| 摘要 |
PURPOSE: Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their uses as therapeutics are provided. The compounds have low toxicity and improved lipid peroxidation(LPO) inhibiting activity, therefore they effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The dialkylhydroxybenzoic acid derivatives containing metal chelating groups are characteristically represented by formula(I), wherein R1 is hydrogen, or straight or branched alkyl; R2 is hydrogen or alkyl; 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 dialkylhydroxybenzoic acid derivatives are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.
|
