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- Title
Inhibitory effect of pyridyloxy- or phenoxylphenoxyalkanate derivatives on rat lens aldose reductase and rat platelet aggregation.
- Authors
Soon Sung Lim; Kuk Hyun Shin; Sang Hoon Jung; Kye Jung Shin; Dong Chan Kim; Sang Woo Park; Hyun Kyung Shin; Sam Rok Keum
- Abstract
The therapeutic potential of aldose reductase inhibitors for the prevention of the secondary complications of diabetes has been extensively reported. On the other hand, the hyperaggregability of platelets in diabetic patients has also been reported as a cause of chronic diabetic complications. The purpose of this study was to develop new compounds with these dual effects from pyridyloxy- or phenoxylphenoxyalkanate synthesized derivatives and examine the effect of their structure-activity relationships on the inhibition of rat lens aldose reductase (RLAR) as well as on platelet aggregation. 2-[4-(2,6-dichloro-3-methyl-phenoxy)-3-nitro-phenoxy]-propionic acid (3) exhibited the most potent inhibitory effect (IC50 = 3.0 ± 0.21 μM), comparable to tetramethylene glutaric acid (IC50 = 6.1 ± 0.2 μM), which is used as a positive control on RLAR, and showed potent inhibitory activities on rat platelet aggregation induced by ADP and collagen (IC50 = 0.093 ± 0.01 and 0.032 ± 0.01 μM, respectively) comparable with aspirin (IC50 = 0.15 ± 0.05 and 0.047 ± 0.01 μM, respectively), used as a positive control.
- Subjects
DIABETES; CARBOHYDRATE intolerance; FATTY acids; COLLAGEN
- Publication
Journal of Pharmacy & Pharmacology, 2004, Vol 56, Issue 7, p941
- ISSN
0022-3573
- Publication type
Article