7-HYDROXY-6-METHOXY-1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES HAVING EFFECTS OF PREVENTING AND TREATING DEGENERATIVE AND INFLAMMATORY DISEASES

摘要

A novel compound is provided to inhibit increase of NO and superoxide in active microglia, gene expression of TNF-alpha, IL-1beta, inducible-type NO synthase and cyclooxygenase-2, translocation of NF-kappaB into the nucleus, gene expression of GTP cyclohydrolase I and over-production of BH4, reduce generation of reactive oxidative species(ROS) and show significant protecting effect on dopaminergic neuron damage caused by the active microglia, thereby being effective for preventing and treating inflammatory diseases and degenerative nerve diseases. A 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivative is represented by a formula(1), wherein R1 is H, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, CH2CH(CH3)2, C6H5, CH2C6H5, C4H7, C3H5 or C6H11 and R2 is COCH2CH3, COCH2CH2CH3, COCH(CH3)2, COCH2CH(CH3)2 or COC6H11. A pharmaceutical composition for preventing and treating inflammatory diseases comprises the 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivative as an effective ingredient.