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

• YAKHAK HOEJI
• /
• v.45 no.6
• /
• pp.565-569
• /
• 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
• /
• v.36 no.1
• /
• pp.7-11
• /
• 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.

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

• Natural Product Sciences
• /
• v.2 no.1
• /
• pp.1-8
• /
• 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
• /
• v.58 no.1
• /
• pp.12-15
• /
• 2014

Polygonum cuspidatum which is widely distributed in Korea has been used as treatments of dermatitis, gonorrhea, favus athlete's foot, hyperlipidemia and inflammation in traditional medicine. We examined anti-oxidant and antiinflammatory activity by measuring DPPH radical scavenging activity and the inhibition of IFN-${\gamma}$ and LPS-induced NO production in RAW 264.7 murine macrophage cells. We isolated and characterized resveratrol (1), trans-resveratrol 3-O-${\beta}$-Dglucopyranoside (2). Compounds 1 and 2 showed potent activities compared with L-NMMA ($N^G$-monomethyl-L-arginine). These results suggested that the stilbene compounds isolated from Polygonum cuspidatum might be used as antiinflammatory agents.

• YAKHAK HOEJI
• /
• v.54 no.5
• /
• pp.387-391
• /
• 2010

Polygonum cuspidatum which is widely distributed in Korea has been used as treatments of dermatitis, gonorrhea and inflammation in traditional medicine. We examined anti-inflammatory activities by the inhibition of NO production in RAW264.7 murine macrophages cells. Phytochemical examination of Polygonum cuspidatum led to the isolation and characterization of emodin (1), emodin 8-O-${\beta}$-D-glucopyranoside (2), emodin 1-O-${\beta}$-D-glucopyranoside (3). Antioxidative activities of these compounds were determined by measuring the radical scavenging effects on DPPH radicals. Compounds 1 and 3 showed potent activities compared with L-NMMA. These results suggested that the antraquinone compounds isolated from Polygonum cuspidatum might be used as antiinflammatory agents.

• Archives of Pharmacal Research
• /
• v.24 no.2
• /
• pp.150-158
• /
• 2001

The activity of nonsteroidal antiinflammatory drugs (NSAIDs) in rheumatoid arthritis is not only due to the inhibition of the production of prostaglandins, which can even have beneficial immunosuppressive effects in chronic inflammatory processes. Since we speculated that these drugs could also act by protecting endogenous proteins against denaturation, we evaluated their effect on heat-induced denaturation human serum albumin (HSA) in comparison with several fatty acids which are known to be potent stabilizers of this protein. By the Mizushimas assay and a recently developed HPLC assays we observed that NSAIDs were slightly less active [$EC_{50}~10^{-5}-10^{-4}$ M] than FA and that the HPLC method was less sensitive but more selective than the turbidimetric assay, i.e. it was capable of distinguishing true antiaggregant agents like FA and NSAIDs from substances capable of inhibiting the precipitation of denatured protein aggregates. In conclusion, this survey could be useful for the development of more effective agents in protein condensation diseases like rheumatic disorders, cataract and Alzheimers disease.

• YAKHAK HOEJI
• /
• v.34 no.2
• /
• pp.80-87
• /
• 1990

3-Substituted 5-aminoisoxazole-4-carboxylates were prepared by the reaction of corresponding bormoaldoximes with cyanoacetate. The 3-trifluoromethylisoxazole derivatives were acylated to amides with various aminopyridine derivatives to afford diamides. The ester group was hydrolyzed and decarboxylated easily to give 3-trifluoromethyl-5-aminoisoxazole. The aminoisoxazole was also converted to amides. 5-Amino-3-trifluoromethylisoxazole-5-one-4-carboxylate was prepared by the reaction of trifluoroacetoaldoximoyl bromide and malonate. 5-Amino-3-methylisoxazole-5-one-4-acetate was prepared by the reaction of hydroxylamine and acetylmalonate. The synthesized compounds were tested for antiinflammatory activities.

• Biomolecules & Therapeutics
• /
• v.9 no.2
• /
• pp.69-78
• /
• 2001

Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachi-donic acid and exists in two isoforms (COX-1 and COX-2). COX-1 is involved in the maintenance of physiological functions such as platelet aggregation, cytoprotection in the stomach and maintenance of normal kidney function. COX-2 is induced significantly in vivo under inflammatory conditions. COX-1 and COX-2 serve different physiological and pathological functions. All commercially available nonsteroidal antiinflammatory drugs (NSAIDS) are inhibitors of both COX-1 and COX-2. Therefore, selective inhibitors of COX-2 may be effective antiinflammatory agents without the ulcerogenic effects associated with current NSAms. Since the mid 1990s, a number of reports have been appeared on the preparation and biological activity of selective COX-2 inhibitors. Recently celecoxib, and rofecoxib, the representative COX-2 inhibitors, are introduced in the drug market. In this paper the relationship of structure-activity for selective COX-2 inhibitors is reviewed.