• 약학회지
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• 제53권2호
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• pp.89-92
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• 2009

Dicaffeoyltartaric acid has a structural feature consisting of two caffeic acid units separated by tartaric acid linker and has been found to be a potent inhibitor of HIV-1 integrase and an antioxidant. In this study, bis(pyronyl)acrylic acid esters joined through a 5-membered ring as a linker were synthesized as the analogues of dicaffeoyltartaric acid.

• 약학회지
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• 제39권5호
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• pp.565-568
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• 1995

A new antiplatelett agent, aspalatone ([3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) was demonstrated to inhibit MDA generation from arachidonic acid catalyzed by partially purified bovine seminal vesicle cyclooxygenase. This inhibition was also observed with acetylsalicylic acid. The results suggest that the mechanism for the antiplatelet effect of aspalatone is, like acetylsalicylic acid, due to its inhibition of cyclooxygenase.

• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.299-302
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• 2011

• Bulletin of the Korean Chemical Society
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• 제31권7호
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• pp.2036-2038
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• 2010

• Biomolecules & Therapeutics
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• 제4권2호
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• pp.122-126
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• 1996

In vitro inhibitory effect of aspalatone ((3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) on collagen-, ADP-, and epinephrine-induced platelet aggregation in human platelet rich plasma (PRP) was compared with the effects of reference drugs (acetylsalicylic acid, cilostazol and ticlopidine). Aspalatone inhibited time and dose dependently human platelet aggregation induced by collagen; relative potency was in the order of cilostazol>acetylsalicylic acid>aspalatone>ticlopidine. Aspalatone, like acetylsalicylic acid, potently inhibited only the secondary phase of ADP-and epinephrine-induced aggregation. Thromboxane $B^2$ production evoked by collagen in human PRP was inhibited significantly and concentration-dependently by aspalatone and acetylsalicylic acid. These results were in agreement with the earlier studies in which the antiplatelet action of aspalatone was indicated to be due to the inhibition of platelet cyclooxygenase activity (Han et al., Arzneim. Forsch./Drug Res. 44(II), 1122, 1994; Suh and Han, Yakhak Hoeji 39, 565, 1995). In addition, the inhibitory activity of aspalatone on the platelet aggregation appears to be inversely related to the rate of nonspecific deacetylation of the drug in plasma.