• 제목/요약/키워드: Oxime

검색결과 134건 처리시간 0.024초

Importance of Imidazolidinone Motif in 4-Phenyl-N-arylsulfonylimidazolidinone for their Anticancer Activity

  • Sharma, Vinay K.;Lee, Ki-Cheul;Joo, Cheon-Ik;Sharma, Niti;Jung, Sang-Hun
    • Bulletin of the Korean Chemical Society
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    • 제32권spc8호
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    • pp.3009-3016
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    • 2011
  • To investigate the possible isosteric replacement of imidazolidinone moiety in 4-phenyl-N-arylsulfonylimidazolidinone for broad and potent anticancer agents, a series of 4-phenyl-l(N)-arylsulfonylimidazolidinones 6a-k, imidazolidinethione analogs 7a-i, and imidazolidine oxime analogs 8a-c were prepared and evaluated for their in vitro anticancer activity against four human cancer cell lines (human lung A549, human colon COLO205, human leukemia K562, human ovary SK-OV-3). Among all the derivatives of N-arylsulfonylimidazolidinone 6a-k, compounds 6f and 6g showed the best inhibition comparable to doxorubicin against all cancer cell lines. Increasing the carbon chain on alkyl moieties of carbamates as shown in 6c-g did not alter the activity. The imidazolidinethione analogs 7a-i and imidazolidin-2-one oxime derivatives 8a-c did not possess any good activity. Therefore, imidazolidinone moiety is the best pharmacophore among the 4-phenyl-Narylsulfonylimidazolidinone derivatives.

Synthesis, Molecular and Microstructural Study of Poly-N-Vinylpyrrolidone Oximo-L-Valyl-Siliconate with IR, 1H-NMR and SEM

  • Singh, Man;Padmaja, G. Vani
    • Bulletin of the Korean Chemical Society
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    • 제31권7호
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    • pp.1869-1874
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    • 2010
  • By reducing PVP with $H_2NOH$.HCl and NaOH 2:2:1 mass ratios in aqueous ethanol, poly-N-vinyl pyrrolidone oxime [PVPO] was prepared with 92% yield. Applying the sol-gel concept, orthosilicic acid [OSA] was made by hydrolyzing TEOS with ethanol in 1:0.5 molar ratios using 1 N KOH aqueous solution as a catalyst. The OSA + PVPO + $_L$-Valine ($\alpha$-amino acid) were mixed with pure ethanolic medium in 1:2:2 mass ratios and refluxed at $78^{\circ}C$ and 6 pH for 6.5 h. A white residue of poly-N-vinyl pyrrolidone oximo-L-valyl-siliconate [POVS] appeared after 5 h. The heating of reaction mixture was stopped and the contents were brought to NTP. The residue formation of POVS was intensified with lowering a temperature and completely solidified within 5 h, was filtered using a vacuum pump with Whatmann filter paper no. 42. The residue of POVS was washed several times with 20% aqueous cold ethanolic solution and dried in vacuum chamber at $25^{\circ}C$ for 24 h. The MP was noted above $350^{\circ}C$. Structural and internal morphology were analyzed with IR and $^1H$-NMR, and SEM respectively. A drug loading and transporting ability of the POVS in water and at pH = 5 and 8 was determined chromatographically.

Zearalenone ELISA kits의 응용에 관한 연구 (Studies on practical application of zearalenone ELISA kits)

  • 윤화중;김태종;이승윤;제갈준;윤지병
    • 대한수의학회지
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    • 제38권2호
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    • pp.297-303
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    • 1998
  • For the extraction and measurement of zearalenone in the corn, bean, wheat and barley contaminated with Fusarium graminearum, the zearalenone-oxime, zearalenone-oxime BSA and zearalenone monoclonal antibodies were studied to develop and apply the direct competitive enzyme linked immunosorbent assay (ELISA). The extraction range of zearalenone with the monoclonal antibodies produced in this experiment was 10ng to 500ng/g feed and the 50% inhibition value was 50ng/ml. The mean recoveries of zearalenone artificially spiked in the ground corn were 89%. The specificity of F-2 monoclonal antibody for the analogues was favorable for the direct competitive ELISA. The result of the experiment showed the zearalenone in the corn, bean, wheat and barely naturally contaminated with the mold would be suitable for extraction and measurement with the monoclonal antibodies.

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라미네이트 강판용 폴리우레탄 접착제의 접착거동 (Adhesion Mechanism of Polyurethane Adhesive for Laminated Steel Plate)

  • 염주선;강호종
    • 폴리머
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    • 제36권2호
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    • pp.119-123
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    • 2012
  • 금속 박막 접착제로 사용되는 용제형 폴리우레탄 접착제의 라미네이팅 조건에 따른 접착 메커니즘과 이에 따른 접착력 변화를 살펴보았다. 강판에 도포된 접착제의 열처리 온도와 시간에 따라 폴리우레탄 접착제의 blocking agent로 사용된 옥심이 분해되어 이소시아네이트기가 발현되고 이들이 강판과 알루미늄 포일의 하이드록실기와 반응하여 강판 접착이 이루어짐을 알 수 있었다. 접착 강도는 접착 온도 및 시간에 따라 발생된 이소시아네이트 함량과 밀접한 관계가 있음을 확인하였다. 하지만 지나친 접착 온도 및 접착 시간의 증가는 접착제에 함유된 용매의 감소와 접착제 분해를 유발시켜 접착 강도를 감소시킴을 알 수 있었다.

A Direct Comparison Study of Asymmetric Borane Reduction of C=N Double Bond Mediated by Chiral Oxazaborolidines

  • Cho Byung Tae;Ryu, Mi Hae;Chun Yu Sung;Dauelsberg Ch.;Wallbaum Sabine;Martens Jurgen
    • Bulletin of the Korean Chemical Society
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    • 제15권1호
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    • pp.53-57
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    • 1994
  • A comparison study on asymmetric borane reduction of ketoxime ethers and N-substituted ketimines possesing C = N double bond mediated by the selected chiral oxazaborolidines (1-6) was investigated. Thus, an aromatic ketoxime O-alkyl ether acetophenone oxime O-methyl ether was reduced to the corresponding amine (1-phenylethylamine 8a) with optical yields, such as 58% ee with 1, 86% ee with 2, 3% ee with 3, 99% ee with 4, 60% ee with 5, and 73% ee with 6. However, the reduction of an aliphatic ketoxime derivative 2-heptanone oxime O-methyl ether provided low optical inductions (7-13% ee). For ketoxime O-trimethylsilyl ethers, the reduction of acetophenone O-trimethylsilyl ether afforded 8a with optical yields which were 90% ee with 1, 40% ee with 2, 2% ee with 3, 62% ee with 4, 5% ee with 5, and 60% ee with 6. The reduction of 2-heptanone O-trimethylsilyl ether also gave the product amine with low optical yields (10-40% ee). In the case of N-substituted ketimines, the reduction of acetophenone N-phenylimine afforded the corresponding amine with 79% ee, 78% ee, 9% ee, 73% ee, 78% ee and 67% ee using 1, 2, 3, 4, 5, and 6, respectively, whereas low optical inductions (5-18% ee) for 2-heptanone N-phenylimine were achieved.

살충제 thiodicarb의 단감 중 잔류분석 및 안전성 평가 (Residue analysis of insecticide thiodicarb in sweet persimmon and its safety evaluation)

  • 노석초;황철환;김민수;마상용;한성수
    • 농약과학회지
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    • 제8권3호
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    • pp.184-188
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    • 2004
  • 살충제 thiodicarb의 단감 중 안전사용기준 설정과 안전성을 평가를 위하여 처리구별 단감 중 thiodicarb의 잔류량을 GLC/NPD로 분석한 결과, thiodicarb의 가수분해 산물인 methomyl oxime의 최소검출량은 0.2 ng이었으며, thiodicarb의 검출한계는 0.05 ppm 이었다. Thiodicarb의 평균 회수율은 0.5 ppm과 2.5 ppm 수준에서 각각 $93.9{\pm}3.9%$$92.8{\pm}2.0%$이었다. 각 처리별 평균 잔류량은 수확전 2회 살포시 $1.50{\pm}0.04$ ppm, 수확전 3회 살포시 $1.86{\pm}0.04$ ppm, 수확전 4회 살포시 $2.11{\pm}0.12$ ppm으로 처리구 모두 thiodicarb의 국내 잠정 잔류허용량(maximum residue limit)인 5 mg/kg 미만이었으며, 단감의 감꼭지나방 방제를 위하여 thiodicarb 40% 수화제를 수확 14일전 4회 살포시 안전성에는 문제가 없을 것으로 판단되었다.

Anthracycline의 합성에 관한 연구

  • 주상섭;하동진;전희정;홍성원
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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    • pp.111-111
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    • 1993
  • Anthracycline의 합성에 있어서 aglycone 뿐만 아니고 sugar도 대단히 중요한 역할을 한다. Anthracycline에 이용되는 sugar인 daunosamine의 전합성의 확립을 통하여 daunosamine의 anlogue을 합성할 목적으로 daunosamine의 전합성을 검토하고 있다. Methyl D-mannopyranoside을 원료로 하여 0-methylation, PhCH(OMe)$_2$ 에 의한 OH의 보호, n-BuLi을 이용한 위치선택적 deblocking, oxime생성, 이어서 Vitride를 이용한 환원으로 daunosamine 합성에 있어서 중요한 중간체인 methyl-3-amino-4,6-benzylidene-2,3-dideoxy-$\alpha$-D-hexopyranoside을 합성하였다.

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