3-(SUBSTITUTION-PHENYLTHIO)-4-HYDROXYQUINOLINE-2(1H)-ONE DERIVATIVE AND METHOD FOR PREPARATION THEREOF

摘要

PURPOSE: Provided are 3-(substitution-phenylthio)-4-hydroxyquinoline-2(1H)-one derivative acting as an antagonist of excitoamino acid and useful to remedy or prevention of neurodegenerative disease, central nerve system disease and schizophrenia, and a method for preparation thereof. CONSTITUTION: 3-(substitution-phenylthio)-4-hydroxyquinoline-2(1H)-one is represented by the formula(1), wherein X is H, S, or NH; R1, R2, R3, and R4 is hydroxy, halogen, nitro, amino, haloalkyl, cyano, alkyl, alkenyl, alkinyl, azido, acylamino, substituted or nonsubstituted aryl, alkoxy, or substituted or nonsubstituted heterocyclic ring; and R5 and R6 is respectively, hydrogen, halogen, amino, carboxylate, thiol, haloalkyl, alkyl, alkenyl, alkinyl, azido, acylamino, sulfonyl, aminosulfonyl, substituted or nonsubstituted aryl, alkoxy, substituted or nonsubstituted heterocyclic ring, acyloxy, alkylthio, alkylcarboxylate, arylcarboxylate, aralkylcarboxlate, alkylester, arylester, aralkylester, urea, amidine, aralkyl, heteroarylalkyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, substituted(halo)-aralkylester, substituted(halo)-arylsulfonyl, heteroarylcarbonyl, aralkylthiourea, substituted(halo)-arylthiourea, alkoxycarbonyl, aminoalkyl or iminoaralkyl.