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도희정,조원제,용철순,이치호,김대덕 전남대학교 약품개발연구소 2001 약품개발연구지 Vol.10 No.-
Various alkyl ester prodrugs of diclofenac were synthesized in order to investigate the relationship between their skin permeation characteristics and physicochemical properties. Solubility in various vehicles was measured at room temperature. I -Octanol/water partition coefficients (Log P) and capacity factors (k') were measured to determine the lipophilicity of the prodrugs. Stability of prodrugs in the skin extract and homogenate was also investigated before conducting the skin permeation studies. Increases in the Log P and capacity factor values were observed when alkyl esters of diclofenac were prepared. Since the aqueous solubility of the prodrugs was not high enough, they were saturated in propylene glycol (PG) for skin permeation studies. Prodrugs were rapidly metabolized to diclofenac, both in skin homogenate and in dermal extract of skin. The skin permeation rate of alkyl ester prodrugs was significantly higher than diclofenac with shorter lag time. Moreover, a parabolic relationship was observed between the permeation rate and the log P values of prodrugs, and the maximum flux was achieved at a log P value of around 4.0.
정병호,조원제,천승훈,박면지,유진철,천문우 朝鮮大學校 1998 藥學硏究誌 Vol.19 No.2
For the development of antifungal agents. modification of naftifine which exhibits significant antimycotic activity was performed by replacing the naphthalene ring of it to hetero cyclic rings such as morpholine. benzothiazole. piperidine and pyridine derivatives. The synthesized compounds were tested in vitro antifungal activity against five different fungi with naftifine as a comparative antimycotic molecule. From the biological evaluation two compounds. (E)-N-(3-phenyl-2-propenyl)-N-(4-piperidinylmethyl)amine(3d) and (E)-N-(3-phenyl-2-propenyl)-N-(3-pyndylmethyl)amine(3D) showed relatively noticeable activity(MIC=50㎍/㎖). On the other hand. the other compounds had no activity.
도희정,조원제,용철순,이치호,김대덕 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
Various alkyl ester prodrugs of diclofenac were synthesized in order to investigate the relationship between their skin permeation characteristics and physicohemical properties. Solubility in various vehicles was meastured at room temperature. 1-Octanol/water partition coefficients (Log P) and capacity factors (k") were measured to detemine the lipophilicity of the prodrugs. Stability of prodrugs in the skin extract and homogenate was also investigated before conduction the skin permeation studies. Increases in the Log P and capacity factor values were observed when alkyl esters of diclofenac were perpared. Since the aqueous solubility of the prodrugs was not high enough, they were saturated in propylene glycol (PG) for skin permeation studies. Prodrugs were rapidly metabolized to diclofenac, both in skin homogenate and in dernal extract of skin. The skin permeation rate of alkyl ester prodrugs was significantly higher than diclofenac with shorter lag time. Morecover, a parabolic relationship was observed between the pemeation rate and the log P values of prodrugs, and the maximum flux was achieved at a log P value of around 4.0.
김민정,도희정,조원제,용철순,최한곤,이치호,김대덕 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.4
Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at 37℃. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from the partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at 37℃. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers tested, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation rate achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.
CoMFA 법을 이용한 3-아릴이소퀴놀린 화합물들의 SK-OV-3 암세포에 대한 가상의 약물 작용 수용체 해석
김의기,민선영,정병호,천승훈,최보길,조원제 전남대학교 약품개발연구소 2002 약품개발연구지 Vol.11 No.-
We have performed a 3D-QSAR/ CoMFA analysis of the cytotoxiv activities of thirty-five 3-arylisoquinoline derivative against SK-OV-3 tumor cell line. The results suggested that the electrostatic, steric and hydrophobic factors of 3-arylisoquinoline were strongly correlated with the antitumor activity. Considerable predictive ability (cross-validated r2 as high as 0.841) was obtained through CoMFA.
CHO, Won-Jea 朝鮮奬學會 1988 學術論文集 Vol.17 No.-
2,3,9,I0-Tetraoxygenated protoberberin alkaloids, berberine (1a), palmatine (1b), and copti¬sine (1c), were efficiently converted into the corresponding 12-hydroxy-2,3,10,11-tetraoxygenated protoberberines (6a, 6b, 6c) through an oxidative C_(8)-C_(8a) bond cleavage with m-chloroperbenzoic acid, followed by the en amide photo-cyclization. On successive treatment with diethyl chlorophos¬phate and sodium in liquid ammonia, the 12-hydroxy derivatives (6a, 6b, 6c) underwent reductive dehydroxylation to produce the corresponding 2,3,I0,11-tetraoxygenated protoberberines, tetrahy¬dropseudoberberine (4a), (± )-xylopinine (4b), and tetrahydropseudocoptisine (4c), respectively.
Cho, Won-Jea,Kim, Eui-Ki,Park, Il Yeong,Jeong, Eun Young,Kim, Tae Sung,Le, Thanh Nguyen,Kim, Dae-Duk,Lee, Eung-Seok 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
A series of 58 3-arylisoquinoline antitumor agents were investigated for defining the phamacophroe model using comparative molecular field analysis (CoMFA) program. The studied compounds relatod to biosostere of benzophenanthridine alkaloid were synthesized and evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). In order to perform the systematic molecular modeling study of these compounds, the conformational search was carried out based on the single X-ray crystallographic structure of 7,8-dimethoxy-3-phenylisoquinolin-(2H)-one(2). Interestingly, two types of structures having different dihedral angles between the isoquinoline ring and 3-aryl ring were found in the crystals. Therefore, CoMFA was performed two different, overlapping ways. The alignments of the structures were based on the common isoquinoline ring and 3-aryl ring. The 3-D-quantitative structure-activity relationship study resulted in significant cross-validated, conventional r^2 values equal to 0.715 and 0.927, respectively.