• 제목/요약/키워드: Combinatorial synthesis

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조합화학을 이용한 CaO-Y2O3-Al2O3계의 Tb활성 형광체의 합성 및 검색 (Combinatorial Synthesis and Screening of the Tb-activated Phosphors in the System CaO-Y2O3-Al2O3)

  • 윤호신;김창해;강윤찬;유승곤;박희동
    • 한국재료학회지
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    • 제13권12호
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    • pp.785-790
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    • 2003
  • We have synthesized some phosphors in the system $CaO-Y_2$$O_3$-$Al_2$$O_3$by combinatorial polymerized-complex method. Composition and synthetic temperature of phosphors in the library was screened from the emission intensities of individual samples under VUV excitation. In $Tb^{ 3+}$-activated $CaO-Y_2$$O_3$-$Al_2$$O_3$, green phosphors showing good intensity were found to be X$O_3$$O_{7}$, CaYA1O$_4$, YA1O$_3$, $Y_3$$Al_{5}$$O_{12}$, $Y_4$$A1_2$$O_{9}$ .

Excavation of Lead Compounds that Inhibit Mast Cell Degranulation by Combinatorial Chemistry and Activity-Guided

  • Hahn, Hoh-Gyu;Oh, Heong-Sub;Cheon, Seung-Hoon;Oak, Min-Ho;Kim, Young-Ran;Kim, Kyeong-Man
    • Archives of Pharmacal Research
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    • 제27권5호
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    • pp.518-523
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    • 2004
  • An allergic reaction ensues after antigen binds to mast cell or basophil high affinity IgE receptor, Fc$\varepsilon$RI, resulting in degranulation of various inflammatory mediators that produce various allergic symptoms. In this study, i) we isolated the active component for the inhibition of mast cell degranulation from the extract of leaves of Castanea crenata and identified it as quercetin; ii) we established the total synthesis procedure of quercetin; iii) using quercetin as positive control, we excavated some lead compounds that possess inhibitory activities for mast cell degranulation by screening the chemical libraries of 1,3-oxazolidine derivatives prepared by solid phase combinatorial chemistry. Some of 1,3-oxazolidine compounds possessing acetyl and 3',4'-dichlorophenyl group displayed strong inhibitory activities on Fc$\varepsilon$RI-mediated mast cell degranulation, suggesting that they can be used as lead compounds for the development of anti-allergic agents.

Synthesis of ZrTiO4 and Ta2Zr6O17 Films by Composition-Combinatorial Approach through Surface Sol-Gel Method and Their Dielectric Properties

  • Kim, Chy-Hyung
    • Bulletin of the Korean Chemical Society
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    • 제28권9호
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    • pp.1463-1466
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    • 2007
  • Single phases of multi-component oxides films, ZrTiO4 and Ta2Zr6O17, could be synthesized by using the combinatorial approach through surface sol-gel route, coating the appropriate mole ratio of 100 mM zirconium butoxide, tantalum butoxide and titanium butoxide precursors on Pt/Ti/SiO2/Si (100) substrate, following pyrolysis at 450 oC, and annealing them at 770 oC. Both the films and bulks of ZrTiO4 and Ta2Zr6O17 showed very stable dielectric properties in temperature range, ?140 to 60 oC, and frequency range, 100 Hz to 1 MHz, promising their applications in wide range of temperatures and frequencies. The dielectric constants of the films were lower and a little more dependent on frequency than those of the bulks. The reduction of dielectric property in the film was mainly due to the interfacial effects that worked as series and parallel-connected capacitances toward the substantial film capacitance.

Liquid-Phase Synthesis of Biaryl Compounds by the Hydrogenolysis of Pentaerythritol-Supported Biarylsulfonates

  • Kim, Chul-Bae;Lee, Sung-Kyung;Park, Kwang-Yong
    • Bulletin of the Korean Chemical Society
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    • 제31권9호
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    • pp.2459-2466
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    • 2010
  • Unfunctionalized biaryl compounds were parallelly and combinatorially prepared by the traceless hydrogenolysis of biarylsulfonates supported on pentaerythritol. The hydrogenolysis using 2-propylmagnesium chloride in the presence of $dppfNiCl_2$ efficiently generated corresponding biaryl derivatives without any memory of the support. The strategy using pentaerythritol as a small soluble support was disclosed to have a potential to combine the benefits of both SPOS and solution-phase reaction with fast reaction rate, facile isolation of intermediates, easy analysis of intermediates and atom economical manner. The novel tetrapodal support is expected to be an efficient substitute for polymeric supports in many circumstances.

Combinatorial Synthesis and Screening of the Eu-activated Phosphors in the System MO-$Al_2O_3-SiO_2$(M=Sr, Ba)

  • Yoon, Ho-Shin;Park, Jung-Kyu;Kim, Chang-Hae
    • 한국정보디스플레이학회:학술대회논문집
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    • 한국정보디스플레이학회 2004년도 Asia Display / IMID 04
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    • pp.650-653
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    • 2004
  • We have synthesized some phosphors in the system MO-$Al_2O_3-SiO_2$(M=Sr, Ba) by combinatorial polymerized-complex method. Composition and synthetic temperature of phosphors in the liblary was screened from the emission intensities of individual samples under 365nm excitation. As we were screened the higher luminescent candidate composition (or candidate host lattice) at 365nm excitation, investigated whether good radiation was possible at the 405 or 465nm excitation by give the host lattice to be discovered more various change. From libraries about 2 systems, the compound to be expected in long wavelength among the compound to be screened are $Sr_4Al_{14}O_{25}$, $Sr_3Al_2O_6$, $SrAl_2Si_2O_8$, and $BaAl_2Si_2O_8$.

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Combinatorial Synthesis and Screening of the Tb-activated Phosphors in the System $CaO-Y_{2}O_3-Al_{2}O_{3}$

  • Yoon, Ho-Shin;Kim, Chang-Hae;Park, Hee-Dong;Ryu, Seung-Kon
    • 한국정보디스플레이학회:학술대회논문집
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    • 한국정보디스플레이학회 2003년도 International Meeting on Information Display
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    • pp.836-839
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    • 2003
  • We have synthesized some phosphors in the system $CaO-Y_{2}O_3-Al_{2}O_{3}$ by combinatorial polymerized-complex method. Composition and synthetic temperature of phosphors in the liblary was screened from the emission intensities of individual samples under VUV excitation. In $Tb^{3+}$-activated $CaO-Y_{2}O_3-Al_{2}O_{3}$, green phosphors showing good intensity were found to be $CaYAl_{3}O_{7}$, $CaYalO_{4}$, $YAlO_{3}$, $Y_{3}Al_{5}O_{12}$, $Y_{4}Al_{2}O_{9}$, $Ca_{3}Al_{2}O6$.

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Engineering of Biosynthesis Pathway and NADPH Supply for Improved L-5-Methyltetrahydrofolate Production by Lactococcus lactis

  • Lu, Chuanchuan;Liu, Yanfeng;Li, Jianghua;Liu, Long;Du, Guocheng
    • Journal of Microbiology and Biotechnology
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    • 제31권1호
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    • pp.154-162
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    • 2021
  • L-5-methyltetrahydrofolate (5-MTHF) is one of the biological active forms of folate, which is widely used as a nutraceutical. However, low yield and serious pollution associated with the chemical synthesis of 5-MTHF hampers its sustainable supply. In this study, 5-MTHF production was improved by engineering the 5-MTHF biosynthesis pathway and NADPH supply in Lactococcus lactis for developing a green and sustainable biosynthesis approach. Specifically, overexpressing the key rate-limiting enzyme methylenetetrahydrofolate reductase led to intracellular 5-MTHF accumulation, reaching 18 ㎍/l. Next, 5-MTHF synthesis was further enhanced by combinatorial overexpression of 5-MTHF synthesis pathway enzymes with methylenetetrahydrofolate reductase, resulting in 1.7-fold enhancement. The folate supply pathway was strengthened by expressing folE encoding GTP cyclohydrolase I, which increased 5-MTHF production 2.4-fold to 72 ㎍/l. Furthermore, glucose-6-phosphate dehydrogenase was overexpressed to improve the redox cofactor NADPH supply for 5-MTHF biosynthesis, which led to a 60% increase in intracellular NADPH and a 35% increase in 5-MTHF production (97 ㎍/l). To reduce formation of the by-product 5-formyltetrahydrofolate, overexpression of 5-formyltetrahydrofolate cyclo-ligase converted 5-formyltetrahydrofolate to 5,10-methyltetrahydrofolate, which enhanced the 5-MTHF titer to 132 ㎍/l. Finally, combinatorial addition of folate precursors to the fermentation medium boosted 5-MTHF production, reaching 300 ㎍/l. To the best of our knowledge, this titer is the highest achieved by L. lactis. This study lays the foundation for further engineering of L. lactis for efficient 5-MTHF biosynthesis.

An Efficient Synthesis of α-Amino-δ-valerolactones by the Ugi Five-Center Three-Component Reaction

  • Kim, Young-Bae;Park, Soo-Jung;Geum, Gyo-Chang;Jang, Min-Seok;Kang, Soon-Bang;Lee, Duck-Hyung;Kim, You-Seung
    • Bulletin of the Korean Chemical Society
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    • 제23권9호
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    • pp.1277-1320
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    • 2002
  • A novel approach to ${\alpha}-amino-{\delta}-valerolactone$ derivatives 8 by the intramolecular Ugi five-center three-component reaction (U-5C-3CR) using the multifunctional starting material, L-pentahomoserine 5 is described.

Rapid Analysis of Metabolic Stability and Structure of Metabolites in New Drug Development

  • Kim, Dong-Hyun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.86-87
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    • 2002
  • Recent technological innovations in the drug discovery process such as combinatorial synthesis and high throughput screening have led to the identification of an increasingly large number of compounds at the hits-to-leads stage. Therefore, rapid and precise pharmacokinetic/metabolic screening is essential to enhance the tractability of selected leads and to minimize the risk of failure in the later stages of drug development. (omitted)

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