Selective fluorination in drug design and development: an overview of biochemical rationales.
Several strategies used in the rational design and synthesis of fluorinated compounds as potential therapeutic agents are reviewed. Applications of fluorine substitution in empirical SAR studies for lead development also are discussed, along with the implications with respect to fluorine target interactions that can be derived from biological activities.
Kirk
Kenneth L
KL
Laboratory of Bioorganic Chemistry, National Institute of Diabetes, and Digestive and Kidney Diseases, National Institutes of Health, DHHS, Bethesda, MD 20892, USA. kennethk@bdg8.niddk.nih.gov
D000818:Animals; D001685:Biological Factors; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D005461:Fluorine / Q000737:chemistry*; D017611:Fluorine Compounds / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D001685:Biological Factors; D004791:Enzyme Inhibitors; D017611:Fluorine Compounds; D006845:Hydrocarbons, Fluorinated; D019275:Radiopharmaceuticals; D005461:Fluorine