• Title/Summary/Keyword: bromo

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Synthesis and COX Inhibitory Activities of Rutaecarpine Derivatives

  • Lee, Eung-Seok;Kim, Seung-Ill;Lee, Seung-Hoo;Jeong, Tae-Cheon;Moon, Tae-Chul;Chang, Hyeun-Wook;Jahng, Yurng Dong
    • Bulletin of the Korean Chemical Society
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    • v.26 no.12
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    • pp.1975-1980
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    • 2005
  • A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity ($IC_{50}$ = 0.27, 0.35 $\mu$M, respectively) with selectivity.

Synthesis of 6-Exomethylene Sulbactam Derivatives (6-엑소메칠렌 Sulbactam 유도체의 합성)

  • 임채욱;정홍식;임철부
    • YAKHAK HOEJI
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    • v.46 no.6
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    • pp.381-386
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    • 2002
  • The synthesis of new 6-exomethylene sulbactam derivatives with 5-methyl-1,3,4-thiadiazole was described. The 6,6-dibromopenam 5 was reacted with $CH_3$MgBr and carbaldehyde 4 to afford the 6-bromo-6-(1-hydroxy-1-methyl)penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxy compound 7 with zinc and acetic acid gave 6-exomethylen penams, Z-isomer 8 and E-isomer 9, which was oxidized to sulfones 10 by m-CPBA. The p-methoxybenzyl compounds 6-10 were deprotected by AlCl$_3$ and neutralized with NaOH solution to give the sodium salts 11-15.

Simultaneous determination of betaine and choline using derivatization by HPLC with UV detection (HPLC-UV검출방법으로 유도체화를 통한 비테인과 콜린의 동시분석)

  • Rhee, Insook;Paeng, Ki-Jung
    • Analytical Science and Technology
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    • v.28 no.2
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    • pp.112-116
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    • 2015
  • Extraction of quaternary ammonium compounds (choline and betaine) from plant samples (spinach) using ion exchange resin (AG1, OH form) is a very simple and inexpensive approach. However, it is very hard to determine amounts of choline and betaine simultaneously using high-performance liquid chromatography-ultraviolet (HPLC-UV) detection. Unlike choline, betaine has low molar absorptivity in UV-visible (UV-Vis) region, which makes it difficult to carry out UV-Vis detection of betaine. The mixture of quaternary ammonium compounds (choline and betaine) was derivatized using 2-bromo acetophenone as a derivatizing agent. As a result, choline did not react with the derivatizing agent, whereas betaine formed a betaine derivative. This betaine derivative exhibited detectable UV absorption with baseline separation between choline and the betaine derivative. Thus, with this method, choline and betaine can be determined simultaneously by using the HPLCUV method through one-step derivatization, which is an easy, sensitive, and reliable method.

Characterization of extracellular fructosyl transferase from aureobasidium pullulans C-23 (Aureobasidium pullulans C-23이 생산하는 세포외 fructosyl transferase의 특성)

  • 이광준;최정도;임재윤
    • Korean Journal of Microbiology
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    • v.29 no.5
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    • pp.301-306
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    • 1991
  • Extracellular fructosyl transferase from Aureobasidium pullulans C-23 was characterized. The molecular weight of the isolated enzyme was determined to be approximately 170,000 by SDS polyacrylamide gel electrophoresis. The enzyme has the pI value of about 3.7. The enzyme was almost completely inhibited by 5mM $Hg^{2+}$ , but was not significantly affected by other cations tested. The enzyme was inactivated by treatment of tryptophan-specific reagent N-bromo- succinimide and tyrosine-specific reagent iodine. The substrate sucrose showed protective effect on the inactivation of the enzyme by the both reagents. These results suggest that tryptophan and tyrosine residues are probably located at or near active site of the enzyme.

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Melatonin increases cell proliferation in the dentategyrus of maternally-separated rats

  • Jung, Kyung-Hee;Jung, Eun-young;Kim, Mi-Ja;Kim, Hye-Kyung;Kim, Yong-Ok;Chang, Un-Jae;Yim, Sung-Vin
    • Proceedings of the KSCN Conference
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    • 2004.05a
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    • pp.439.2-439
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    • 2004
  • Melatonin in mammals, produced by the pineal gland and elsewhere, has shown antioxidant and neuroprotective properties in neuronal cells. We investigated whether melatonin would increase newly-born cells (cell proliferation) in the dentate gyrus of maternally-separated rats. To examine the effect of melatonin on cell proliferation of the dentate gyrus in maternally-separated rats, 5-bromo-2'-deoxyuridine (BrdU) immunohistochemistry was performed.(omitted)

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The Enzymatic Characteristics of the Cytidine Deaminase in Salmonella typhimurium

  • Lee, Sang-Mahn
    • Korean Journal of Environmental Biology
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    • v.21 no.1
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    • pp.60-65
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    • 2003
  • The cytidine deaminase was partialy purified with sephadex G-200 and the characteristics of the enzyme were clarified. The molecular mass of the plasmid-encoded protein was identified as about 30 kDa in a minicell system. The native enzyme was estimated to have the molecular mass of 60 kDa by gel filtration. This indicates that the native enzyme may exist as a dimer composed of two identical subunits. The enzyme was reasonably stable in the pH range of 6 to 9, and was labile under high temperature above $50^{\circ}C$. Mercaptoethanol, pCMB, mercury and copper were found to inhibit the enzyme activity. The cytidine analogues of bromo- and iodo-(deoxy)-cytidine were also found to inhibit the activity, while fluorodeoxycytidine and azacytidine were found to activate it. Deoxycytidine, cytidine, ara-C and Methyldeoxycytidine have excellent substrates for the enzyme.

Acupuncture Suppresses Intrastriatal Hemorrhage-Induced Neuronal Cell Death and Proliferation in Rats

  • Cho, Nam-Hun;Park, Dong-suk;Lee, Jae-Dong
    • The Journal of Korean Medicine
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    • v.24 no.4
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    • pp.127-135
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    • 2003
  • Objectives : Intracerebral hemorrhage (ICH) is one of the most devastating types of stroke. The effect of acupuncture on the intrastriatal hemorrhage-induced neuronal cell death and cell proliferation in rats is examined. Methods : Cell death and cell proliferation in rats was investigated via terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay and immunohistochemistry for caspase-3 and 5-bromo-2'-deoxyuridine (BrdU). Results : Results showed that apoptotic cell death in the striatum and cell proliferation in the hippocampal dentate gyrus significantly increased following intrastriatal hemorrhage in rats, and that acupunctural treatment at the Zusanli acupoint suppressed the hemorrhage-induced increase in apoptosis in the striatum and cell proliferation in the dentate gyrus. Conclusions : It is suggested that acupunctural treatment, especially at the Zusanli acupoint, may aid recovery following central nervous system sequelae following ICH.

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Cloning and Expression of $\beta$-l,4-Glucosidase Gene from Pseudomonas sp. in Escherichia coli and Bacillus subtilis (Pseudomonas sp. $\beta$-1,4-Glucosidase 유전자의 Esherichia coli와 Bacillus subtilis에의 Cloning 및 발현)

  • 김양우;전성식;김석재;정영철;성낙계
    • Microbiology and Biotechnology Letters
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    • v.21 no.2
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    • pp.113-118
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    • 1993
  • Fro the purpose of producing glouse from cellobiose or oligo saccharide and obtaining genetic information of beta-1,4-glucosidase gene, alpha beta-1,4-glucosidase gene of Pseudomonas sp. LBC505, potent cellulase complex and xylanase producing strain, was cloned in Esherichia coli and Bacillus subtilis into pUC19 and pBD64, respectively. Recombinant plasmid pGL1 contained 1.2kb EcoRI fragment was isolated from transformants forming blue color around colony on LB agar plate containing 20 ng/ml of 5-bromo-4-chloro-3-indolyl-beta-D-glucopyranoside(X-glu) and ampicillin.

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Synthesis of Poly Imide/α'ω'-di Poly Acrylamide (3-Mercaptopropyl) Trimethoxysilane Terminated Copolymer (양 말단에 MPTMS-아크릴아미드로 치환된 폴리이미드의 합성)

  • Min, Jun Ho;Park, Chan Young;Min, Seong Kee
    • Korean Journal of Materials Research
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    • v.26 no.9
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    • pp.478-485
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    • 2016
  • An amide group was introduced to restrain the cohesion of silica nano-particles and copolymerized with polyamic acid. Amide block copolymers were prepared using silica and (3-mercaptopropyl) trimethoxysilane (MPTMS) with a siloxane group, using 2, 6-Lutidine as a catalyst. Amide block polymers and copolymers were synthesized via ATRP after brominating pyromellitic dianhydride (PMDA) and polyamic acid of methylene diphenyl diamine (MDA) using ${\alpha}$-bromo isobutyryl bromide. Characteristic peaks of copolymer with amide and imide groups and patterns of amorphous polymers were studied using FT-IR and XRD analyses; an analysis of the surface characteristic groups was conducted via XPS. Changes in the thermal properties were examined through DSC and TGA; solubility for solvents was also studied.