• Title/Summary/Keyword: bromo

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The Syntehsis and Antimicrobial Activities of Some 1,4-Naphthoquinones (II)

  • Ryu, Chung-Kyu;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.15 no.3
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    • pp.263-268
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    • 1992
  • In order to evaluate the antimicrobial effect of 2, 3-disubstitued-1, 4-naphtoquinone derivatives we newly synthesized several 2-bromo-3-(substituted)-1, 4 naphthoquninones. Amination reaction of 2, 3-dihalo-1, 4 naphthoquinones with aryl and aliphatic amines in ethanol gave 2-halo-3-(N-alkyl or N-aryl)1, 4-naphtoquinone derivatives (1a, b-10a, b) i 60% 90%) yield. These derivatives subjected to antibacterial and antifungal activities. in vitro, against Bacilllus subtilis ATCC 6633 Candida albicans 10231 and local, Psudomonas aeruginosa NCTC10490, Staphylococcus aureus ATCC 6538p. Escherichia coli NIHJ Aspergillus niger KCTC 1231, Tricophyton mentagrophytes KCTC 6085. Among these derivatives 1b, 6b and 7a showed the potent antibacterial activities 1b, 8b and 9b have derivatives, 1b, 6b and 7a showed the potent antibacterial activities. 1b, 8b and 9b have the antifungal activities. 1b is most effective in preventing the growth of Bacillus subtilis and Psudomonas aeruginosa. Candida albicans. Aspergillus niger. Tricophyton mentagrophytes. The several of these compounds demonstrated a broad spectrum of activities in vitro.

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Effect of Liuweidihuang-tang on Alcohol-induced Decrease in New Cell Formation in Rat Dentate Gyrus

  • Bahn Goon Ho;Yoon Doh Joon;Park Jin Kyung;Lee Taeck Hyun;Jang Mi Hyoon;Shin Min Chul;Kim Chang Ju;Paik Eun Kyung;Park Jae Hyung;Cho Son Hae;Lee Choong Yool
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.5
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    • pp.1055-1059
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    • 2002
  • Liuweidihuang-tang has been traditionally used for the treatment of delayed mental and physical development in children, complications of diabetes. and glomerulonephritis. In the present study, the effect of Liuweidihuang-tang on cell proliferation in the dentate gyrus of alcohol-intoxicated Sprague-Dawley rats was investigated via 5-bromo-2' -deoxyuridine (BrdU) immunohistochemistry. Alcohol administration was shown to decrease the number of BrdU-positive cells in the dentate gyrus, while Liuweidihuang-tang treatment increased new cell formation in the dentate gyrus under normal conditions and alcohol intoxication. It was thus demonstrated that aqueous extract of Liuweidihuang-tang exerts a protective effect against alcohol-induced decrease in new cell formation.

Effects of Ginseng radix on Alcohol-induced Decrease in New Cell Formation and Nitric Oxide Synthase Expression in Dentate Gyrus of Rats (인삼이 흰쥐의 치상회에서 알코올에 의한 새로운 신경세포 생성 및 nitric oxide synthase 발현에 미치는 영향)

  • Min-Chul, Shin;Ee-Hwa, Kim;Youn-Hee, Kim
    • The Journal of Korean Medicine
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    • v.23 no.3
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    • pp.26-32
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    • 2002
  • 목적 : 본 연구에서는 알코올 독성에 대하여 흰쥐의 치상회에서 새로운 신경세포의 생성 및 nitric oxide synthase (NOS) 발현에 인삼이 미치는 영향을 5-bromo-2-deoxyuridine (BrdU) 면역 조직 화학법 및 nicotinamide adenine dinucleotide phosphate-diaphorase (NADPH-d) 조직화학법을 통해서 관찰하고자 한다. 방법 : 실험동물을 정상군, 인삼처치군, 알코올처치군 및 알코올-인삼 처치군으로 분류하여 각각의 실험군에 3일간 BrdU (50mg/kg)를 복강주사하였다. 인삼처치군은 30mg/kg 용량의 인삼 전탕액을 중완혈에 약침주사하였고, 알코올 처치군은 2 g/kg 용량의 알코올을 투여하였으며. 알코올-인삼 처치군은 2 g/kg 용량의 알코올 및 30mg/kg 용량의 인삼 전탕액을 투여한 후 각각의 BrdU 양성 세포수와 NADPH-d 양성세포수를 관찰하였다. 결과 : 알코올 투여군은 BrdU 양성세포 및 NADPH-d 양성세포 발현이 감소하였으나, 인삼 및 알코올 인삼처치군에서는 알코올 투여군에 비해서 모두 증가하였다. 결론 : 인삼은 알코올에 의해서 유발된 새로운 신경세포 생성의 감소에 대하여 보호효과가 있으며, 알코올에 의해서 부가적으로 영향 받는 산화질소는 세포생성 조절에 중요한 역할을 하는 것으로 사려된다.

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Crystal Structure Analysis of Methyl 8-bromo-3-phenyl-5a,9a-dihydro-3H-chromen [4,3-c][1,2] isoxazole-3a(4H)-carboxylate

  • Malathy, P.;Sharmila, P.;Srinivasan, J.;Manickam, Bakthadoss;Aravindhan, S.
    • Journal of Integrative Natural Science
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    • v.9 no.2
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    • pp.103-112
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    • 2016
  • The crystal structure of the potential active Methyl 8-bromo-3-phenyl-5a,9a-dihydro-3H-chromen [4,3-c][1,2] isoxazole-3a(4H)-carboxylate ($C_{18}H_{15}BrNO_4$) has been determined from single crystal X-ray diffraction technique. The title compound crystallizes in the triclinic space group Pī with unit cell dimension a=8.3129 (3) ${\AA}$, b=9.5847 (4) ${\AA}$ and c=11.1463(4) ${\AA}$ [${\alpha}=98.457(3)^{\circ}$, ${\beta}=102.806(2)^{\circ}$ and ${\gamma}=105.033(5)^{\circ}$]. Single crystals suitable for X-ray diffraction were obtained by slow evaporation method, the isoxazole and six membered pyran rings adopts envelope conformation. In the crystal, molecules are linked via pairs of inter molecular $C-H{\ldots}O$ hydrogen bonds to form dimmers.

Effects of Cyclic Nucleotides and Glipizide on the Cardiovascular Response of Baclofen in the Rats (흰쥐의 척수에서 Cyclic Nucleotides 및 Glipizide가 Baclofen의 심혈관반응에 미치는 영향)

  • Koh, Hyun-Chul;Ha, Ji-Hee;Shin, In-Chul
    • The Korean Journal of Physiology and Pharmacology
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    • v.1 no.6
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    • pp.647-655
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    • 1997
  • The purpose of present study is to investigate the influence of a spinal gamma-aminobutyric acid B($GABA_B$) receptor on a central regulation of blood pressure(BP) and heart rate(HR), and to define its mechanism in the spinal cord. In urethane-anesthetized, d-tubocurarine-paralyzed and artificially ventilated male Sprague-Dawley rats, intrathecal administration of drugs were carried out using injection cannula(33-gauge stainless steel) through the guide cannula(PE 10) which was inserted intrathecally at lower thoracic level through the puncture of a atlantooccipital membrane. Intrathecal injection of an $GABA_B$ receptor agonist, baclofen(30, 60, 100 nmol) decreased both BP and HR dose-dependently. Pretreatment with 8-bromo-cAMP(50 nmol), a cAMP analog, or glipizide(50 nmol), a ATP-sensitive $K^+$ channel blocker, attenuated the depressor and bradycardic effects of baclofen(100 nmol), but not with 8-bromo-cGMP(50 nmol), a cGMP analog. These results suggest that the $GABA_B$ receptor in the spinal cord plays an inhibitory role in central cardiovascular regulation and that this depressor and bradycardic actions are mediated by the decrease of cAMP via the inhibition of adenylate cyclase and the opening of $K^+$ channel.

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Effects of A-solution on Halitosis and Oral Status in Preoperative NPO Patients (A-solution을 이용한 구강 가글링이 수술 전 금식 환자의 구취와 구강 상태에 미치는 효과)

  • Song, Ji-Ah;Hur, Myung-Haeng
    • Journal of Korean Academy of Nursing
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    • v.42 no.3
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    • pp.405-413
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    • 2012
  • Purpose: The aim of this study was to explore the effects of A-solution on halitosis and oral status in preoperative NPO patients. Methods: A nonequivalent control group, non-synchronized pretest-posttest design was used in this study. The participants in this study were 66 patients who were admitted for gynecologic surgery. The experimental treatment was to give oral gargling with A-solution, blended essential oils and diluted with distilled water. To identify the experimental treatment effects, halitosis, salivary pH, and oral status were measured by a portable halitosis detector, visual analogue scale, Bromo Thymol Blue (BTB), Bromo Cresol Purple (BCP) test paper and oral assessment guide. Data were analyzed using $X^2$-test, t-test with PASW 18.0 version. Results: Participants were homogeneous before experimental treatment. Objective halitosis in the experimental group, measured by a portable halitosis detector (t=-8.34, p<.001) was significantly lower than the control group. Subjective halitosis was significantly lower in the experimental group (t=-9.29, p<.001). Salivary pH was significantly different between two groups (t=8.81, p<.001). Oral status was significantly better in the experimental group (t=-13.31, p<.001). Conclusion: These findings indicate that oral gargling using A-solution is effective in reducing patient halitosis, and improving oral status.

Properties of PMMA Dyed with Reactive Azo Dye (반응성 아조염료로 착색한 PMMA의 성질)

  • Geum, Neri;Heo, Ji-Won
    • Applied Chemistry for Engineering
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    • v.17 no.4
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    • pp.426-431
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    • 2006
  • Acryl and vinyl sulfone functionalized blue and orange azo dyes were prepared by the coupling reaction of 6-bromo-2-cyano-4-nitroaniline and 2,5-dimethoxy-4-(vinylsulfonyl)benzenamine with 3-acrylamido-(N,N-diethylamino)benzene and 3-methyl-(N,N-diethylamino)benzene, respectively, for the coloring of poly(methyl methacrylate) (PMMA). Allyl functionalized dye was also prepared by reacting vinyl sulfone-containing dye with allylamine. Three types of dyeing method were used: the copolymerization of reactive dye with methyl methacrylate (MMA) and dyeing by polymerization of MMA in the presence of polymeric dye and dye 2 without reactive function. The color fastness for the three PMMAs were evaluated by comparing the solubility of dye under various conditions.

6- [(Halopheny1) amino]-7-Bromo-5,8-Quinolinediones Treatment of Candidiasis in Normal Mice

  • Kim, Sung-Hee;Kim, Do-Hee;Lee, In-Kyung;Kim, Dong-Hyun;Ryu, Chung-Kyu
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.167-167
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    • 1996
  • A series of 6-[(N-Halophenyl)amino] -7-Bromo-5,8-quinolinediones (BQs) newly synthesized were tested for antifungal activities, in vitro, against Candida sp., Aspergillus niger and Trichophyton mentagrophytes. The MIC values were determined by the twofold dilution method. Among these derivatives, BQ4 and 7 showed more potent antifungal activities than fluconazole and ketoconazole. BQ 4 and 7 were compared with fluconazole in the treatment of established systemic infections with Candida albicans in normal rats. Intraperitoneally administered BQs for 7 days and 14 days reduced Candida albicans colony count in kidneys and livers as well as fluconazole. The therapeutic potential of BQs has been assessed by evaluating their activities (survival rate) against systemic infections in normal mice with Candida albicans. These compounds, particularly showed activities comparable with fluconazole. BQ4 and 7 had about EO$\_$50/, 0.05, 0.06mg/kg but fluconazole had ED$\_$50/, 6.0mg/kg respectively.

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Structural Analysis of 2-Benzyl-3-[3-(4-bromo-phenyl)-1-phenyl-1H-pyrazol-4yl]-4,6-dioxo-5-phenyl-octahydro-pyrrolo[3,4-C]pyrrole-1-carboxylic Acid Ethyl Ester through X-ray Crystallography

  • Ganapathy, Jagadeesan;Pramesh, M.;Perumal, P.T.;Sanmargam, Aravindhan
    • Journal of Integrative Natural Science
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    • v.8 no.3
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    • pp.192-203
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    • 2015
  • In view of the growing medicinal importance of pyrazole and its derivatives, the single crystal X-ray diffraction study was carried out for the potential active 2-Benzyl-3-[3-(4-bromo-phenyl)-1-phenyl-1H-pyrazol-4yl]-4,6-dioxo-5-phenyl-octahydro-pyrrolo[3,4-C]pyrrole-1-carboxylic acid ethyl ester ($C_{37}H_{31}BrN_4O_4$, H2O). In the title compound are two molecules exist in the asymmetric unit. It crystallizes in the monoclinic space group $P{\hat{i}}$ with unit cell dimension $a=13.361(18){\AA}$, $b=13.424(17){\AA}$ and $c=21.649(2){\AA}$ [${\alpha}=80.745(9)^{\circ}$, ${\beta}=79.770(10)^{\circ}$ and ${\gamma}=60.788(6)^{\circ}$]. The pyrazole ring adopts planar conformation. The sum of the bond angles at nitrogen atom of the pyrazole ring indicates the $Sp^2$ hybridized state. The crystal structure is stabilized by intramolecular C-H...O hydrogen bond interaction.

Highly Stable Photoluminescent Qunatum Dot Multilayers by Layer-by-Layer Assembly via Nucleophilic Substitution Reaction in Organic Media

  • Yun, Mi-Seon;Kim, Yeong-Hun;Jeong, Sang-Hyeok;Baek, Hyeon-Hui;Jo, Jin-Han
    • Proceedings of the Materials Research Society of Korea Conference
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    • 2011.05a
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    • pp.244.2-244.2
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    • 2011
  • We introduce a novel and robust method for the preparation of nanocomposite multilayers, which allows the excellent photoluminescent (PL) properties as well as the accurate control over the composition and dimensions of multilayers. By exchanging the oleic acid stabilizers of CdSe@ZnS quantum dots (QDs) synthesized in organic solvent with 2-bromo-2-methylpropionic acid (BMPA) in the same solvent, these nanoparticles were be alternately deposited by nucleophilic substitution reaction with highly branched poly(amidoamine) dendrimer (PAMA) through layer-by-layer (LbL) assembly process. Our approach does not need to be transformed into the water-dispersible nanoparticles with electrostatic or hydrogen-bonding groups, which can deteriorate their inherent properties, for the built-up of multilayers. The nanocomposite multilayers including QDs exhibited the strong PL properties achieving densely packed surface coverage as well as long-term PL stability under atmospheric conditions in comparison with those of conventional LbL multilayers based on electrostatic interaction. Furthermore, we demonstrate that the flexible multilayer films with optical properties can be easily prepared using nucleophilic substitution reaction between bromo and amino groups in organic media. This robust and tailored method opens a new route for the design of functional film devices based on nanocomposite multilayers.

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