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4,5-치환 3-alkoxy-6-allylthiopyridazine 유도체 합성
권순경(Soon Kyoung Kwon) 대한약학회 2002 약학회지 Vol.46 No.3
Through a modification of allicin structure a disagreeable odor and chemical instability of allicin can be improved. 3-Alkoxy-6-allylthiopyridazine derivatives exhibit a superior effect for prevention and treatment of hepatic disease s induced by carbon tetrachloride and aflatoxin B1 and leer prevention of human tissues from radiation. These compounds inhibit also efficiently SK-Hep-1 cell proliferation through induction of apoptosis. So another 4,5-mono- or di-substituted 3-alkyloxy-6- allylthlopyridazine derivatives were synthesized on purpose to and out SAR of allylthiopyridazine in hepatoprotective and hepatotherapeutic acitivitis and to develop more effective drug candidate.
권순경(Soon Kyoung Kwon) 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.3
Chirality is important in the context of biological activity because at a molecular level, asymmetry dominates biological process. While most pharmaceuticals of natural origin are single enantiomers, most of the synthesized chiral drugs are used in the form of racemic mixtures of two or more diastereomers. The enantiomers of a racemic drug generally differ in pharmacodynamic and pharmacokinetic properties as a consequence of stereoselective interaction with optically active molecular components of living organism. In pharmacokinetics and pharmacodynamics enantioselectivity plays an important role. The information on the sum of eutomer and distomer in a racemic drugs is very important in the estimation of therapeutic advantage and/or toxicity of racemates. The choice of preferentially developing a single enantiomer should be based on actual therapeutic advantages and especially improved safety.
히단토인 유도체 형성에 있어서 alpha-Diethaylaminoacetophenone의 탈이반응
권순경(Soon Kyoung Kwon) 대한약학회 1978 약학회지 Vol.22 No.4
It is known that hydantoin derivative can be synthesized according to the method of Bucherer-Bergs, which employs the interaction of the carbonyl compounds with potassium cyanide and ammonium carbonate in dilute alcohol solution. In a converting study of alpha-diethylaminoacetophenone with KCN and (NH4)2CO3 to hydantoin, the attempted 5-diethylaminomethyl-5-phenylhydantoin was not formed. In this reaction diethylaminomethyl group was unexpectedly eliminated and 5-phenylhydantoin was obtained, instead of the anticipated compound.
알릴티오필다진 유도체 합성 및 UV-C 조사에 대한 방어효과
권순경(Soon Kyoung Kwon),현지원(Jin Won Hyun) 대한약학회 2000 약학회지 Vol.44 No.1
Four 3-alkoxy-6-allylthiopyridazines and 3-chloro-6-allylthiopyfidazine were synthesized and their protective effects against oxidative stress and UV-C irradiation were tested. 3-Methoxy-6-allylth-iopyridazine and 3-ethoxy-6-allylthiopyridazine did not show protective effect on the oxidative stress but showed the strongest protective effect on UV-C irradiation among the tested compounds. Especially 500mcg/ml of the two compounds was the most effective concentration.
(-)-4-(파라클로로비페닐)-2-히드록시테트론 산의 합성
권순경(Soon Kyoung Kwon),Donald T. Witiak 대한약학회 1996 약학회지 Vol.40 No.5
4-Aryl-2-hydroxytetronic acids which can be construded as a "lipophilic vitamin C analogue", are known to have antilipidemic and antiaggregatory activities in stead of antiscorbutic activity of vitamin C. A new compound 4-(p-chlorobiphenyl)-2-hydroxytetronic acid (8), which is structurally closely connected with the most active 4-(p-chlorophenyl)-2-hydroxytetronic acid, was synthesized from alpha-(p-chlorobiphenyl)-alpha-hydroxyacetic acid (1) through 7 steps as a potentially bioactive compound.
권순경(Soon Kyoung Kwon) 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.2
Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachidonic 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 NSAIDs. 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.
권순경(Soon Kyoung Kwon) 대한약학회 1982 약학회지 Vol.26 No.2
The behavior of the 5-phenylhydantoin (5-phenyl-2,4-imidazolidinedione) ring in the aminomethylation reaction was studied in order to determine the orientation of this substitution. In case of monoaminomethylation, 3-morpholinomethyl-5-phenylhydantoin (or 3-piperidinomethyl-5-phenylhydantoin) was synthesized by the condensation of 5-phenylhydantoin with one mole of morpholine (or piperidine) and one mole of formaldehyde. 1,3-Dimorpholinomethyl-5-phenylhydantoin was obtained in the attempted condensation of 5-phenylhydantoin with two moles of morpholine and two moles of formaldehyde. Despite the close resemblance to morpholine the attempted condensation of 5-phenylhydantoin with piperidine and formaldehyde under reflux gave no expected 1, 3-dipiperidinomethyl-5-phenylhydantoin. In case of diaminometbylation using piperidine and formaldehyde, only 3,5-dipiperidinomethyl-5-phenylhydantoin was formed.
(+/-)-alpha-Hydroxy-alpha-(p-Chlorobiphenyl)acetic acid 합성과 분할
권순경(Soon Kyoung Kwon) 대한약학회 1995 약학회지 Vol.39 No.4
Optically pure (-)-and (+)-alpha-hydroxy-alpha-(p-chlorobiphenyl)acetic acids were prepared. The racemate was synthesized through three steps. By condensation of p-chlorobiphenyl with diethyl ketomalonate in the presence of SnCl4 diethyl alpha-hydroxy-alpha-(p-chlorobiphenyl)malonate (1) was formed and subsequently (+/-)-alpha-hydroxy-alpha-(p-chlorobiphenyl)acetic acid (3) was obtained through hydrolysis and decarboxylation. For the separation of the racemate the classcal resolution method, derivatization of a racemate by reaction with an optically pure compound was employed. In this case the optically pure compounds were [R]-(+)-alpha-methylbenzylamine and [S]-(-)-alpha-methylbenzylamine. Diastereomeric salts between acids and bases could be easily separated by crystallization in absolute ethanol.