• 제목/요약/키워드: amine derivatives

검색결과 109건 처리시간 0.02초

장기간 과량의 마늘투여가 HK phenotype 진도견의 혈액상에 미치는 영향 (The Effect of Long-term Administration of Excessive Amount of Garlic on Hematology in HK Phenotype Jindo-Dog)

  • 진태원;김홍태;장우석;오태호;송재찬;정규식;박승춘;이근우
    • 한국임상수의학회지
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    • 제18권3호
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    • pp.237-242
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    • 2001
  • The garlic has been eaten widely regardless of easten and westen countries to cure the various disease like cancer, tuberculosis, dentalgia, toxemia and leprosy from ancient times. Even now it is reported that they lower the level of triglycerides and cholesterol in blood and that they also affect on the cohesive power of the platelets. In addition, it is also known that it lowers the glucose level in blood. Especially, the sulfur containing amine acid and the derivatives of the garlic has the counteracting effect to heavy metals. Nowadays, the garlic is known for its efficiency for the various kinds of cancer, neoplasms, hypertension, arteriosclerosis and apoplexy. However, it is reported that the intake of the excessive amount of garlic causes hemolytic anemia recently. The hemolytic anemia is more severe especially in HK phenotype dogs which has Na-K-ATPase activity. Therefore, this study was performed to examine the effect on the blood of the HK phenotype Jindo dogs when administered the excessive amount of garlic. HK phenotype group showed the significant decrease on RBC, WBC, PCV, Hb, MCV, MCHC, GSH, Met-Hb but LK phenotype group didn's show the significant decrease. AST, ALT, BUN, creatinine, CPK, glucose, and total protein values were within normal ranges during the period.

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FMOC 표식에 의한 Sugar Chain의 분석 (Application of FMOC-Cl for the Quantitative Determination of N-linked Oligosaccharides)

  • 김동현;황보식;정구용
    • 한국식품과학회지
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    • 제29권4호
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    • pp.630-634
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    • 1997
  • N-glycanase처리에 의해 얻어진 1-amino-oligosaccharide를 FMOC-Cl로 표식 하는 방법을 확립하였다. 이 방법에 의해 얻어진 FMOC-표식 oligosaccharides는 기존의 방법보다 약 4배의 감도를 나타내었다. Amido 80 column을 사용한 분석에 의하여, Man 5-9 GlcNAc 2 amines의 5개의 성분은 각각 분리되어 용출 되었으며, 회수율은 기존의 방법과 거의 같았다. 1-amino-oligosaccharides는 0.05 pmol에서 1.5 pmol 사이에서 직선적인 관계를 나타내었으며, 2-aminopyridine에 의한 표식과 비교하였을 때, 안정된 화합물을 형성하고 있으며, 감도가 높아 미량의 oligosaccharides의 분석에 매우 적합한 것이 확인되었다.

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Development of a Single Chain Antibody Using a Phage Display Cloning Method for the Detection of 2,4-Dinitrotoluene

  • Na, Jung-Hyun;Joo, Man-Seok;Lee, Won-Kyu;Shim, Hyunbo;Lim, Si-Hyung;Jung, Sang Taek;Yu, Yeon Gyu
    • Bulletin of the Korean Chemical Society
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    • 제34권2호
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    • pp.460-464
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    • 2013
  • Single-chain variable fragments of antibodies (scFv) specific to 2,4-dinitrotoluene (DNT) were isolated from a phage library displaying synthetic human scFv fragments with 6 diversified complementary determining regions (CDRs). A DNT derivative that contained an extended amine group was synthesized and conjugated to the NHS-group that was linked to magnetic beads. Phages specific to the immobilized DNT derivatives were isolated from the library after 4 rounds of sequential binding and elution processes. The displayed scFv fragments from the isolated phages showed consensus CDR sequences. One DNT-specific scFv was expressed in E. coli and purified using Ni-affinity chromatography. The purified DNT-specific scFv binds specifically to the immobilized DNT-derivative with $K_D$ value of $6.0{\times}10^{-7}$ M. The scFv and DNT interaction was not disrupted by the addition of 4-nitrotoluene or benzoic acid. These data demonstrate that the screened scFv from the phage displayed library could be used for selective and sensitive detection of explosives such as TNT.

Phenylcyclohexylamine의 정량적 구조-작용 상관관계에 관한 연구 (Quantitative Structure-Activity Relationship Study on Phenylcyclohexylamine)

  • 김자홍;손성호;양기수;홍성완
    • 대한화학회지
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    • 제42권4호
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    • pp.378-382
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    • 1998
  • Phenylcyclohexylamine과 dexoxadrol에 대한 정량적 구조-작용 상관관계에 관한 계산을 반경험적 분자궤도법인 PM3와 Hyper Chem 프로그램을 이용하여 수행하였다. 19개의 PCA 유도체들의 프론티어 오비탈 크기와 LogP 값은 운동에 영향을 미치는 독성과 MES 발작 실험에서 $MES\;ED_{50}$$TD_{50}$을 예측하는 좋은 매개 변수라는 사실을 알았다.

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뇌 신경물질 운반체 영상용 방사성의약품 (Radiopharmaceuticals for Neurotransmitter Imaging)

  • 오승준
    • Nuclear Medicine and Molecular Imaging
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    • 제41권2호
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    • pp.118-131
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    • 2007
  • Neurotransmitter imaging with radiopharmaceuticals plays major role for understanding of neurological and psychiatric disorders such as Parkinson's disease and depression. Radiopharmaceuticals for neurotransmitter imaging can be divided to dopamine transporter imaging radiopharmaceuticals and serotonin trnasporter imaging radiopharmaceuticals. Many kinds of new dopamine transporter imaging radiopharmcaeuticals has a tropane ring and they showed different biological properties according to the substituted functional group on tropane ring. After the first clinical trials with $[^{123}I]{\beta}-CIT$, alkyl chain substituent introduced to tropane ring amine to decrease time for imaging acquisition and to increase selectivity. From these results, $[^{123}I]PE2I$, [18F]FE-CNT, $[^{123}I]FP-CIT$ and $[^{18}F]FP-CIT$ were developed and they showed high uptake on the dopamine transporter rich regions and fast peak uptake equilibrium time within 4 hours after injection. $[^{11}C]McN$ 5652 was developed for serotonin trnasporter imaging but this compound showed slow kinetics and high background radioactivity. To overcome these problems, new diarylsulfide backbone derivatives such as ADAM, ODAM, AFM, and DASB were developed. In these candidates, $[^{11}C]AFM$ and $[^{11}C]DASB$ showed high binding affinity to serotonin transporter and fast in vivo kinetics. This paper gives an overview of current status on dopamine and serotonin transporter imaging radiopharmaceuitcals and the development of new lead compounds as potential radiopharmaceuticals by medicinal chemistry.

벤질술포닐 흡광단에 결합된 2-니트로벤질계의 광화학에 관한 연구 (Photochemistry of o-Nitrobenzyl System Coupled with a Benzylsulfonyl Chromophore)

  • 김희종;장순기;주동준
    • 공업화학
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    • 제10권1호
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    • pp.124-128
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    • 1999
  • 개별적인 반응성이 알려진 니트로기와 벤질술포닐기가 벤젠 고리 위에서 서로 인접하여 위치할 때 광반응성에 미치는 상호 작용에 대해서 연구하고자 하였다. 니트로기를 포함하는 술포닐 에스테르(cyclohexyl 및 phenyl 2-nitro-${\alpha}$-toluenesulfonate)와 슬포닐아미드(시클로헥실, 페닐, 벤질, 및 피페리딜 2-nitro-${\alpha}$-toluenesulfonamide)의 용액 중 광반응 생성물로부터 벤질술포닐기와 그 ortho 위치에 존재하는 니트로기가 광반응시 서로 상승작용을 하지 않는다는 것을 알 수 있었다. 용액상의 광반응은 이어 필름 상에서의 광반응으로 확인 및 응용되었다. 즉, 두 가지의 2-nitro-${\alpha}$-toluensulfonamide를 포함한 poly(methacrylonitrile)(PMAN) 박막을 NaCl 판 위에 입히고 여기에 254 nm 자외선을 쪼이면서 관찰된 필름의 IR 스펙트럼의 변화로부터도 용액상의 광반응을 일부 확인하였으며 정량실험도 실시하였다. 또한, 본 용액실험의 결과인 광화학적 아민 발생은 poly(glycidyl methacrylate)를 이용한 상 발생 실험에 응용되어 성공적으로 광화학적 에폭시 가교를 수행할 수 있었다.

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저분자량 수용성 키토산이 분급화된 유전자 전달체의 제조 및 특성 (Preparation and Characterization of Low Molecular Weight Water Soluble Chitosan Gene Carrier Fractioned according to Molecular Weight)

  • 장민자;김동곤;정영일;장미경;나재운
    • 폴리머
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    • 제31권6호
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    • pp.555-561
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    • 2007
  • 다양한 분자량을 가진 저분자량 수용성 키토산을 얻기 위해 젖산염이 결합되어 있는 키토산 올리고당을 한외여과막 장치를 이용하여 분리하였고, 새로운 염 제거법으로 유리 아민기를 가진 LMWSC를 제조하였다. 젖산염이 제거된 LMWSC의 특성과 탈아세틸화도가 적외선 분광기(Infrared spectroscopy, IR) 및 핵자기공명장치($^1H-Nuclear$ Magnetic Resonance, $^1H-NMR$)에 의해 확인되었다. 분자량을 나타내는 다분산지수(PDI)는 $1.278{\sim}1.499$로 비교적 좁은 분자량분포를 나타내었다. 유전자 전달체로서의 가능성을 확인하기 위하여, 성공적으로 분자량에 따라 분리된 키토산 올리고당과 염이 제거된 LMWSC의 유전자 전이효율이 293T cell을 이용하여 확인하였다. 또한 유전자 전이효율을 향상시키기 위해 제조된 LMWSC 유도체가 Balb/C mice를 이용하여 평가되었다.

Effect of Number and Location of Amine Groups on the Thermodynamic Parameters on the Acridine Derivatives to DNA

  • Kwon, Ji Hye;Park, Hee-Jin;Chitrapriya, Nataraj;Han, Sung Wook;Lee, Gil Jun;Lee, Dong Jin;Cho, Tae-Sub
    • Bulletin of the Korean Chemical Society
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    • 제34권3호
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    • pp.810-814
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    • 2013
  • The thermodynamic parameters for the intercalative interaction of structurally related well known intercalators, 9-aminoacridine (9AA) and proflavine (PF) were determined by means of fluorescence quenching study. The fluorescence intensity of 9AA decreased upon intercalation to DNA, poly[$d(A-T)_2$] and poly[$d(G-C)_2$]. A van't Hoff plot was constructed from the temperature-dependence of slope of the ratio of the fluorophore in the absence and presence of a quencher molecule with respect to the quencher concentration, which is known as a Stern-Volmer plot. Consequently, the thermodynamic parameters, enthalpy and entropy change, for complex formation was calculated from the slope and y-intercept of the van't Hoff plot. The detailed thermodynamic profile has been elucidated the exothermic nature of complex formation. The complex formation of 9AA with DNA, poly[$d(A-T)_2$] and poly[$d(G-C)_2$] was energetically favorable with a similar negative Gibb's free energy. On the other hand, the entropy change appeared to be unfavorable for 9AA-poly[$d(G-C)_2$] complex formation, which was in contrast to that observed with native DNA and poly[$d(A-T)_2$] cases. The equilibrium constant for the intercalation of PF to poly[$d(G-C)_2$] was larger than that to DNA, and was the largest among sets tested despite the most unfavorable entropy change, which was compensated for by the largest favorable enthalpy. The favorable hydrogen bond contribution to the formation of the complexes was revealed from the analyzed thermodynamic data.

제3세대 백금착체 항암제 신약개발 1. Design, synthesis and antitumor activity of 3rd generation platinum complexes.

  • 김대기;김강혁;김종식;주상섭;김기협;김노경
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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    • pp.73-73
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    • 1993
  • As part of a research program to develope 3rd generation anti tumor platinum complexes, a series of platinum complexes which have 4, 5-bis-(aminomethyl)- 1, 3-dioxolane derivatives as bidenate amine ligands, represented by the general structual formula was prepared. The R$_1$ and/or R$_2$ substituents in this series of platinum complexes can be hydrogen. alkyl, of jointly formed cyclohexane. Two Xs can be a bidenate leaving ligand such as 1, 1-cyclobutanedicarboxylate, malonate, dimethylmalonate, ethylmalonate, glycolate, L-lactate, or N-methyliminodiacetate. From based on the pharmacological and toxicological studies, we have chosen SKI 2053R, cis-malonato[(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) complex (NSC D644591) as a candidate for clinical evaluation. The antitumor activity of a new anti tumor platinum complex, cis-malonato [(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) (SKI 2053R, NSC D644591), was compared with those of cisplatin and carboplatin using murine tumors. We evaluated three platinum complexes against L1210/CPR, a subline of L1210 leukemia resistant to cisplatin for their abilities to overcome tumor resistance to cisplatin. The in vitro cytotoxicity of SKI 2053R to L1210 cell line was 2.5-fold less potent thann that of cisplatin, and was 10-fold more cytotoxic than that of carboplatin. SKI 2053R retained similar cytotoxic effect and anti tumor activity to L1210/CPR cell line, like the cytotoxicity of SKI 2053R to L1210 cell line, while either cisplatin or carboplatin had not property to overcome the acquired cisplatin-resistance. SKI 2053R exhibited greater or comparable antitumor activity than cisplatin or carboplatin in murine tumor models.

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아민계 분산제가 실리카 고무배합물의 물성에 미치는 영향 (Influence of Amine Base Dispersing Agent on Properties of Silica Filled Rubber Compounds)

  • 박성수;길상규;장병만;송기찬;김수경
    • 폴리머
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    • 제25권4호
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    • pp.503-511
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    • 2001
  • 기존 실리카 분산제는 주로 Zn, K의 지방산 유도체이며 지방산과 금속비누의 혼합물은 활성을 높이는데 사용되었다. Zn-K 비누 형태의 실리카 분산제는 탄화수소 사슬의 유동성을 증가시켜 실리카가 함유된 고무 배합물의 점도를 낮추어 주며 그 결과 가공성이 향상된다. 실리카 분산제는 가류 특성에 영향을 미쳐서는 안되는데 Zn-K 비누형태의 분산제는 스코치 및 가류시간을 단축시켰다. 그러나 새로이 개발된 분산제의 경우 금속을 함유하지 않은 non-metal 형태이며 분산제가 실리카와 고무간의 interaction을 유도하여 실리카 분산도를 크게 향상시켰으며 이로 인해 경도 및 점도 저하를 유도하였다. 또한 새로운 분산제는 실리카 고무배합물의 가교특성 및 스코치 안정성에 영향을 미치지 않았다.

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