期刊
MEDICINAL CHEMISTRY RESEARCH
卷 25, 期 7, 页码 1403-1410出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-016-1572-4
关键词
Quinoxaline-2,3-dione; Hydrazones; alpha-Amino-3-hydroxy-5-methylisoxazole propionate (AMPA); Demyelination; Neuroprotective
There is a growing interest in the design and synthesis of the quinoxaline-2,3-dione derivatives and hydrazones due to their neuroprotective activity, anticancer, anti-inflammatory, analgesic, anticonvuls ant, antiviral, antibacterial and antifungal activity, and hydra zone-based coupling methods are used in medical biotechnology to couple drugs and also to target antibodies. Different series of alpha-amino-3-hydroxy-5-methylisoxazole propionate receptor antagonists are described to be effective in the therapy of neurodegenerative disorders in the literature, one of which is based on the quinoxaline-2,3-dione structure, which has a high affinity and selectivity over receptors. Quinoxaline-2,3-bis hydrazone(s) were prepared by the nucleophilic addition reaction at the second and third position of quinoxaline-2,3-dione using different hydrazines (a-f) in conventional and microwave oven methods successfully with the good percentage of yields. The six synthesized compounds showed satisfactory analytical results. The oral administration of the synthesized drugs (20 mg/kg body weight) showed its curative and preventive effect against intracranial administration of ethidium bromide-induced demyelination in rats proved by the battery of behavioral and histological studies. The synthesized drugs are useful to counteract various demyelinating disorders which will be a great relief for our society. Further studies are needed on the molecular mechanisms of these compounds with neuroprotective activity.
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