- CYP267A1 and CYP267B1 from sorangium cellulosum so ce56 are highly versatile drug metabolizers
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The guidelines of the Food and Drug Administration and International Conference on Harmonization have highlighted the importance of drug metabolites in clinical trials. As a result, an authentic source for their production is of great interest, both for t
- Kern, Fredy,Khatri, Yogan,Litzenburger, Martin,Bernhardt, Rita
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supporting information
p. 495 - 504
(2016/04/05)
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- Monooxygenation of aromatic compounds by dioxygen with bioinspired systems using non-heme iron catalysts and tetrahydropterins: Comparison with other reducing agents and interesting regioselectivity favouring meta-hydroxylation
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Monooxygenation of aromatic compounds by dioxygen in the presence of catalytic amounts of an iron(II) salt and tetrahydropterins as reducing agents occurs with a regioselectivity favouring meta-hydroxylation of arenes bearing an electron-donating substituent, such as anisole, phenetole, toluene, and ethylbenzene. Comparison of similar systems using various reducing agents showed that only tetrahydropterins and ascorbate led to such a major meta-hydroxylation. The tetrahydropterin- and ascorbate-dependent systems should be useful for the preparation of meta-hydroxylated metabolites of aromatic drugs, as shown here in the case of diclofenac.
- Mathieu, Delphine,Bartoli, Jean Fran?ois,Battioni, Pierrette,Mansuy, Daniel
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p. 3855 - 3862
(2007/10/03)
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- Hepatic metabolism of diclofenac: Role of human CYP in the minor oxidative pathways
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The aim of this study was to re-examine the human hepatic metabolism of diclofenac, with special focus on the generation of minor hydroxylated metabolites implicated in the idiosyncratic hepatotoxicity of the drug. Different experimental approaches were u
- Bort, Roque,MacE, Katherine,Boobis, Alan,Gomez-Lechon, Maria-Jose.,Pfeifer, Andrea,Castell, Jose
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p. 787 - 796
(2007/10/03)
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- Synthesis and quantitative structure-activity relationships of diclofenac analogues
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The synthesis of a series of 2-anilinophenylacetic acid, close analogues of diclofenac, is described. These compounds were tested in two models used for evaluating the activity of nonsteroidal antiinflammatory drugs (NSAID's), inhibition of cyclooxygenase enzyme activity in vitro, and adjuvant-induced arthritis (AdA) in rats. Statistically significant correlations were found between the inhibitory activities of the compounds in these two models, indicating that cyclooxygenase inhibition seems to be the underlying mechanism for the antiinflammatory activity of these compounds. Quantitative structure-activity relationship (QSAR) analysis revealed that the crucial parameters for activity in both models were the lipophilicity and the angle of twist between the two phenyl rings. Optimal activities were associated with halogen or alkyl substituents in both ortho positions of the anilino ring. Compounds with OH groups in addition to two ortho substituents or compounds with only one or no ortho substituents were less active.
- Moser,Sallmann,Wiesenberg
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p. 2358 - 2368
(2007/10/02)
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