NOVEL HETEROCYCLIC DERIVATIVES AND MEDICINAL USE THEREOF

摘要

Tetrahydroisoquinoline-carboxylic acid compounds (I) are new. Tetrahydroquinoline compounds of formula (I) and their salts are new; [Image] R 1H or 1-6C alkyl; R 2COCR 4=CR 4R 5, COCtriple boundCR 6, COCOR 7, NR 8COR 9 or aryl; R 54-8C alkyl, 2-8C alkenyl, aryl or aromatic heterocyclyl; R 61-8C alkyl; R 71-8C alkyl or 1-8C alkoxy; R 4, R 8H or 1-4C alkyl; R 91-8C alkyl, 1-8C alkoxy, aryl or aryl-1-3C alkoxy; R 3H or 1-4C alkyl; X : O or S; R 2 0optionally substituted phenyl; n : 1-4. ACTIVITY : Antidiabetic; Antilipemic; Antiarteriosclerotic; Anorectic, Antiinflammatory. Administration of 2-(2,4-hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-(3S)-carboxylic acid (Ia) to db/db mice at 3 mg/kg/day orally reduced blood glucose levels by 59.9% and blood triglyceride levels by 77.1% after 2 weeks. MECHANISM OF ACTION : PPAR-Antagonist; Hypoglycemic.