Studies on Disease-Modifying Antirheumatic Drugs. IV. Synthesis of Novel Thieno[2,3-b : 5,4-c']dipyridine Derivatives and Their Anti-inflammatory Effect

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The syntheses and anti-inflammatory activities of novel thieno[2,3-b]pyridine and thieno[2,3-b : 5,4-c']-dipyridine derivatives are desrcibed. These compounds were designed by modification of the quinoline template of a new type of disease-modifying antirheumatic drug (DMARD), TAK-603,and prepared by the Friedlander reaction as a key reaciton. Their anti-inflammatory effects were evaluated using an adjuvant arthritis rat model. Most of the compounds which included a dithylamino moiety in the side chain had potent anti-inflammatory effect. In particular, ethyl 2-(diethylaminomethyl)-4-(3,4-dimethoxyphenyl)thieno[2,3-b : 5,4-c']dipyridine-3-carboxylate (21) exhibitied more potent activity than TAK-603.
公益社団法人日本薬学会の論文
1999-07-15