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Phase II biotransformation of NSAID flobufen
Babú, Yogeeta ; Wsól, Vladimír (advisor) ; Nobilis, Milan (referee) ; Kuchař, Miroslav (referee)
Xenobiotic chemicals are chemicals foreign to life that are usually derived synthetically or from an abiotic process. The synthetic xenobiotic chemicals are often of enormous value to human society and are usually the majority of the chemicals in such important groups of substances as petrochemicals, pesticides, plastics and pharmaceuticals, where the term drug is usually applied when referring to xenobiotics. Biotransformation is a major mechanism for drug elimination, as they undergo biotransformation after they enter the body. Biotransformation, which almost always produces metabolites that are more polar than the parent compound, usually terminates the pharmacologic action of the parent drug and, via excretion, increases removal of the drug from the body. However, other consequences are possible, including similar or different pharmacologic activity, or toxicological activity. The routes by which drugs may be biotransformed are many and varied and include oxidation, reduction, hydrolysis and conjugation reactions, among others. It is important that these pathways are understood, as the route of metabolism of a drug can determine its ultimate pharmacological or toxicological activity. Drug biotransformation is divided into two phases: Phase I, or functionalisation reactions and Phase II, or conjugative...
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Phase II biotransformation of NSAID flobufen
Babú, Yogeeta ; Wsól, Vladimír (advisor) ; Nobilis, Milan (referee) ; Kuchař, Miroslav (referee)
Xenobiotic chemicals are chemicals foreign to life that are usually derived synthetically or from an abiotic process. The synthetic xenobiotic chemicals are often of enormous value to human society and are usually the majority of the chemicals in such important groups of substances as petrochemicals, pesticides, plastics and pharmaceuticals, where the term drug is usually applied when referring to xenobiotics. Biotransformation is a major mechanism for drug elimination, as they undergo biotransformation after they enter the body. Biotransformation, which almost always produces metabolites that are more polar than the parent compound, usually terminates the pharmacologic action of the parent drug and, via excretion, increases removal of the drug from the body. However, other consequences are possible, including similar or different pharmacologic activity, or toxicological activity. The routes by which drugs may be biotransformed are many and varied and include oxidation, reduction, hydrolysis and conjugation reactions, among others. It is important that these pathways are understood, as the route of metabolism of a drug can determine its ultimate pharmacological or toxicological activity. Drug biotransformation is divided into two phases: Phase I, or functionalisation reactions and Phase II, or conjugative...
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Synthesis, study and structure activity relationships of antiinflammatory drugs derived from leukotriens
Junek, Richard ; Hartl, Jiří (advisor) ; Beneš, Luděk (referee) ; Kuchař, Miroslav (referee) ; Kuneš, Jiří (referee)
7 Summary A series of arylalkanoic acids derivatives bearing methyl(phenethyl)amino groups were prepared and their antileukotrienic activities involving LTB4 were evaluated. Regression analysis of the first group of derivatives of arylacetic acid has shown a strong dependence of these activities on lipophilicity for both LTB4 receptor binding and inhibition of LTB4 biosynthesis, parabolic relationships were derived. The values of slopes of the ascending linear parts of these dependences indicate various types of hydrophobic binding at the site of ligand interaction with relevant biomacromolecules. Regression analysis showed the slightly different parabolic dependences of this activity on lipophilicity of -methyl and -unsubstituted alkanoic acids derivatives. The relationship derived for -unsubstituted alkanoic acids extended by group of similar derivatives of arylacetic acids was without any change of regression coefficients and statistical criteria. It was concluded, that the most active compounds belong to 2-arylpropanoic acids derivatives with lipophilicity close to log Popt (= 6.98). The antiinflammatory effect of the compounds under study was evaluated in three animal models of inflammation and their possible utilization in the treatment of ulcerative colitis was followed. It can be stated that the...
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