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Archives of pharmacal research : a publication of ... 21건

  1. [국내논문]   Synthesis and Study of Antibacterial and Antifungal Activities of Novel 2-[[(Benzoxazole/benzimidazole-2-yl)sulfanyl]acetylamino]thiazoles   피인용횟수: 2

    Kaplancikli, Zafer-Asim (Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry ) , Gulhan, Turan-Zitouni (Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry ) , Revial, Gilbert (Laboiratoire de Chimie Organique, CNRS (ESA 7084) ESPCI ) , Guven, Kiymet (Anadolu University, Faculty of Science, Department of Biology)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1081 - 1085 , 2004 , 0253-6269 ,

    초록

    Several 2-[[(benzoxazole/benzimidazole-2-yl)sulfanyl]acetylamino]thiazoles derivatives were synthesized by reacting 4-substituted-2-(chloroacetylamino)thiazoles with benzoxazole/benzimidazole-2-thioles in acetone and in the presence of $K_2CO_3$ . The chemical structures of the compounds were elucidated by IR, $^1H-NMR$ , and $FAB^{+}-MS$ spectral data. Their antimicrobial activities against Micrococcus luteus (NRLL B-4375), Bacillus cereus (NRRL B-3711), Proteus vulgaris (NRRL B-123), Salmonella typhimurium (NRRL B-4420), Staphylococcus aureus (NRRL B-767), Escherichia coli (NRRL B-3704), Candida albicans and Candida globrata (isolates obtained from Osmangazi Uni. Fac.of Medicine) were investigated and in this investigation, a significant level of activity was illustrated.

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  2. [국내논문]   Synthesis and Antinociceptive Activity of (5-Chloro-2(3H)-Benzoxazolon-3-yl) Propanamide Derivatives   피인용횟수: 1

    Onkol, Tijen (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University ) , Sahin, M.Fethi (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University ) , Yidirim, Engin (Department of Pharmacology, Faculty of Medicine, Osmangazi University ) , Erol, Kevser (Department of Pharmacology, Faculty of Medicine, Osmangazi University ) , Ito, Shigero (Institute for Medicinal and Dental Engineering, Tokyo Medicinal and Dental University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1086 - 1092 , 2004 , 0253-6269 ,

    초록

    In this study, (5-chloro-2(3H)-benzoxazolon-3-yl)propanamide derivatives were synthesized. The chemical structures of the compounds were elucidated by their IR and $^1H-NMR$ spectral data and microanalysis. The compounds were tested for anti nociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods. The varying levels of anti nociceptive activity of the compounds were compared with those of dipyrone and aspirin. Among these compounds, compound 5e, 5g, and 5h have been found to be significantly more active than the others and the standards in all the tests.

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  3. [국내논문]   Synthesis and Antimicrobial Activity of Certain Novel Quinoxalines  

    Refaat, Hanan-M. (Organic Chemistry Department, Faculty of Pharmacy, Cairo University ) , Moneer, Ashraf-A. (Organic Chemistry Department, Faculty of Pharmacy, Cairo University ) , Khalil, Omneya-M. (Organic Chemistry Department, Faculty of Pharmacy, Cairo University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1093 - 1098 , 2004 , 0253-6269 ,

    초록

    In this study, certain 3-methyl-2-[4-(substituted amino carbonyl)anilino] quinoxalines, (2a-d) and (3a-d), were synthesized from the new key compound 2-[4-(ethoxycarbonyl)anilino]-3-methyl quinoxaline (1). In addition, a series of 2-[4-(arylidene hydrazinocarbonyl)anilino]-3-methyl quinoxalines (5a-e), as well as their cyclized oxadiazolinyl derivatives (6a-e), and a series of 2-[4- $N^2$ -acylhydrazinocarbonyl)anilino]-3-methyl quinoxalines (7a-d), as well as their cyclized oxadiazolyl derivatives (8a-d) were also prepared. Some of these derivatives were evaluated for antimicrobial activity in vitro. It was found that all the selected compounds exhibit antimicrobial activity and that compound 5b had a broad spectrum of activity.

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  4. [국내논문]   Synthesis and Biological Activity of Benzoxazole Containing Thiazolidinedione Derivatives   피인용횟수: 1

    Jeon, Ra-Ok (College of Pharmacy, Sookmyung Women′s University ) , Park, So-Yeon (College of Pharmacy, Sookmyung Women s University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1099 - 1105 , 2004 , 0253-6269 ,

    초록

    The peroxisome proliferator-activated receptors (PPARs) are a primary regulator of lipid metabolism. Potency for activation of PPAR $\gamma$ , one of a subfamily of PPARs, particularly mirrors glucose lowering activity. We prepared thiazolidinediones featuring benzoxazole moiety for subtype selective PPAR $\gamma$ activators. 5-[4-[2-(Benzoxazol-2-yl-alkylamino)ethoxy]benzyl]thiazolidine-2,4-diones have been prepared by Mitsunobu reaction of benzoxazolylalkylaminoethanol 8 and hydroxybenzylthiazolidinedione 6 and their activities were evaluated. Most compounds tested were identified as potent PPAR $\gamma$ agonists.

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  5. [국내논문]   Gymnastone, A New Benzofuran Derivative from Gymnaster koraiensis   피인용횟수: 2

    Dat, Nguyen-Tien (College of Pharmacy, Chungnam National University ) , Kiem, Phan-Van (Institute of Natural Products Chemistry, Academy of Sciences and Technology, Hanoi, Vietnam ) , Cai, Xing-Fu (College of Pharmacy, Chungnam National University ) , Shen, Quanghai (College of Pharmacy, Chungnam National University ) , Bae, Ki-Hwan (College of Pharmacy, Chungnam National University ) , Kim, Young-Ho (College of Pharmacy, Chungnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1106 - 1108 , 2004 , 0253-6269 ,

    초록

    A new benzofuran derivative, named gymnastone [5-hydroxy-6-acetyl-2-(2-propane-1,2,3-triol)-benzofuran (1)], was isolated from the aerial part of Gymnaster koraiensis, together with viscidone (2) by repeated column chromatography. The structures of both compounds were identified by physico-chemical and spectral analysis including COSY, HMQC, and HMBC experiments.

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  6. [국내논문]   Pentacyclic Triterpenoids from Mallotus apelta   피인용횟수: 2

    Kiem, Phan-Van (Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology ) , Minh, Chau-Van (Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology ) , Huong, Hoang-Thanh (Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology ) , Nam, Nguyen-Hoai (Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology ) , Lee, Jung-Joon (Korea Research Institute of Bioscience and Biotechnology ) , Kim, Young-Ho (College of Pharmacy, Chungnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1109 - 1113 , 2004 , 0253-6269 ,

    초록

    A new triterpene (1) and six known pentacyclic terpenoids (2-7) were isolated from the methanol extract of the dried leaves from Mallotus apelta. Based on the spectral and chemical evidence, their structures were determined to be 3 $\alpha$ -hydroxyhop-22(29)-ene (1), hennadiol (2), friedelin (3), friedelanol (4), epifriedelanol (5), taraxerone (6), and epitaraxerol (7).

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  7. [국내논문]   Determination of Flavonoids, Tannins and Ellagic Acid in Leaves from Rubus L. Species   피인용횟수: 1

    Gudej, Jan (Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Bialystok, ul., Department of Pharmacognosy, Faculty of Pharmacy, Medical University of dz, ul. ) , Tomczyk, Michal (Department of Pharmacognosy, Faculty of Pharmacy, Medical University of Bialystok, ul.)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1114 - 1119 , 2004 , 0253-6269 ,

    초록

    This paper describes the quantitative determination of flavonoids, tannins and ellagic acid in the leaves from wild and cultivated variations of Rubus L. species (Rosaceae): raspberry (2 wild and 13 cultivars) and blackberry (3 wild and 3 cultivars). The content of flavonoids was analyzed using spectrophotometric (the Christ-M llers method) and HPLC analysis after acid hydrolysis. The content of tannins was determined by the weight method, with hide powder, described by German Pharmacopoeia 10 (DAB 10). Ellagic acid content was examined using the HPLC method after acid hydrolysis. Flavonoid content, determined using the Christ-Muller's method was higher for the blackberry leaves than for the raspberry leaves and varied between 0.46% and 1.05%. Quercetin and kaempferol were predominant in all samples analyzed using the HPLC method. The highest flavonoid content was found in the leaves of R. nessensis (1.06%); with results in all of the examined samples varying between 0.27% and 1.06%. The concentration of ellagic acid in all species was determined after acid hydrolysis and ranged from 2.06% to 6.89%. The leaves of raspberries are characterized by greater amounts of tannins (varying between 2.62% and 6.87%) than the leaves of other species. The results from this study indicate that the analyzed species are a rich source of flavonoids, ellagic acid and tannins, which may be used for the quality assessment of Rubus L. species leaves.

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  8. [국내논문]   Anti-Diabetic Activities of Fucosterol from Pelvetia siliquosa   피인용횟수: 4

    Lee, Yeon-Sil (Seokwon Life Science Research Institute, World Sea Green Co. Ltd. ) , Shin, Kuk-Hyun (Seokwon Life Science Research Institute, World Sea Green Co. Ltd. ) , Kim, Bak-Kwang (College of Pharmacy, Seoul National University ) , Lee, Sang-Hyun (College of Pharmacy, Seoul National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1120 - 1122 , 2004 , 0253-6269 ,

    초록

    Fucosterol isolated from Pelvetia siliquosa was tested for its anti-diabetic activity in vivo. Fucosterol, when administered orally at 30 mg/kg in streptozotocin-induced diabetic rats, was caused a significant decrease in serum glucose concentrations, and exhibited an inhibition of sorbitol accumulations in the lenses. Fucosterol, when administered orally at 300 mg/kg in epinephrine-induced diabetic rats, was also caused an inhibition of blood glucose level and glycogen degradation. These results demonstrated that fucosterol is a main anti-diabetic principle from the marine algae P. siliquosa.

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  9. [국내논문]   Protective Constituents Against Sepsis in Mice from the Root Cortex of Paeonia suffruticosa   피인용횟수: 5

    Li, Gao (College of Pharmacy, Yanbian University ) , Seo, Chang-Seob (College of Pharmacy, Yeungnam University ) , Lee, Kyeung-Seon (College of Pharmacy, Yeungnam University ) , Kim, Hyo-Jin (College of Pharmacy, Yeungnam University ) , Chang, Hyun-Wook (College of Pharmacy, Yeungnam University ) , Jung, Jun-Sub (Department of Pharmacology, Hallym University College of Medicine, Institute of Natural Medicine ) , Song, Dong-Keun (Department of Pharmacology, Hallym University College of Medicine, Institute of Natural Medicine ) , Son, Jong-Keun (College of Pharmacy, Yeungnam University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1123 - 1126 , 2004 , 0253-6269 ,

    초록

    The bioassay-guided fractionation of protective agents against sepsis-induced lethality from the root cortex of Paeonia suffruticosa ANDREWS (Ranunculaceae) led to the isolation of eight known compounds: paeonol (1), 2,5-dihydroxy-4-methoxyacetophenone (2), acetovanillone (3), paeonoside (4), paeoniflorin (5), oxypaeoniflorin (6), apiopaeonoside (7), and methyl 3-hydroxy-4-methoxybenzoate (8). Among them, 3 showed the highest survival rate (100% with a dose of 30 mg/kg versus 17% for the control experiment) and reduced alanine aminotransferase level to be a half of the control value on the sepsis model induced by lipopolysaccharide/D-galactosamine.

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  10. [국내논문]   Acetylcholinesterase Inhibitors from the Aerial Parts of Corydalis speciosa   피인용횟수: 2

    Kim, Dae-Keun (College of Pharmacy, Woosuk University ) , Lee, Ki-Taek (College of Pharmacy, Woosuk University ) , Kim, Sung-Hoon (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Park, Hee-Wook (Department of Oncology, Graduate School of East-West Medical Science, Kyung Hee University ) , Lim, Jong-Pil (College of Pharmacy, Woosuk University ) , Shin, Tae-Yong (College of Pharmacy, Woosuk University ) , Eom, Dong-Ok (College of Pharmacy, Woosuk University ) , Yang, Jae-Heon (College of Pharmacy, Woosuk University ) , Eun, Jae-Soon (College of Pharmacy, Woosuk University ) , Baek, Nam-In (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.27 no.11 ,pp. 1127 - 1131 , 2004 , 0253-6269 ,

    초록

    In a bioassay-guided search for acetylcholinesterase inhibitors from Korean natural resources, four isoquinoline alkaloids, corynoxidine (1), protopine (2), palmatine (3), and berberine (4) have been isolated from the methanolic extract of the aerial parts of Corydalis speciosa. Structures of these compounds were elucidated on the basis of spectroscopic techniques. These compounds inhibited acetylcholinesterase activity in a dose-dependent manner, and the $IC_50$ values of compounds 1-4 were 89.0, 16.1, 5.8, and 3.3 $\mu$ M, respectively.

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