising to find that the same principle has been applied to prostaglandins, more specifically prostacyclin. The specific activity and high instability of Prostacyclin make it an ideal candidate for similar fluorination techniques. The design and preparation of fluorinated analogs with the aim of improving the chemical and metabolic stability of this important molecule will be discussed.