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Pharmacological properties of the reversihle inhibitor of the gastric H+/K+ ATPase,AU-164
Yum, Eul Kgun,Kim, Hyo Jung,Cheon, Hyae Gyeong,Choi, Jong Kwon 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.3
AU-164 was synthesized as a reversible gastric H^+/K^+ ATPase inhibitor, and its effects were tested in various systems. AU-164 inhibited rabbit gastric H^+/K^+ ATPase with an IC_(50) of 9 μM. On the other hand, AU-164 was a weak inhibitor for dog kidney Na^+/K^+ ATPase, indicating the selectivity for gastric H^+/K^+ ATPase. The reversible property of the AU-164-induced inhibition of H^+/K^+ ATPase was confirmed by filtering the inhibition mixture through Sephadex G-25M column. In vivo basal acid secretion was also inhibited by AU-164 under the pylorus ligation of Sprague-Dawley rats. In addition, AU-164 protected dose dependently gastric lesion induced by ethanol in rats. The ED_(50) value of 62 mg/kg p.o. was estimated. These results suggest that AU-164 is a potent, selective and reversible gastric H^+/K^+ ATPase inhibitor, and that AU-164 has a potential use for the clinical therapeutics of peptic ulcer disease.
Yum, Eul Kgun,Park, Woul Seong,Kim, Se Hoan,Kang, Seung Kyu,Kim, Sung Soo,Ahn, Jin Hee The Chemical Society of Japan 2008 Chemistry letters Vol.37 No.10
<P>Palladium-catalyzed carboalkoxylation of 2-bromo-3-phenylindenones in various alcoholic solvents afforded diverse alkyl 1-oxo-3-phenyl-1<I>H</I>-indene-2-carboxylates in high yields.</P>
Yum, Eul Kgun,Yang, Ok-Kyung,Kim, Ji-Eun,Park, Hee Jung Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.9
We have developed a one-step synthesis of benzofurans from o-iodophenol and various terminal alkynes, by using Pd catalyst supported on nano-sized carbon balls (NCB) under copper- and ligand free conditions. This recyclable catalyst could be reused more than 5 times in the same heteroannulation reaction. The results have demonstrated that diverse 2-substituted benzofurans with tolerant functional groups can be prepared simply and conveniently under these conditions.
Studies on the Mechanism of Action of the Gastric H+ + K+ ATPase Inhibitor KH 3218
Cho, Sung Yun,Yum, Eul Kgun,Yang, Sung Il,Kim, Hyo Jung,Cheon, Hyae Gyeong,Kim, Do Yeob 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.3
The novel compound KH 3218 was synthesized and evaluated for its ability to inhibit the gastric H^++K^+ ATPase activity in vitro as well as to lessen gastric acid secretion in vivo. KH 3218 inhibited rabbit gastric H^++K^+ ATPase in a concentration and time dependent manner. IC_(50) value was estimated to be about 15μM. The inhibition of the H^++K^+ ATPase by KH 3218 was blocked by sulfhydryl reducing agents, dithiothreitol or β-mercaptoethanol. The inhibition of the enzyme was not reversible by 50 fold dilution of the incubation mixtures, suggesting the irreversible nature of the inactivation. In the pylorus-ligated rat, KH 3218 reduced the total acid output as compared with the control. In addition, KH 3218 was capable of inhibiting H. pylori urease activity. These data suggest that KH 3218 is a potent inhibitor for H^++K^+ ATPase activity as well as for gastric acid secretion, and has a potential to be developed as a novel antiulcer agent.
Suh, Jee Hee,Yum, Eul Kgun,Cho, Young Sik Pharmaceutical Society of Japan 2015 Chemical & pharmaceutical bulletin Vol. No.
<P>We describe the synthesis and biological evaluation of N-aryl-5-aryloxazol-2-amine derivatives that are able to inhibit 5-lipoxygenase (5-LOX), a key enzyme of leukotriene synthesis, for the treatment of inflammation-related diseases including asthma and rheumatoid arthritis. A novel structural moiety containing oxazole was initially identified from a chemical library using an in vitro enzymatic and cell-based assay, and its synthesized oxazole derivatives were further examined to develop a structure-activity relationship (SAR). SAR analysis demonstrated that a hydroxyl or amino group at the p-position on N-phenyl was essential for the 5-LOX-inhibitory activities of the derivatives, and that other halogen and methyl group-substituted derivatives affected the potency, positively or negatively. As a result, derivatives selected through first-round screening were further optimized using a cell-based assay and an in vivo assay to develop a potent, selective 5-LOX inhibitor. A final hit exhibited an improved efficacy in arachidonic acid-induced ear edema when applied topically but not orally. Moreover, it showed the additional advantage of sustainable antiinflammatory activity over a reference compound, zileuton. Taken together, chemical entities bearing an oxazole scaffold could be promising as therapeutic drugs for the treatment of chronic inflammatory skin disorders.</P>
SYNTHESIS OF PYRIDOPYRROLO[2,1-a]ISOINDOLES BY PALLADIUM-CATALYZED ANNULATION
Kang, Song Su,Yum, Eul Kgun,Sung, Nack-Do 충남대학교 형질전환복제돼지연구센터 2004 논문집 Vol. No.8
Diverse pyridopyrrolo[2,1-α]isoindoles were prepared by palladium-catalyzed annulation of benzylidene(4-iodopyridin-3-yl)amines and aromatic substituted internal alkynes under Pd(OAc)₂, _n-Bu₄NCl, and Et₃N at 110 ℃.