• 제목/요약/키워드: 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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    • 제30권7호
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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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    • 제27권7호
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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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    • 제10권6호
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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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흰쥐의 담취액 분비에 미치는 수종 중추흥분 및 억제물질의 영향 (Studies on the effects of central nervous system stimulants and depressant on exocrine pancreas)

  • 박서경
    • 대한약리학회지
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    • 제12권1호
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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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Hexaazatrinaphthylene 유도체를 정공 주입층으로 사용한 고효율 녹색 인광 OLEDs (Efficient Green Phosphorescent OLEDs with Hexaazatrinaphthylene Derivatives as a Hole Injection Layer)

  • 이재현;이종희
    • 공업화학
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    • 제26권6호
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    • pp.725-729
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    • 2015
  • 유기발광다이오드(organic light emitting diodes, OLEDs)는 높은 효율, 안정성, 신물질 개발과 같은 연구들을 바탕으로 차세대 디스플레이 및 조명으로써의 높은 기술력과 학문적 발전을 달성하였다. 본 논문에서는 hexaazatrinaphthylene (HAT) 유도체들을 OLEDs 소자의 정공주입층으로 사용하여 제작된 고효율의 녹색 인광 OLEDs 소자의 특성을 연구하였다. Indium Tin Oxide (ITO)전극과 정공수송층 사이에 삽입된 박막의 HAT 유도체층은 $1,000cd/m^2$의 구동 조건에서 OLEDs 소자의 외부양자효율을 기존의 8.8%에서 13.6%로, 전류효율을 30.8 cd/A에서 47.7 cd/A로 각각 향상시켰다. 삽입된 HAT 유도체층은 발광층 내부에서 최적화된 전자-정공의 균형을 이루게 하여 소자의 효율 향상에 기여하였다.

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

  • 김호식;한성욱;김종대
    • 대한화학회지
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    • 제33권5호
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    • pp.551-557
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    • 1989
  • 아닐린과 부틸, 헥실, 옥틸기를 가진 n-알킬 알코올류로부터 6-alkylbenzofuroxan류를 합성하고, 이들과 1,3,5-trihydroxybenzene을 반응시켜 7-alkyl-1,3-dihydroxyphenazine-5,10-dioxide류를 합성하였다. 그리고 benzofuroxan과 1,3,5-trihydroxybenzene을 반응시켜 1,3-dihydroxyphenazine-5,10-dioxide도 합성하였다. 이들 phenazine dioxide 유도체의 수용액에 대한 표면장력을 측정하였는데 알킬기의 탄소수가 증가할수록 표면장력이 저하됨을 알았다. 또한 항균성을 희석법에 의하여 조사하였는데 알킬기의 탄소수가 4개인 부틸유도체의 경우가 가장 항균성이 강했으며, 알킬기가 없는 phenazine dioxide 유도체보다는 알킬기가 치환된 phenazine dioxide 유도체의 항균성이 더 강하다는 것을 알았다.

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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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    • 제29권7호
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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.

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

  • 이승건
    • 대한조선학회지
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    • 제27권3호
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    • pp.31-37
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    • 1990
  • 선박의 방향안정성 등을 논할 때 필요하게 되는 선형조종미계수에 대해서는 이론적, 실험적으로 그 추정법이 제안되고 있다. 이중, 실험적 방법은 모형선에 규칙적인 강제동요를 시켜서 원하는 값들을 구하고 있으나, 한규칙 동요에 대해서 그 주파수에 대한 값만 나오므로 넓은 범위의 운동주파수에 걸쳐 미계수의 값들을 얻고자 할 때는 방대한 회수의 실험을 행해야 한다, 이러한 단점을 개선하기 위해 고안된 것이 본 논문에서 취급하는 Transient Maneuvering Method(TMM)로서, 기본원리는 모형에게 과도적 운동을 시켜 그로 인한 동유체력을 계측하고 이를 Fourier 변환하므로서 여러가지 주파수에 대한 미계수의 값을 얻게 되는 것이다. 종래의 이 분야 연구자들은 모형을 움직일 때 전동모터를 사용했으나 모터를 사용할 경우 원하는 과도 운동을 충분히 시킬 수 없으므로 본 논문에서는 유압 펌프를 사용하여 좋은 효과를 얻었다. 그 외에도 입력신호를 다소 개량하여 최종결과의 S/N비를 개선하는데 성공하였다. 실험에 사용한 모델은 Todd의 계열 60(Cb=0.7) 2M급이고, 이 결과를 종래의 PMM 시험결과와 비교하였다.

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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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    • 제60권6호
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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.

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

  • 김주신
    • 한국식품위생안전성학회지
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    • 제23권1호
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    • pp.1-5
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    • 2008
  • 미강 추출 상업용 유통 감마오리자놀의 콜레스테롤 자동산화에 의한 C-7 산화 콜레스테롤 유도체 생성 저해 효과가 수용성 모델 시스템을 이용하여 검토되었다. C-7 콜레스테롤 산화 유도체 (C-7 oxidized cholesterol derivatives: C-7 OCDs) 생성을 위해 콜레스테롤과 감마오리자놀이 분산된 수용성 모델시스템은 구리이온을 촉매로 pH 5.5와 $80^{\circ}C$의 가혹 조건에서 20시간 동안 반응되었다. 산화 유도 기간에 따른 C-7콜레스테롤 산화 유도체 (7-ketocholesterol, 7{\alpha}$-hydroxy-cholesterol과 7b-hydroxycholesterol)의 생성 정도와 감마오리자놀 및 콜레스테롤 변화 추이 정도가 핵산과 에틸아세테이트를 이용한 용매 추출법과 고속 액체크로마토그래프 (high-performance liquid chromatography) 테크닉을 이용 정량적으로 분석되었다. 분석 결과 콜레스테롤 산화 유도 기간에 따른 7-ketocholesterol 생성비율은 7-hydroxycholesterol 이성체 (${\alpha}$-형:${\beta}$-형) 대비 약 2:1의 비율로 생성되었으며, 7-hyoxycholesterol 이성체에 있어서는 ${\alpha}$-형 대비 ${\beta}$-형의 생성 정도가 약 1:2의 비율로 나타났고, 총 C-7 산화콜레스테롤의 생성은 상대적인 고농도(300 ppm) 감마오리자놀 처리 모델 시스템에서 효과적으로 저해되었다.