| 摘要 |
PURPOSE: N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups, a preparation process thereof and the uses thereof as therapeutics are provided. The compounds have low toxicity and improved lipid peroxidation(LOP) inhibiting activity, so that they can effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups represented by formula(I) are provided, wherein R1 is branched alkyl, aralkyl, aryl or substituted aryl; R2 is hydrogen or COR6 wherein R6 is alkyl or aryl; R3 is CO2H, CONH2 or CONR4R5; R4 is hydrogen, alkyl, or aryl; and R5 is unsaturated or saturated heterocyclic having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl and tetrazolyl. The N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.
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