It has been pointed out that fluorine, due to its ability to increase the lipophilicity of the molecule, greatly affects the hydrophobic interaction between the drug molecule and the receptor..
How is fluorine used in medicine?
Fluorine is an indispensable tool in the medicinal chemists' toolbox. Due to its small size and strong electron-withdrawing property, fluorine is widely used in medicinal chemistry to improve a molecule's potency and permeability, modulate its pKa and lipophilicity, and control its conformation..
What are the biological uses of fluorine?
Biological role Fluoride is an essential ion for animals, strengthening teeth and bones. It is added to drinking water in some areas. The presence of fluorides below 2 parts per million in drinking water is believed to prevent dental cavities..
What are the medical uses of fluorine?
Fluoride protects teeth from the bacteria in plaque. It also promotes new bone formation. This is different than most medicines used for weak bones (osteoporosis), which fight osteoporosis by keeping bone from being broken down. People commonly use fluoride to prevent cavities..
What is the biological role of fluorine?
Biological role Fluoride is an essential ion for animals, strengthening teeth and bones. It is added to drinking water in some areas. The presence of fluorides below 2 parts per million in drinking water is believed to prevent dental cavities..
What is the role of fluorine in medicinal chemistry?
The main rationale for introducing fluorine into compounds is either to improve the metabolic stability, alter the physicochemical properties or improve the binding affinity of these compounds..
What is the use of fluorine in medicinal chemistry?
Fluorine substitution is being increasingly used to enhance the binding affinity of a compound to a target protein. This can occur by direct interaction of fluorine with the protein or indirectly by influencing the polarity of other groups of the compound which interact with the protein..
Where is fluorine used in medicine?
Fluorines also find their uses in common mineralocorticoids, a class of drugs that increase the blood pressure. Adding a fluorine increases both its medical power and anti-inflammatory effects. Fluorine-containing fludrocortisone is one of the most common of these drugs..
Why is fluorine used in medicinal chemistry?
As the C–F bond-dissociation energy (BDE) is very high (typically 109 kcal/mol or above), fluorine is often used by medicinal chemists to block a metabolic soft spot, which can reduce a molecule's metabolic clearance and/or prevent the formation of reactive metabolites..
Fluorination in most cases provides a better option due to its high lipophilicity and increases the absorption of drugs. So judicial use of fluorine atoms in the molecule increases the bioavailability and increases potency of drugs.
It has been pointed out that fluorine, due to its ability to increase the lipophilicity of the molecule, greatly affects the hydrophobic interaction between the drug molecule and the receptor.
The substitution of fluorine atoms for hydrogen atoms is a common method employed in medicinal chemistry to enhance ligand binding to proteins.
Provides a thorough overview of the role of fluorine in pharmaceutical science and development Includes chapters on fluorinated analogues of
Provides a thorough overview of the role of fluorine in pharmaceutical science and development; Includes chapters on fluorinated analogues
Is fluoride inorganic or organic?
Fluoride is present in human and animal serum in two forms, inorganic fluoride and organic fluorine [ 74–76 ]. The former consists of ionic and non‐ionic fluoride and the latter of fluorine covalently bound within an organic molecule originating from natural or industrial sources [ 77,78 ].
What is a fluorine atom?
The small and highly electronegative fluorine atom can play a remarkable role in medicinal chemistry. Selective installation of fluorine into a therapeutic or diagnostic small molecule candidate can enhance a number of pharmacokinetic and physicochemical properties such as:
improved metabolic stability and enhanced membrane permeation.
What is bioorganic and medicinal chemistry of fluorine?
Bioorganic and Medicinal Chemistry of Fluorine is divided in two main parts:
the first one deals with generalities con- cerning the specific properties of fluorinated compounds and their preparation; the second part is dedicated to the different classes of fluorinated compounds involved in bioorganic chemistry and to their biological properties.
Why are fluorinated chemicals important?
Fluorinated chemicals are of growing importance, withapplications in medicine. Fluorine substitution has profound effects on the properties of organiccompounds. The very high electronegativity of fluorine can modify electron distribution in themolecule, affecting its absorption, distribution and metabolism.
Bioorganic and medicinal chemistry of fluorine
Fluorine may interact with biological systems in the form of fluorine-containing compounds. Though elemental fluorine (F2) is very rare in everyday life, fluorine-containing compounds such as fluorite occur naturally as minerals. Naturally occurring organofluorine compounds are extremely rare. Man-made fluoride compounds are common and are used in medicines, pesticides, and materials. Twenty percent of all commercialized pharmaceuticals contain fluorine, including Lipitor and Prozac. In many contexts, fluorine-containing compounds are harmless or even beneficial to living organisms; in others, they are toxic.
Comparison of the nonsteroidal antiandrogen (NSAA) bicalutamide with other antiandrogens reveals differences between the medications in terms of efficacy, tolerability, safety, and other parameters. Relative to the other first-generation NSAAs, flutamide and nilutamide, bicalutamide shows improved potency, efficacy, tolerability, and safety, and has largely replaced these medications in clinical practice. Compared to the second-generation NSAAs, enzalutamide and apalutamide, bicalutamide has inferior potency and efficacy but similar tolerability and safety and a lower propensity for drug interactions.
Fluorine is a chemical element with the symbol F
Chemical element, symbol F and atomic number 9
Fluorine is a chemical element with the symbol F and atomic number 9. It is the lightest halogen and exists at standard conditions as a highly toxic, pale yellow diatomic gas. As the most electronegative reactive element, it is extremely reactive, as it reacts with all other elements except for the light inert gases.
