2,3-Dihydro-1-benzofuran-5-ols as analogues of alpha-tocopherol that inhibit in vitro and ex vivo lipid autoxidation and protect mice against central nervous system trauma
| Autor: | Verne J, Frank Bolkenius, M. A. Petty, J. M. Grisar |
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| Rok vydání: | 1995 |
| Předmět: |
Male
Antioxidant Tertiary amine medicine.medical_treatment Drug Evaluation Preclinical Neuroprotection Lipid peroxidation chemistry.chemical_compound Mice Superoxides Drug Discovery medicine Animals Craniocerebral Trauma Vitamin E Benzofurans Autoxidation Brain Free Radical Scavengers In vitro Cerebrovascular Disorders chemistry Biochemistry Molecular Medicine Lipid Peroxidation alpha-Tocopherol Ex vivo |
| Zdroj: | Journal of medicinal chemistry. 38(3) |
| ISSN: | 0022-2623 |
| Popis: | A series of alpha-tocopherol analogues was synthesized with potential therapeutic value for such pathological conditions as stroke and trauma. A set of criteria such as the inhibition of in vitro lipid peroxidation, superoxyl radical scavenging, and brain penetration, as measured by ex vivo inhibition of lipid peroxidation, was applied to select the most effective compound. 2,3-Dihydro-2,2,4,6,7-pentamethyl-3-[(4-methylpiperazino)methyl]-1 - benzofuran-5-ol dihydrochloride (22) was selected because of its superior antioxidant properties and better brain penetration. This compound also protected mice against the effects of head injury. The criteria thus turned out to be useful for the characterization of a neuroprotective analogue of alpha-tocopherol. |
| Databáze: | OpenAIRE |
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