• Title/Summary/Keyword: 7-derivatives

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Solvent Effects on the Solvatochromism of 7-Aminocoumarin Derivatives in Neat and Binary Solvent Mixtures: Correlation of the Electronic Transition Energies with the Solvent Polarity Parameters

  • Choi, Jin-Yeong;Park, Eun-Ju;Chang, Seung-Hyun;Kang, Tai-Jong
    • Bulletin of the Korean Chemical Society
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    • v.30 no.7
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    • pp.1452-1458
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    • 2009
  • The change in the electronic absorption and emission energy of 7-aminocoumarin derivatives in binary solvent mixtures has been studied. The electronic transition energy along with the Stokes' shift is correlated with the orientation polarizability of the solvent as well as the empirical solvent polarity parameters $E_T$ (30). It is observed that the emission peak shift traces the change of $E_T$ (30) value very closely in binary solvent mixtures. The emission transition more strongly depends on the solvent polarity than the absorption, which indicates the dipole moment gets larger on excitation. From the dependence of the Stokes’ shift of 7-aminocoumarins with the solvent polarity parameters and the ground state dipole moment obtained by the semi-empirical calculations, the excited state dipole moment was estimated. The fluorescence lifetime change of 7-aminocoumarins in binary solvent mixtures was measured and the results are explained in terms of molecular conformation and solvent polarity. The study indicates the empirical solvent polarity $E_T$ (30) is a good measure of microscopic solvent polarity and it probes in general the non-specific solvent interactions.

A Convenient Synthesis of 8-Alkyl-2' (or 3')-azido (or amino)-2' (or 3')-deoxyadenosine as Diverse Synthetic Precursors of Cyclic Adenosine Diphosphate Ribose (cADPR)

  • Kim, Beom-Tae;Kim, Bo-Seung;Han, Chy-Hyoung;O, Kwang-Joong;Kim, Sun-Ja;Chun, Jae-Chul;Lee, Jin-Ho;Kim, Sung-Eun;Hwang, Ki-Jun
    • Bulletin of the Korean Chemical Society
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    • v.27 no.7
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    • pp.986-990
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    • 2006
  • As key nucleoside intermediates for the preparation of cyclic adenosine diphosphate ribose (cADPR, 1) analogues, 8-alkyl-2' (or 3')-azido(or amino)-adenosine derivatives (16-19) were successfully prepared by alkylating selectively protected adenosine derivatives (12, 13) via Pd(0) catalyzed cross-coupling reaction with tetraalkyltin reagents, followed by the sugar modification of these 8-alkyl-adenosine derivatives according to our precedent procedure. Compared to other precedent procedures, our 8-alkylation methodology using selectively TBDMS-protected 8-alkyl adenosine derivatives as starting materials will be utilized very conveniently to prepare highly functionalized adenosine analogues, which will be serve as key intermediates for the cADPR.

Partitioning and Inactivation of Viruses by Cold Ethanol Fractionation and Pasteurization during Manufacture of Albumin from Human Plasma

  • Kim, In-Seop;Eo, Ho-Gueon;Chang, Chon-Geun;Lee, Soung-Min
    • Journal of Microbiology and Biotechnology
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    • v.10 no.6
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    • pp.858-864
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    • 2000
  • The purpose of the present study was to examine the efficacy and mechanism of the fraction IV cold ethanol fractionation and pasteurization ($60^{\circ}C$ heat treatment for 10h) steps, involved in the manufacture of albumin from human plasma, in the removal and/or inactivation of blood-born viruses. A variety of experimental model viruses for human pathogenic viruses, including the Bovine viral diarrhoea virus (BVDV), Bovine herpes virus (BHV), Murine encephalomyocarditis virus (EMCV), and Porcine parvovirus (PPV), were selected for this study. Samples from the relevant stages of the production process were spiked with the viruses, and the amount of virus in each fraction was then quantified using a 50% tissue culture infectious dose ($TCID_{50}$). The mechanism of reduction for the enveloped viruses (BHV and BVDV) during fraction IV fractionation was inactivation rather than partitioning, however, it was partitioning in the case of the non-enveloped viruses (EMCV and PPV). The log reduction factors achieved during fraction IV fractionation were ${\geq}6.9$ BHV, $\geq5.2$ for BBDV, 4.9 for EMC, and 4.0 for PPV. Pasteurization was found to be a robust and effective step in inactivating the enveloped viruses as well as EMCV. The log reduction factors achieved during pasteurization were $\geq7.0$ for BHV, $\geq6.1$ for BVDV, $\geq6.3$ for EMCV, and 1.7 for PPV. These results indicate that the production process for albumin has sufficient virus-reducing capacity to achieve a high margin for virus safety.

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Studies on the effects of central nervous system stimulants and depressant on exocrine pancreas (흰쥐의 담취액 분비에 미치는 수종 중추흥분 및 억제물질의 영향)

  • Park, Suh-Kyung
    • The Korean Journal of Pharmacology
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    • v.12 no.1
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    • pp.15-22
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    • 1976
  • The clinical abuse of C.N.S. stimulants during recent years has directed particular attention. Effect of various organs other than C.N.S. was also extensively investigated with those agents. It has been shown that, although there is a wide variation in sensitivity between species, caffeine stimulates gastric secretion in man, cat, guinea pig and dog. Roth and Ivy(1944) reported that caffeine and histamine acted synergistically in stimulating gastric secretion in the cat. Vaille et al(1966) studied that production of pancreatic juice in the rat was enhanced, but bile secretion was not affected by caffeine. In clinical study the effect of chlorpromazine on the external pancreatic secretion in the 24 subjects, the volume fell more than 20% in 7 subjects. (Skajaa et al 1960) It is widely known that C.N.S. stimulants enhanced spontaneous motor activity in the mice, while tranquilizers depressed the activity. Woo (1975) reported that the group of mice treated with chlorpromazine showed markedly inhibited motor activity and in the group of mice treated with amphetamine, there was a significant increase in the motor activity. The purpose of the present experiment was to study the effects of C.N.S. stimulants and depressant on the exocrine pancreas, and on the spontaneous motor activity in the rats. The results obtained are summarized as follows. 1. In animals treated with xanthine derivatives, the volume of pancreatobiliary secretion was markedly increased. 2. Total bilirubin output was elevated markedly in the xanthine derivatives and imipramine treated animals. The bilirubin concentration was increased in xanthine derivatives treated group. 3. The concentration of cholate in the bile was decreased in the chlorpromazine treated group. 4. The activity of lipase in the pancreatobiliary juice was elevated markedly in the xanthine derivatives treated group only. 5. In the all experimental groups, the activity of amylase in pancreatobiliary juice was significantly elevated. 6. In the caffeine treated group, spontaneous motor activity was markedly increased in $30{\sim}60$ minutes, and the amphetamine treated group showed the increased motor activity in first 30 minutes. 7. The group of rats treated with chlorpromazine showed markedly inhibited motor activity after 30 minutes, and the imipramine treated group showed similar result but less inhibition.

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Efficient Green Phosphorescent OLEDs with Hexaazatrinaphthylene Derivatives as a Hole Injection Layer (Hexaazatrinaphthylene 유도체를 정공 주입층으로 사용한 고효율 녹색 인광 OLEDs)

  • Lee, Jae-Hyun;Lee, Jonghee
    • Applied Chemistry for Engineering
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    • v.26 no.6
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    • pp.725-729
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    • 2015
  • Organic light emitting diodes (OLEDs) are regarded as the next generation display and solid-state lighting due to their superb achievements from extensive research efforts on improving the efficiency and stability of OLEDs in addition to developing new materials. Herein, efficient green phosphorescent OLEDs were obtained by using hexaazatrinaphthylene (HAT) derivatives as a hole injection layer. External quantum and current efficiencies of OLEDs were enhanced from 8.8% and 30.8 cd/A to 13.6% and 47.7 cd/A, respectively by inserting a thin layer of HAT derivatives between the ITO and hole transporting layer. The enhancement of OLEDs was found to be originated from the inserted HAT derivatives, which resulted in the optimized hole-electron balance inside the emission layer.

Synthesis and Antimicrobial Properties of Surfactants Containing Phenazine Ring (IV) (페나진 고리를 가진 계면활성제의 합성과 그 항균성 (제 4 보))

  • Ho Sik Kim;Sung Wook Han;Jong Dae Kim
    • Journal of the Korean Chemical Society
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    • v.33 no.5
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    • pp.551-557
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    • 1989
  • 7-Alkyl-1,3-dihydroxyphenazine-5,10-dioxides were synthesized by the reaction of 1,3,5-trihydroxybenzene with 6-alkylbenzofuroxans which had been obtained from aniline and n-alkyl alcohols bearing butyl, hexyl and octyl group. 1,3-Dihydroxyphenazine-5,10-dioxide was also prepared by the reaction of 1,3,5-trihydroxybenzene with benzofuroxan. The surface tension of aqueous solutions of these phenazine dioxide derivatives was determined by surface tensiometer and it was found out that the surface tension decreased with an increase of the number of carbon in the alkyl group. The antimicrobial activities of these phenazine dioxide derivatives were investigated in terms of minimum inhibitory concentration by the common twofold dilution technique. The derivative bearing butyl group showed the highest activity among these derivatives examined. It was observed that the antimicrobial activity of these alkyl substituted phenazine dioxide derivatives was stronger than that of the unsubstituted phenazine dioxide derivative.

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Highly CO2-soluble 5-Amido-8-hydroxyquinoline Chelating Agents for Extraction of Metals in Sc-CO2

  • Chang, Fei;Park, Seo-Hun;Kim, Hakwon
    • Bulletin of the Korean Chemical Society
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    • v.29 no.7
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    • pp.1327-1331
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    • 2008
  • Novel $CO_2$-soluble 8-hydroxyquinoline (8-HQ) chelating agents were synthesized and evaluated for solubility and metal ion extraction ability in supercritical $CO_2\;(Sc-CO_2)$. Among them, secondary amide-containing 8- HQ derivatives cannot be dispersed well into Sc-$CO_2$, but tertiary amide-containing derivatives can dissolve completely in Sc-$CO_2$ even at low CO2 pressures, perhaps owing to the predominant intermolecular interaction between the chelating agent and the $CO_2$ molecule. Based on 8-HQ chelating agent solubility data, we investigated the extraction of metal ions ($Co^{2+}$, $Cu^{2+}$, $Sr^{2+}$, $Cd^{2+}$, and $Zn^{2+}$) using two highly $CO_2$-soluble 8-HQ derivatives (4d, 4e) in Sc-$CO_2$. The extraction efficiency of tertiary amide-containing 8-HQ ligands, both fluorinated and non-fluorinated forms, was dramatically increased in the presence of diethyl amine (organic base). We suggest that diethyl amine could play an important synergistic role in the stronger metal binding ability of 8-HQ through an in situ deprotonation reaction in Sc-$CO_2$ medium.

The Linear Stability Derivatives by the Transient Maneuvering Method (과도응답법(過渡應答法)을 이용한 조종미계수(操縱微係數)의 추정(推定)에 관한 연구(硏究))

  • Seung-Keon,Lee
    • Bulletin of the Society of Naval Architects of Korea
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    • v.27 no.3
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    • pp.31-37
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    • 1990
  • To obtain the values of linear stability derivatives, both analytical and experimental methods are now proposed and in use. The experimental method is well known as the planar motion mechanism(PMM) test. Its concept is to drive the model with a prescrived frequency and amplitude of the motion and pick up the hydrodynamic forces. But this kind of method is inconvenient in case we want to know the stability derivatives in wider range of the frequencies. So a different method is attempted that with one test run, we can get the derivatives in wider range of the frequencies. This technique forces the impulsive motion on the model, using the power of the oil pressure pump. This kind of method was originated by Scragg, C.A., Cummins, W.E, or Frank, T., This resarch is a further development of such preceding works. Todd's series 60(Cb=0.7) 2.00M model is chosen for the test and the results are compared with Van Leeuwen's famous PMM test results.

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In Vitro Evaluation of Two Novel Antimalarial Derivatives of SKM13: SKM13-MeO and SKM13-F

  • Thuy-Tien Thi Trinh;Young-ah Kim;Hyelee Hong;Linh Thi Thuy Le;Hayoung Jang;Soon-Ai Kim;Hyun Park;Hak Sung Kim;Seon-Ju Yeo
    • Parasites, Hosts and Diseases
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    • v.60 no.6
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    • pp.401-407
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    • 2022
  • Antimalarial drugs play an important role in the control and treatment of malaria, a deadly disease caused by the protozoan parasite Plasmodium spp. The development of novel antimalarial agents effective against drug-resistant malarial parasites is urgently needed. The novel derivatives, SKM13-MeO and SKM13-F, were designed based on an SKM13 template by replacing the phenyl group with electron-donating (-OMe) or electron-withdrawing groups (-F), respectively, to reverse the electron density. A colorimetric assay was used to quantify cytotoxicity, and in vitro inhibition assays were performed on 3 different blood stages (ring, trophozoite, and schizonts) of P. falciparum 3D7 and the ring/mixed stage of D6 strain after synchronization. The in vitro cytotoxicity analysis showed that 2 new SKM13 derivatives reduced the cytotoxicity of the SKM13 template. SKM13 maintained the IC50 at the ring and trophozoite stages but not at the schizont stage. The IC50 values for both the trophozoite stage of P. falciparum 3D7 and ring/mixed stages of D6 demonstrated that 2 SKM13 derivatives had decreased antimalarial efficacy, particularly for the SKM13-F derivative. SKM13 may be comparably effective in ring and trophozoite, and electron-donating groups (-OMe) may be better maintain the antimalarial activity than electron-withdrawing groups (-F) in SKM13 modification.

Commercial ${\gamma}$-Oryzanol Inhibits the Formation of C-7 Oxidized Cholesterol Derivatives (OCDs) in an Aqueous Model System during Cholesterol Autoxidation (수용성 모델시스템 내에서의 상업적 ${\gamma}$-Oryzanol의 C-7 산화 콜레스테롤 유도체 생성 저해효과)

  • Kim, Joo-Shin
    • Journal of Food Hygiene and Safety
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    • v.23 no.1
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    • pp.1-5
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    • 2008
  • The inhibition of cholesterol autoxidation by commercial ${\gamma}$-Oryzanol (0, 50, 100, and 300 ppm) was studied in an aqueous model system for 20 h at pH 5.5 and $80^{\circ}C$. The inhibition effectiveness of the commercial ${\gamma}$-Oryzanol was followed by the retention of cholesterol and the formation of C-7 oxidized cholesterol derivatives (OCDs). Changes in the amount of ${\gamma}$-Oryzanol in the aqueous system were determined during cholesterol autoxidation. A method to detect the levels of 7-ketocholesterol, $7{\alpha}$-hydroxycholesterol and $7{\beta}$-hydroxycholesterol in an aqueous model system with ${\gamma}$-Oryzanol was developed by using the hexane-ethyl acetate extraction system and high-performance liquid chromatography. Results showed that the levels of C-7 OCDs in an aqueous dispersion containing 300 ppm of ${\gamma}$-Oryzanol were not significantly (p>0.05) increased, when compared to other treatments (0, 50, and 100 ppm), during the accelerated cholesterol oxidation.