File Name: fluoride and drugs thesis .zip
- Roles of Fluorine in Drug Design and Drug Action
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- Fluoride in Quaternary groundwater aquifer, Nile Valley, Luxor, Egypt
- Roles of Fluorine in Drug Design and Drug Action
Roles of Fluorine in Drug Design and Drug Action
DOI : The article discusses the basic properties of fluorine atom that have made it so useful in drug development. It presents several examples of therapeutically useful drugs acting against many life-threatening diseases along with the mechanism as to how fluorine influences the drug activity.
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.
Because of its small size, it hardly produces any steric effect, rather due to electronic properties enters into electrostatic and hydrogen-bond interactions.
Thus, it greatly affects the drug-receptor interaction and leads to increase the activity of the drugs. Keywords: Fluorine, fluorinated drugs, fluorinated pyrazoles, fluorinated benzazoles, fluorinated quinolones, hydrophobic. Abstract: The article discusses the basic properties of fluorine atom that have made it so useful in drug development. Volume 16 , Issue 10 , Journal Home. Graphical Abstract: Abstract: The article discusses the basic properties of fluorine atom that have made it so useful in drug development.
Zhou, Y. Filler, R. Fluorine in medicinal chemistry: a century of progress and a year retrospective of selected highlights.
Future Med. Kirk, K. Fluorine in medicinal chemistry: Recent therapeu-tic applications of fluorinated small molecules. Gakh, A. Extreme modulation properties of aromatic fluorine. Selective fluorination in drug design and development: an overview of biochemical rationales. Fluorine in pharmaceuticals: looking beyond intuition. Science , , , Isanbor, C. Fluorine in medicinal chemistry: A review of anti- cancer agents. Recent advances in fluorinated pharmaceuticals based on natural products. Prakesch, P.
Synthesis of fluoro analogues of unsaturated fatty acids and corre-sponding acyclic metabolites. Natarajana, R. Microbial cleavage of C-F bond. Fluorine in medicinal chemistry. ChemBioChem , , 5 5 , Jeschke, P.
The unique role of fluorine in the design of active ingredients for modern crop protection. Ojima, I. Use of fluorine in the medicinal chemistry and chemical biology of bioactive compounds--a case study on fluorinated taxane anticancer agents. Yoder, N. Fluorinated amino acids in protein design and engineering. Smart, B. E Fluorine substituent effects on bioactivity. Dax, K. Synthesis of deoxyfluoro sugars from carbohydrate precursors. Schlosser, M. Some influences of fluorine in bioorganic chemistry.
Bush, I. Metabolism of oxygenated steroids. Wettstein, A. Hansch, C. Bock, C. An ab initio study of the stability of the symmetrical and unsymmet-rical difluoroethylenes relative to ethylene and monofluoroethylene. Perkin Trans. Paulini, R. Orthogonal multipolar interactions in structural chemistry and biology. Black, W. Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Sani, M. The trifluoroethylamine function as peptide bond replacement. ChemMedChem , , 2 12 , Maryanoff, B. Westerik, J. Aldehydes as inhibitors of papain. Thompson, R. Use of peptide aldehydes to generate transition-state analogs of elastase. Biochemistry , , 12 1 , Shah, D.
Takahashi, L. Brady, K. Structure of chymotrypsin-trifluoromethyl ketone inhibitor complexes: comparison of slowly and rapidly equilibrating inhibitors. Biochemistry , , 29 33 , X-ray diffraction analysis of the inhibition of porcine pancreatic elastase by a peptidyl trifluoromethylketone. Veale, C. Nonpeptidic inhibitors of human leukocyte elastase. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidinone-containing trifluoromethyl ketones.
Peet, N. Angelastro, M. Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. Ogilvie, W. Abraham, Bhavsar, A. Peptidomimetic inhibitors of the human cytomegal-ovirus protease. LaPlante, S. Characterization of the human cytomegalovirus protease as an induced-fit serine protease and the implications to the design of mechanism-based inhibitors.
Warner, P. Non-peptidic inhibitors of human leukocyte elastase. The design and synthesis of pyridone-containing inhibitors. Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase. Ding, Y-S. Snyder, S. Chemistry of fluorine - 18 radiopharmaceuticals.
Handbook of Radiopharmaceuticals; Welch, M. J ; Redvanly, C. The unique role of halogen substituents in the design of modern agrochemicals. Pest Manag. Fried, J. Fluorine in health care: Organofluorine contain-ing blockbuster drugs. McGrath, N. A Graphical journey of innovative organic architectures that have im-proved our lives.
Ilardi, E. Data-mining for sulfur and fluorine: an evaluation of pharmaceuticals to reveal opportunities for drug design and discovery. LaRosa, J. Intensive lipid lowering with atorvastatin in patients with stable coronary disease.
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The occurrence of fluoride in ground water is the focus of the public and has attracted the attention of many scientists all over the world due to its importance in public health. Deficiency or increase of fluoride uptake is considered a public health problem due to the narrow permissible limit which should not exceed 1. The range of fluoride tolerance and toxicity is narrow. Deviation from the optimal levels therefore results in dental health effects such as caries and fluorosis. Many studies have found fluorosis to be invariably associated with high concentrations of fluoride in drinking water.
Gaffey Fall Henderson Fall Smith Winter Valkanas Fall Alakhzami Summer
ENVIRONMENTAL HEALTH CRITERIA FOR FLUORINE AND FLUORIDES. Rage. PREFACE. sample and to avoid contamination with outside fluoride and loss of fluoride after Stockholm, Karolinska Institute, Thesis. EKSTRAND, J. Assoc., MCQUEEN, E.G. () New Zealand Committee on Adverse Drug.
Fluoride in Quaternary groundwater aquifer, Nile Valley, Luxor, Egypt
Dental caries is still one of the major public health problems. The most effective way of caries prevention is the use of fluoride. The aim of our research was to review the literature about fluoride toxicity and to inform physicians, dentists and public health specialists whether fluoride use is expedient and safe.
Fluoride contamination has been recognised as one of the major problems worldwide, imposing a serious threat to human health and affecting the safety of drinking water. Adsorption is one of the widely considered appropriate technologies for water defluorination. The present study describes the preparation of a zirconium-based metal organic framework MOF adsorbent using a solvothermal method and its adsorption efficiency for removal of fluoride ions from water.
Roles of Fluorine in Drug Design and Drug Action
Recently, epidemiological studies have suggested that fluoride is a human developmental neurotoxicant that reduces measures of intelligence in children, placing it into the same category as toxic metals lead, methylmercury, arsenic and polychlorinated biphenyls. If true, this assessment would be highly relevant considering the widespread fluoridation of drinking water and the worldwide use of fluoride in oral hygiene products such as toothpaste. To gain a deeper understanding of these assertions, we reviewed the levels of human exposure, as well as results from animal experiments, particularly focusing on developmental toxicity, and the molecular mechanisms by which fluoride can cause adverse effects. Even for unusually high fluoride exposure levels, an MoE of at least ten was obtained. Furthermore, concentrations of fluoride in human plasma are much lower than fluoride concentrations, causing effects in cell cultures. In contrast, 21 of 23 recent epidemiological studies report an association between high fluoride exposure and reduced intelligence. The discrepancy between experimental and epidemiological evidence may be reconciled with deficiencies inherent in most of these epidemiological studies on a putative association between fluoride and intelligence, especially with respect to adequate consideration of potential confounding factors, e.
The discovery of fluoride in dentistry has revolutionized treatment modalities with a new aspect of prevention and conservation of tooth structure coming into foreplay. Since then, there has been a lot of research on both topical and systemic fluoridation in an overzealous attempt to control the most debilitating dental problem of caries. Although topical fluoride is still being widely used as a preventive measure for dental caries, systemic administration of the same has gained major criticism worldwide due to the low margin of safety of fluoride and no control over the amount of individual intake when administered on a community level. This problem is more prevalent in countries with presence of natural fluoride belts that extend from Turkey to China and Japan through Iraq, Iran, and Afghanistan increasing the chances of both dental and skeletal fluorosis and hence increasing the focus toward defluoridation. This historical review highlights the distribution of fluoride worldwide and in India and also discusses about the various claims of the antifluoride lobby.
Ingestion of excess fluoride, most commonly in drinking-water affects the teeth and bones. It results in major health disorders like dental fluorosis, skeletal fluorosis and non-skeletal fluorosis. People exposed to large amounts of fluoride show dental effects much earlier than the skeletal effects. Dental fluorosis affects children and discolours and disfigures the teeth. Skeletal fluorosis affects the bones and major joints of the body like neck, back bone, shoulder, hip and knee joints resulting in to severe pain, rigidity or stiffness in joints. Severe forms of skeletal fluorosis results in marked disability.
hygiene, and medical products including fluorinated drugs. Appl. Sci. , 10 The study of fluoride exposure and sleep patterns among a sample of adolescents living in the Ph.D. Thesis, University of Surrey,. Guildford.
Fluorochemicals are a widely distributed class of compounds and have been utilized across a wide range of industries for decades. Given the environmental toxicity and adverse health threats of some fluorochemicals, the development of new methods for their decomposition is significant to public health. However, the carbon—fluorine C—F bond is among the most chemically robust bonds; consequently, the degradation of fluorinated hydrocarbons is exceptionally difficult.
Size Range 20 to 34 , David Brunken-Deibert. Woolfork and David S. Entrapment of proteins in high-performance affinity columns for chromatographic studies of drug-protein interactions , Saumen Poddar, Elliott Rodriguez, Shiden Azaria, and David S.
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File Download FullText. Cheung, Y. Oral health issues in recovering drug addicts.
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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 element, it is extremely reactive, as it reacts with all other elements, except for argon , neon , and helium. Among the elements, fluorine ranks 24th in universal abundance and 13th in terrestrial abundance. Fluorite , the primary mineral source of fluorine which gave the element its name, was first described in ; as it was added to metal ores to lower their melting points for smelting , the Latin verb fluo meaning "flow" gave the mineral its name.
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Затем они приобретали как бы полупрозрачность, завершаясь у пола непроницаемой чернотой - посверкивающей черной глазурью кафеля, отливавшей жутковатым сиянием, создававшим какое-то тревожное ощущение прозрачности пола. Черный лед. В центре помещения из пола торчала, подобно носу исполинской торпеды, верхняя часть машины, ради которой было возведено все здание. Ее черный лоснящийся верх поднимался на двадцать три фута, а сама она уходила далеко вниз, под пол.
Чатрукьян посмотрел на телефонный аппарат и подумал, не позвонить ли этому парню: в лаборатории действовало неписаное правило, по которому сотрудники должны прикрывать друг друга. В шифровалке они считались людьми второго сорта и не очень-то ладили с местной элитой. Ни для кого не было секретом, что всем в этом многомиллиардном курятнике управляли шифровальщики. Сотрудников же лаборатории безопасности им приходилось терпеть, потому что те обеспечивали бесперебойную работу их игрушек. Чатрукьян принял решение и поднял телефонную трубку, но поднести ее к уху не успел.