| Autor: |
Otake K; Research Laboratories, Kyoto Pharmaceutical Industries, Ltd., Nakagyo-ku, Kyoto, Japan., Azukizawa S, Takahashi K, Fukui M, Shibabayashi M, Kamemoto H, Kasai M, Shirahase H |
| Jazyk: |
angličtina |
| Zdroj: |
Chemical & pharmaceutical bulletin [Chem Pharm Bull (Tokyo)] 2011; Vol. 59 (7), pp. 876-9. |
| DOI: |
10.1248/cpb.59.876 |
| Abstrakt: |
2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor γ (PPARγ) and PPARα agonist activities and protein-tyrosine phosphatase 1B (PTP-1B) inhibitory activities. PPARγ agonist activity of 14 was comparable to that of rosiglitazone, and PTP-1B inhibitory activity was about 10-fold weaker than that of ertiprotafib, a PTP-1B inhibitor. Compound 14 showed high oral absorption in rats and potent hypoglycemic effects in KK-A(y) mice. In conclusion, 14 would be an excellent lead compound for a new type of anti-diabetic drug with triple actions. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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