• 제목/요약/키워드: carboxylic moiety

검색결과 27건 처리시간 0.019초

Sensitive and Mild Fluorogenic Reagents for Biogenic Carboxylic Acids in HPLC

  • Ushijima, Tamano;Saito, Mikihiko;Sasamoto, Kazumi;Ohkura, Yosuke;Ueno, Keiyu
    • 분석과학
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    • 제8권4호
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    • pp.545-551
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    • 1995
  • Five acid hydrazides as precolumn fluorescence derivatization reagents for carboxylic acids in HPLC, which have the benzofuran or benzothiazole moiety conjugated to a furan, thiophene or oxazoline ring, were synthesized and examined in view of reactivity, separability and sensitivity. Of these hydrazides, 2-(5-hydrazinocarbonyl-2-oxazolyl)-5,6-dimethoxybenzothiazole (BTOH) was most favorable. The detection limit of lauric acid as a model acid was 0.1 pmol per $10-{\mu}l$ injection volume at S/N=3, which was roughly equal to that of an analogous compound, 2-(5-hydrazinocarbonyl-2-furyl)-5,6-dimethoxybenzothiazole. The reagent allowed rapid assays of carboxylic acids ($C_{12:0}-C_{20:4}$) within 20 min with satisfactory scparability. The method was applied to the determination of fatty acids in human sera from healthy volunteers as well as from patients with diabetes or thyroid dysfunction.

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상용성이 개선된 접착 증진제의 합성 및 이를 함유한 자외선 경화형 접착제의 특성분석 (Synthesis of Adhesion Promoters with Improved Compatibility and Properties of UV-Curable Adhesives Containing Adhesion Promoters)

  • 박정현;원종우;김주열;윤유정;권오형;황진상
    • 접착 및 계면
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    • 제19권4호
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    • pp.145-153
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    • 2018
  • 본 연구에서는 상용성이 개선된 접착 증진제를 개발하기 위해 malenized polybutadiene과 2-hydroxyethyl acrylate(HEA)의 반응을 통해 다양한 함량의 아크릴레이트 반응기와 carboxylic acid가 도입된 접착 증진제(PBCA)를 합성하였다. 합성된 접착 증진제는 maleic anhydride의 개환 반응을 통해 도입된 아크릴레이트 반응기와 carboxylic acid의 함량, 그리고 접착 증진제의 첨가량을 달리하여 접착 필름을 제조하고 제조된 접착 필름의 표면 특성, 접착력 등의 기계적 특성과 흡습 특성 등의 변화를 확인하였다. 접착 증진제의 분자 내에 도입된 carboxylic acid의 함량이 증가할수록 접착 필름의 접착력은 증가하는 경향을 보였으며, 기존의 상용화된 접착 증진제와 비교하여 기계적 물성 또한 개선됨을 확인하였다. 특히, 분자 내에 소수성의 폴리부타디엔 주쇄와 친수성의 maleic anhydride 및 carboxylic acid가 동시에 존재함으로 인해 다양한 친수성 및 소수성 재료와의 상용성이 대폭 개선되었음을 확인하였다.

새로운 베타락탐계 항생물질 합성과 항균활성 (Studies on Synthesis and Antimicrobial Activity of New ${\beta}-Lactam$ Antibiotics)

  • 고옥현;홍석순;하재천;김영수
    • 약학회지
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    • 제38권3호
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    • pp.322-331
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    • 1994
  • For the development new cephalosporin antibiotics with aminothiazolmethoxyimino moiety in the C-7 position and triazolthiomethyl moiety in the C-3 position of cephem ring, $7{\beta}$-[(z)-2-(2-aminothiasol-4-yl)-2-(methoxyimino)acetamido]-3-[5-(aryl or het.)-4-phenyl-4H-1,2,4-triazol-3-yl]thiomethyl-3-cephem-4-carboxylic acids were synthesized. These compounds were tested for antimicrobial activitiy in vitro against ten species of microorganisms. It showed remarkable antibacterial activity against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341 and Escherichia coli ESS. The antibacterial activity of most new compounds showed more active than cefazoline, but these compounds were lower active than cefotaxime against Pseudomonas aeruginosa IFO 13130.

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고속액체크로마토그라피에 의한 프로스타글란딘류의 고감도 형광 분석법 (A Sensitive Fluorescent Detection Method for Prostaglandins by High Performance Liquid Chromatography)

  • 이용문;문동철
    • 약학회지
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    • 제36권5호
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    • pp.506-511
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    • 1992
  • The Prostaglandins were derivatized rapidly with monodansyl cadaverine as a fluorophore in mild conditions. The carboxylic moiety of prostaglandins was activated with diethyl phosphorocyanidate and successively coupled with fluorophore in dimethylformamide at room temperature. The labeling yield was reached about 95% at 15 min using arachidic acid $(C_{20:0})$ as a test sample. This derivative showed constant fluorescent intensity at $4^{\circ}C$ for 180 days. The derivatives of prostaglandins were shown high solvent selectivity with tetrahydrofuran in reversed-phase column. therefore, these derivatives could be successfully separated on YMC pack A-212(S-5 120A C8) column in tetrahydrofuran-based eluents. The detection limits of these derivatives was ca. 500 fmol and determination limits was ca. 5 pmol as injected amount in fluorescent detection $({\lambda}ex.\;340\;nm,\;{\lambda}em.\;520\;nm)$. In this method, the ranges of recovery and coefficient of variation were $93.6{\sim}102.7%$ and $4.3{\sim}5.8%$, respectively.

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감광성 DMNB 기를 함유한 새로운 포지형 감광성 폴리이미드의 합성 및 물성 (Synthesis and Characterization of New Positive Photosensitive Polyimide Having Photocleavable 4,5-Dimethoxy-2-nitrobenzyl (DMNB) Groups)

  • 최옥자;류윤미;정민국;이명훈
    • 폴리머
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    • 제26권6호
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    • pp.701-709
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    • 2002
  • 새로운 포지티브형 감광성 폴리이미드 전체를 합성하기 위하여, 폴리아믹산의 인부 카르복시산 기를 $K_2$CO$_3$/HMPA 조건 하에서 광분해성 감광성 기인 4,5-dimethoxy-2-nitrobenzyl bromide의 반응시켜 에스테르를 형성하고 나머지 카르복시산기를 화학적 이미드화시켜 poly[imide-co-(amic ester)]를 합성하였다. 합성된 고분자의 구조는 FT-IR, $^1$H-NMR 등으로 확인하였고, DSC와 TGA를 이용하여 열적 특성을 확인하였다. 또한 이 고분자에 자외선을 조사하면 감광성 기인 4,5-dimethoxy-2-nitrobenzyl 기가 분해되어 카르복시산 기를 형성함에 따라 고분자가 알칼리 현상액에 대해 용해하였으며, 이를 이용하여 포지티브 패턴을 형성할 수 있었다. 여러가지 4,5-dimethoxy-2-nitrobenzyl ester 농도를 갖는 poly[imide-co-(amic ester)]의 겔분율 실험을 통하여 감광곡선을 얻었으며, 이를 통해 이 고분자의 감광특성을 조사하였다. 그 결과 감도는 4000~6000 mJ/$\textrm{cm}^2$ 이었으며, 조도는 3.1~4.9 정도인 것으로 확인되었다.

새로운 의약품의 합성에 관한 연구 (Ⅲ) : 새로운 세파로스포린 항생물질의 합성과 그의 생물활성에 관한 연구 (Studies on the Synthesis of New Medicinal Agent (Ⅲ) : Studies on the Synthesis and Antibacterial Activites of New Cephalosporin Derivatives)

  • 최원식;최소영
    • 대한화학회지
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    • 제38권8호
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    • pp.603-607
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    • 1994
  • 새로운 cephalosporin 항생물질인 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(substituted pyrimidin-2-yl)thiomethyl]-3-cephem-4-carboxylic acid derivatives(2a∼2d)유도체들을 합성하였다. 7-ACA의 3-위치에는 pyridinylthiomethyl기를 도입시키고, 7-위치에는 thiazine를 치환시켜서 구조 변화에 대한 항균 활성을 측정하였다. 그 결과 이들 유도체들은 기준물질인 cefotaxim보다 낮은 항균력을 나타내었다.

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시스 또는 트란스-3-아미노-4-메틸티오메틸피롤리디닐기를 포함하는 퀴놀론 항균물질의 합성과 효능검색 (Syntheses and Antibacterial Activities of New Quinolones Containing cis- or trans-3-Amino-4-methylthiomethylpyrrolidino Moiety)

  • Lee, Jae-Wook;Lim, Gui-Taek
    • 생명과학회지
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    • 제13권6호
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    • pp.943-949
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    • 2003
  • 7번 위치에 하롤겐이 치환된 여로종류의 퀴놀론 모핵과 시스 또는 트란스-3-아미노-4-메틸오메틸피롤리딘을 반응시켜 7-(시스 또는 트란스-3-아미노-4-메틸티오메틸피롤리디닐) 퀴롤론-3-카르복실산의 신규 항균제를 합성하였다. 새롭게 합성된 퀴놀론의 약효는 그람양성균에 대해 대조물질인 시프로플로삭신보다 매우 탁월하였고, 녹농균이외의 그람음성균에 대해서도 대조물질과 거의 유사하였다. 그리고 임상에서 문제가 되고 있는 메티실린 내성 포도상구균(MRSA)에 대한 신규 퀴놀론의 약효는 더욱더 향상되어진 것으로 나타났다.

불소계 폴리올에스테르의 합성과 윤활 특성 (Synthesis and Lubrication Properties of Semi-Fluorinated Polyol Esters)

  • 백진욱;정근우;김영운
    • 한국윤활학회:학술대회논문집
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    • 한국윤활학회 2001년도 제33회 춘계학술대회 개최
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    • pp.149-155
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    • 2001
  • New semi-fluorinated polyol esters were synthesized by condensation reaction of polyols (NPG and TMP) and carboxylic acids such as 2-ethylhexanoic acid, stearic acid and perfluorooctanoic acid. The structures of polyol esters were confirmed by FT-IR and H-NMR etc. And, the fluorinated polyol esters were insoluble in several oils, however, the semi-fluorinated polyol esters were soluble in several oils depended on the structure of polyol esters. The physical properties such as 4-ball wear property and extreme-pressure (EP) properties were characterized by measuring wear scar diameter through ASTM D2266 and by determining the load-carrying through ASTM D2783 method, respectively. As the results, wear scar diameters of oils in which the semi-fluorinated polyol esters were added were not changed compared to those of not added oils. While extreme-pressure properties remarkably Increased with fluorine contents of the esters depended on the structure of acid moiety and polyol moiety. Also, the extreme-pressure property of semi-fluorinated NPG polyol ester in gasoline engine oil was better than that of commercial Teflon coating additive.

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Tyrosinase inhibitory effect of gentisic acid derivatives

  • Lee, Yeon-Jung;Yoon, Sung-Il;Kim, Jung-Sun;Lee, Chi-Ho;Kim, Dae-Duk
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.294.2-295
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    • 2003
  • Gentisic acid, a skin-whitening agent, is known to possess tyrosinase inhibition activity. In order to develop an effective skin-whitening agent, hydroquinone derivatives in which the carboxylic acid moiety of gentisic acid was replaced with various functional groups, were selected and evaluated for their ability to inhibit tyrosinase activity as well as to inhibit melanin release. (omitted)

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Synthesis of Nonclassical Quinazolinone Antifolates as Thymidylate Synthase Inhibitors and Their Antitumor Activity In Vitro

  • Baek, Du-Jong;Kang, Tae-Beom;Kim, Hyun-Ju
    • Bulletin of the Korean Chemical Society
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    • 제25권12호
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    • pp.1898-1906
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    • 2004
  • Nonclassical quinazolinone analogs I, II, and III, in which the glutamic acid moiety of the classical antifolates is substituted by phenylglycine, phenylalanine or aminobenzoic acid and their methyl esters, were synthesized and evaluated as lipophilic inhibitors of thymidylate synthase (TS). The target compounds were generally potent inhibitors of L. casei and human TS with $IC_{50}$ values within the narrow range of 0.2-10 ${\mu}$M and 0.003-0.03 ${\mu}$M, respectively. Further, most of the target compounds showed cytotoxicity against tumor cell lines of murine and human origin with $IC_{50}$ values of as low as 0.050 ${\mu}$M. Substitution of another hydroxyl or carboxylic acid/ester group at the phenyl ring further increased the potency of TS inhibition and cell growth inhibition. Most effective were compounds If and Ic in which extra carboxylic acid/ester was present at the phenyl ring with nanomolar $IC_{50}$ values of 0.0044 and 0.0093 ${\mu}$M against human TS and submicromolar cytotoxic growth inhibition against all four tumor cell lines.