• Title/Summary/Keyword: Combinatorial synthesis

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Design and Combonatorial Synthesis of Selenoflavonoids and Indole Compounds for Neuroprotective Drug

  • Jeong, Jin-Hyun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.69-71
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    • 2003
  • As recent as 10 years ago, a method of developing new medicine was developed by a new compounding method moving away from an existing one. Combinatorial chemistry made it easier to combine various kinds of compounds in a very short time and with little effort from existing methods. Through combinatorial chemistry, a number of compounds were synthesized using HTS(High Throughput Screening), with many reports reaching a clinical stage in search of new candidate material. (omitted)

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Synthesis of Barium Hexaaluminate Phosphros Using Combinatorial Chemistry (조합화학을 이용한 망간(2+)과 유로피움)2+)이 첨가된 Barium Hexaaluminate 형광체의 합성 및 광특성 분석)

  • 박응석;최윤영;손기선;김창해;박희동
    • Journal of the Korean Ceramic Society
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    • v.37 no.2
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    • pp.134-139
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    • 2000
  • The main objective of the present investigation is to show the feasibility of combinatorial chemistry by applying this method to phosphor syntehses. In this respect barium hexaaluminate phosphor was prepared by the split-pool combinatorial method, which enabled much more rapid search of optimum compositions of target phosphors than conventional synthetic methods. Barium hexaaluminate phosphors doped with Eu2+ exhibit blue emission while those co-doped with Mn2+ and Eu2+ exhibit green emission. Basically, the phosphor doped with 1.3 mole of Ba and 0.06~0.15 mole of Eu2+ exhibit the maximum value of emission intensity at 435${\mu}{\textrm}{m}$. Under the UV and VUV extitations, the barium hexaaluminate phosphor co-doped with Mn2+ and Eu2+ shows strong green emission.

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Synthesis of combinatorial library of $\beta$-ketoacetoanilide chlorides and their antifungal activity against main plant pathogens ($\beta$-Ketoacetoanilide 염화물의 조합 라이브러리 합성 및 주요 식물병원균에 대한 항균활성)

  • Hahn, Hoh-Gyu;Nam, Kee-Dal;Bae, Su-Yeal;Yang, Bum-Seung;Lee, Seon-Woo;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
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    • v.8 no.1
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    • pp.8-15
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    • 2004
  • A synthesis of new $\beta$-ketoacetoanilide chloride derivatives and anti fungal activity of these compounds library against 6 typical plant pathogens were described. Reaction of ketene dimer with chlorine followed by treatment of aniline derivatives gave 89 kinds of the corresponding $\beta$-ketoacetoanilide chlorides through combinatorial synthetic technology using Carousel Reaction Stations. Evaluation of antifungal activity (in vivo) of this chemical library against rice blast, rice sheath blight, tomato aray mold, tomato late blight, wheat leaf rust and barley powdery mildew was carried out. In general, $\beta$-ketoacetoanilide chlorides which present a substituent at 4 in phenyl group(para) of the compounds showed selective control activity against tomato late blight caused by Phytophthora infestans.

In Vitro Combinatorial Mutagenesis of the 65th and 222nd Positions of the Green Fluorescent Protein of Aequarea victoria

  • Nakano, Hideo;Okumura, Reiko;Goto, Chinatsu;Yamane, Tsuneo
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.7 no.5
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    • pp.311-315
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    • 2002
  • By the in vitro combinatorial mutagenesis, which is a sequential reaction of PCR mutagenesis and in vitro coupled transcription/translation with Escherichia coli S30 extract, S65 and E222 of green fluorescent protein of Aequarea victoria were comprehensively changed to all possible combinations of amino acids, thus totally 400 mutant (including a wild type) proteins were simultaneously produced and their fluorescent properties were analyzed. Although a few mutations had been reported so far at the 222nd position, replacement E222 to all other19 amino acids gave fluorescent signal to the mutants by changing Ser 65 to Ala together. Among the mutants, replacement to G, A, S, Q, H and C gave relatively high fluorescence. The in vitro combinatorial mutagenesis, therefore, has been proved valuable for comprehensive structure-function studies of proteins.

Effective Generation of Lead Compounds by High Throughput Organic Synthesis: using Multipurpose Privileged Bezopyrans

  • Gong, Young-Dae;Seo, Jin-soo;Hwang, Jong-Yeon;Park, Ji-Yeon;Yoo, Sung-Eun
    • Proceedings of the PSK Conference
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    • 2003.10a
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    • pp.89-89
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    • 2003
  • Numerous lead compounds, based on multipurpose privileged structures, can be generated that address a variety of targets from a gene family of interest, irrespective of therapeutic area. Solid-phase organic synthesis has been emerged as a powerful technique in generating combinatorial libraries of small organic molecules useful for drug discovery. Heterocyclic compounds provide scaffolds on which pharmacophores can be arranged to yield potent and selective drugs and a variety of heterocycles have been synthesized on solid support. (omitted)

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Synthesis of (Gd0.74Y0.11Tb0.15P1.15)OδPhosphors Using Combinatorial Chemistry (조합화학을 이용한 (Gd0.74Y0.11Tb0.15P1.15)Oδ 형광체 합성 및 발광특성)

  • 이재문;유정곤;박덕현;김지식;손기선
    • Journal of the Korean Ceramic Society
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    • v.41 no.5
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    • pp.381-387
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    • 2004
  • Recently developed Plasma Display Panels (PDP) require phosphors of high luminance at Vacuum Ultraviolet (VUV) excitation. The present investigation developed new PDP phosphors using combinatorial chemistry method. We applied T $b^{3+}$ -activated yttrium gadolinium phosphates system to our combinatorial fine-tuning technique. As a result, the optimum composition was determined to be (G $d_{0.74}$ $Y_{0.11}$T $b_{0.15}$) $P_{1.15}$ $O_{\delta}$ through the two-step combinatorial screening process including excess phosphorous and Gd replacement. We found that the sample of the optimum composition shows a higher luminescence efficiency at VUV excitation and a shorter decay time than the commercially available Z $n_2$ $SiO_4$:Mn phosphor.