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  • Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported. The conjugates consist of, on one side, the therapeutically important drug succinobucol ([4-{2,6-di-tert-butyl-4-[(1-{[3-tert-butyl-4-hydroxy-5-(propan-2-yl)phenyl]sulfanyl}ethyl)sulfanyl]phenoxy}-4-oxo-butanoic acid]) possessing an antioxidant and anti-inflammatory activity, and on the other side, plant stanol/sterols (stigmastanol, β-sitosterol and stigmasterol) possessing an ability to lower the blood cholesterol level. A cholesterol-succinobucol prodrug was also prepared in order to enhance the absorption of succinobucol through the intestinal membrane into the organism and to target the drug into the place of lipid metabolism—The enterohepatic circulation system.
  • Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported. The conjugates consist of, on one side, the therapeutically important drug succinobucol ([4-{2,6-di-tert-butyl-4-[(1-{[3-tert-butyl-4-hydroxy-5-(propan-2-yl)phenyl]sulfanyl}ethyl)sulfanyl]phenoxy}-4-oxo-butanoic acid]) possessing an antioxidant and anti-inflammatory activity, and on the other side, plant stanol/sterols (stigmastanol, β-sitosterol and stigmasterol) possessing an ability to lower the blood cholesterol level. A cholesterol-succinobucol prodrug was also prepared in order to enhance the absorption of succinobucol through the intestinal membrane into the organism and to target the drug into the place of lipid metabolism—The enterohepatic circulation system. (en)
Title
  • Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability
  • Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability (en)
skos:prefLabel
  • Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability
  • Succinobucol’s New Coat - Conjugation with Steroids to Alter Its Drug Effect and Bioavailability (en)
skos:notation
  • RIV/61389030:_____/11:00368252!RIV12-AV0-61389030
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  • I, P(2B06024), P(ED0030/01/01), P(GA203/09/2037), P(OC10001), Z(AV0Z40550506), Z(AV0Z50380511)
http://linked.open...iv/cisloPeriodika
  • 11
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  • 233336
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  • RIV/61389030:_____/11:00368252
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  • succinobucol; phytosterol; atherosclerosis (en)
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  • CH - Švýcarská konfederace
http://linked.open...ontrolniKodProRIV
  • [2F6CEB8A8DD5]
http://linked.open...i/riv/nazevZdroje
  • Molecules
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  • 16
http://linked.open...iv/tvurceVysledku
  • Buřičová, Lucie
  • Drašar, P.
  • Jurček, Ondřej
  • Kolehmainen, E. T.
  • Wimmer, Zdeněk
  • Ulrichová, J.
  • Horníček, Jan
  • Galandáková, A.
  • Ikonen, S.
  • Wimmerová, Martina
http://linked.open...ain/vavai/riv/wos
  • 000297697200038
http://linked.open...n/vavai/riv/zamer
issn
  • 1420-3049
number of pages
http://bibframe.org/vocab/doi
  • 10.3390/molecules16119404
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