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- W2085053424 abstract "2,2-Dimethylchromenes and chromans containing cytochrome P-450 resistant 2,2,2-trifluoroethoxy aryl substituents were synthesized and their activity as lipid peroxidation inhibitors evaluated and compared with that exhibited by the corresponding non-fluorinated derivatives. Lipid peroxidation was stimulated in rat liver microsomes by addition of Fe—ascorbate or NADPH, and determined with the TBARS (thiobarbituric acid reactive substances) test. In assays using Fe—ascorbate stimulation, only those derivatives with a OH group at C6 (i.e. 6 and 12) elicited good inhibitory activities (IC50 = 6.0 and 5.3 μM, respectively). In respect to the NADPH dependent incubations, inhibitory activity of compound 11 (IC50 = 6.0 μM) was the highest found within the 6,7-dialkoxy derivatives tested. Results on metabolism assays with this compound showed the generation of phenol 12 (i.e. the putative active antioxidant species); on the other hand, no metabolite resulting from dealkylation at C7 was detected, thus confirming the resistance conferred by the CF3CH2O group to the cytochrome P-450 promoted cleavage. Finally, in assays where incubations in the presence of NADPH were prolonged up to three hours, inhibitory activity of the non-fluorinated 6,7-dialkoxychroman 8 remained constant, thus suggesting that a continued release of the species responsible for the inhibitory activity was produced. However, inhibition elicited by the fluorinated analog 11 showed a small decrease during the third hour of incubation. This decrease could be attributed to the slight inhibition of the cytochrome P-450 metabolism exerted by substrates bearing the CF3CH2O substituent, which would decelerate the generation of the active phenol species. Concerning the derivatives with a free hydroxyl at C6 (i.e. compounds 9 and 12), although their inhibitory activities decreased during the period studied, that of fluorinated compound 12 was more persistent." @default.
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- W2085053424 date "1993-09-01" @default.
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- W2085053424 title "Inhibition of rat liver microsomal lipid peroxidation elicited by 2,2-dimethylchromenes and chromans containing fluorinated moieties resistant to cytochrome P-450 metabolism" @default.
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- W2085053424 doi "https://doi.org/10.1016/s0968-0896(00)82124-0" @default.
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