| 摘要 |
Indole derivatives (I), are new. Indole derivatives of formula (I) and their salts are new. Ra, RbH, halo, 1-6C alkyl, CF3, CN, COR2, OR2 or phenyl (optionally substituted by 1-4C alkyl or CF3); R21-4C alkyl, CF3 or phenyl (optionally substituted by 1-4C alkyl or CF3); R2H or 1-4C alkyl; R : H or 1-3C alkyl; n : 1-3; X : a bond or O, and Ar1phenyl, naphthyl, quinolinyl, isoquinolinyl, pyridinyl, pyrazolyl, imidazolyl, isoxazolyl, thiazolyl, benzothiazolyl, 2,1,3-benzothiadiazolyl, 3,4-dihydro-1,4-benzoxazinyl, 5,6,7,8-tetrahydronaphthlaneyl, 1,2,3,4-tetrahydroquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, 1,2,3,4-tetrahydro-2-oxoquinolinyl, 3,4-dihydro-2H-benzopyranyl, indolyl, 2,3-dihydroindolyl, 2,3-dihydrobenzofuranyl, 1,3-benzodioxolyl, 1,4-benzodioxanyl or benzoxazolyl (all optionally substituted by halo, 1-6C alkyl, CF3, CN, CO-R2, OR2, NH-COR2, morpholinyl, amino or 4-morpholinosulfonyl). Independent claims are included for the preparation of (I). [Image] - ACTIVITY : Antilipemic; Antidiabetic; Cardiovascular-Gen.; Antiinflammatory; Neuroprotective; Nootropic; Antiparkinsonian; Anorectic; Antiarteriosclerotic; Cardiant; Hypotensive; Antiarthritic; Antirheumatic. - MECHANISM OF ACTION : Peroxisome proliferator activated receptor (PPAR) activator. In a test used to determine activation of PPAR-alpha and/or PPAR-gamma , results showed that (I) exhibited an EC50 value of 50 nM. |
