摘要 |
Pyrrolopyridine derivatives (I) and their salts are new. Pyrrolopyridine derivatives of formula (I) and their salts are new. R1, R2H, halo or CF3, preferably R1 is Cl; R3, R4H or 1-4C alkyl; R : H or 1-3C alkyl; n : 1-2; X : a simple bond or O; and Ar1(hetero)aromatic e.g. phenyl, naphthyl, benzothiazolyl, 3,4-dihydro-1,4-benzoxazinyl, 1,3-benzodioxolyl, 1,4-benzodioxanyl or benzoxazolyl (all optionally substituted by 1-6C alkyl, 1-4C alkoxy or amino), preferably phenyl or heteroaromatic. Independent claims are included for the preparations 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. The ability of (I) to activate PPAR-alpha and/or PPAR-gamma was tested. The results showed that (I) exhibited an EC50 value of 4-1500 nM. |