In:
Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 56, No. 7 ( 2010-02-18), p. 941-945
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.
Type of Medium:
Online Resource
ISSN:
0022-3573
,
2042-7158
DOI:
10.1211/0022357023664
Language:
English
Publisher:
Oxford University Press (OUP)
Publication Date:
2010
detail.hit.zdb_id:
2041988-0
detail.hit.zdb_id:
2050532-2
SSG:
15,3
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