• YAKHAK HOEJI
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• v.45 no.6
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• pp.565-569
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• 2001

Five novel cinmetacin amide derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity was compared with cinmetacin. Cinmetacin and hydroxysuccinimide were reacted with dicyclohexyl carbodiimide to give cinmetacin active ester (4), which was treated with amines to yield cinmetacin amides (5-9). Compounds (5) and (9) gave stronger analgesic activity than cinmetacin and compounds (5), (6), (9) showed comparable antiinflammatory activity to cinmetacin.

• YAKHAK HOEJI
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• v.45 no.1
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• pp.1-6
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• 2001

Nine cinmetacin derivatives as potential nonsteroidal analgesic and antiinflammatory compounds were prepared and their analgesic-antiinflammatory activity was compared with cinmetacin. Salicylic acid and phenols were reacted with dicyclohexyl carbodiimide (DCC) to give phenol salicylates (1-4). Cinmetacin was treated with DCC and phenol derivatives to yield cinmetacin esters (5-13). Compounds (5, 7, 8, 10, 12, and 13) showed stronger analgesic activity than cinmetacin, but only compound (5) showed comparable antiinflammatory activity to cinmetacin.

• YAKHAK HOEJI
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• v.35 no.2
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• pp.73-84
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• 1991

Quinoline, pyrazolo-[5, 4-b]-pyridine, isoxazolo-[5, 4-b]-pyridine, pyrazolo-[4, 3-c]-quinoline, isoxazolo-[5, 4-e]-thiazine, and isothiazolo-[5, 4-e]-thiazine derivatives were prepared as possible antiinflammatory agents. Some of the synthesized compounds showed antiinflammatory activities comparable to Aspirin and Naproxen.

• Natural Product Sciences
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• v.2 no.1
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• pp.1-8
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• 1996

Flavonoids are widely distributed polyphenol compounds in plant kingdom and known to possess varieties of biological/pharmacological activities in vitro and in vivo. A search for antiinflammatory/immunoregulatory flavonoids as potential therapeutic agents has been continued, since serious side effects of currently used nonsteroidal and steroidal antiinflammatory drugs limit their long term uses for the inflammatory disorders. In this reserch, various flavonids were isolated and tested for their in vivo antiinflammatory activity and in vitro inhibitory activity of lymphocyte proliferation. Using a mouse ear edema assay, it was found that certain flavones/flavonols possess mild antiinflammatory activity and a C-2,3-double bond might be essential. Isoflavones were less active. These flavonoids inhibited in vitro lymphocyte proliferation, relatively specific for T-cell proliferation $(IC_{50}=1-10\;{\mu}M)$ and the inhibition was reversible. We have also tested several biflavonoid derivatives, since we recently found that biflavones were phospholipase $A_2$ inhibitors. It was demonstrated that biflavones such as ochnaflavone and ginkgetin inhibited lymphocyte proliferation induced by both concanavaline A and lipopolysaccharide. The inhibition was irreversible in contrast to that of flavones/flavonols. And antiinflammatory activity of biflavonoids are discussed.

• YAKHAK HOEJI
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• v.36 no.1
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• pp.7-11
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• 1992

2-Substituted benzimdazoles were prepared by reacting o-phenylenediamine with acid chlorides, which has advantages over the known synthetic procedures. The compounds prepared showed no significant antiinflammatory activity, thus are of no interest as antiinflammatory agents.

• Archives of Pharmacal Research
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• v.17 no.1
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• pp.31-35
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• 1994

For comparing with flavones/flavonols, isoflavonoids isolated from Pueraria radix and chemically synthesized from biochanin A were evaluated for the antiinflammatory activity using mouse ear edema test, Isoflavonoids such as daildzein and puerarin hsowed the significant antiinflammatory activity at a dose of 2 mg/mouse, although their activity was generally less than that of flavones/flavonols. 7-O-Substitution of biochanin A was not facorable for the antiinflammatory activity.

• Biomolecules & Therapeutics
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• v.6 no.3
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• pp.269-275
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• 1998

These studies were conducted to investigate the antiinflammatory effects and the mechanism of action of natural products. We used the methods of "carrageenan induced foot edema" , "PAF (platelet activating factor) induced foot edema" , "inhibition test of vascular permeability" , "inhibition test of white blood cell migration" , "formation of granuloma" and "adjuvant induced arthritis" to examine the antiinflammatory erects of Angelica gigas, Ledebouriella seseloides, Ginkgo biloba and Bamboo salt (Jukyom). The oral administration of the water extract of Angelica gigantis radix, the methanolic extract of Ginkgo folium and the aqueous solution of Bamboo salt showed antiinflammatory effect on carrageenan and PAF induced foot edema in SD rat at a dose of 1 g/kg. The same administration of methanolic extract of Ginkgo folium also inhibited the vascular permeability in mice. The aqueous solution of Bamboo salt inhibited the formation of ganuloma in SD rats at a oral dose of 1 g/kg. Angelica gigantis radix seems to have antiinflammatory effect by inhibition of PAF.

• YAKHAK HOEJI
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• v.46 no.3
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• pp.149-154
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• 2002

Six novel 4-aminoantipyrine derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiinflammatory-analgesic activity were compared with antiprine. Succinyl chloride and Ac $_2$O were reacted with glycine, respectively, to give glycine compounds (3-4, 9-10), which were treated with hydroxysuccinimide and dicyclohexyl carbodiimide to yield active esters (5-6, 11-12), and then reacted with 4-aminoantipyrine to prepare 4-aminoantipyrine derivatives (7-8, 13-14). 4-Aminoantipyrine reacted with succinyl chloride and Ac $_2$O, respectively, to give succinyl bis aminoantipyrine (15) and acetyl aminoantipyrine (16). Compounds (7), (8) and (13) gave comparable antiinflammatory activity to antipyrine.

• Archives of Pharmacal Research
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• v.16 no.1
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• pp.25-28
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• 1993

Our previous report demonstrated that certain flavonoid aglycones such as apigenin (flavone), quercetin, morin (flavonols), and biochanin A (isoflavone) showed in vivo antiinflammatory activity via topical and oral routes of adminstation. As a continual study, the various flavonoid glycosides have been evaluated in mouse ear edema assay using archidonic acid or croton-oil as a inflammagen. Flavonoids were orally administered (2 mg/mouse) and ear edema inhibition was measured. Significant antiinflammatory activities were found esepcially in flavone and flavonol glycosides (15-29% inhibition) although the flavonoid derivatives tested showed less antiinflammatory activity than hydrocortisone or indomethacin. Chalcone and flavanone derivatives were not significantly active. And in general, flavonol glycosides of kaempferol-type were found to have a higher oral antiinflammatory activity than that of flavonol glycosides of quercetin-type in mice.

• Archives of Pharmacal Research
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• v.16 no.1
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• pp.29-31
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• 1993

A methanol extract of the roots of bupleurum longiradiatum (Umbelliferar) showed antiinflammatory activity in rats. Hexane, chloroform, butanol, and aqueous fractions from the methanol extract were tested with the result that only the hexane fraction exhibited positive activity. Fractionation of the hexane extract resulted in isolation of arborinone as an active principle.