• 제목/요약/키워드: Solid phase synthesis

검색결과 313건 처리시간 0.022초

Synthesis of Decapeptide of L-Aspartic Acid and Benzyl-L-Aspartic Acid by Solid Phase Peptide Synthesis

  • Yoo, Bong-K.;Jalil Miah, M.A.;Lee, Eung-Seok;Han, Kun
    • Archives of Pharmacal Research
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    • 제28권7호
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    • pp.756-760
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    • 2005
  • Polyene macrolide amphotericin B (AmB) is the drug of choice for the treatment of disseminated fungal infections. However, because of its pronounced side effects, the drug has limited applicability. There are few interesting reports, which state that co-administration of the drug with homo-peptide of polyaspartic acid reduces the side effects of the drug. In our present study, an approach has been made to systematically synthesize low molecular weight heteropeptides consisting of L-aspartic acid and its derivative. It was hypothesized that such heteropeptides will reduce the toxic side effects of the drug by facile hydrophobic binding between the polymer and the drug. We have employed the strategy of solid phase peptide synthesis (SPPS) to synthesize low molecular weight hetero-peptides by using L-aspartic acid and benzyl-L-aspartic acid to induce the hydrophobic binding between the peptide and the drug. In future, the proposed methodology can be employed to tailor other polypeptides substituted with benzyl groups to reduce the nephrotoxicity of AmB.

연료전지용 LSGM 페로브스카이트계 전해질의 합성 및 특성 연구 (Synthesis and Characterization of LSGM Solid Electrolyte for Solid Oxide Fuel Cell)

  • 성영훈;조승환;;김도경
    • 한국세라믹학회지
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    • 제44권12호
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    • pp.696-702
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    • 2007
  • The family of (Sr,Mg)-doped $LaGaO_3$ compounds, which exhibit high ionic conductivity at $600-800^{\circ}C$ over a wide range of oxygen partial pressure, appears to be promising as the electrolyte for intermediate temperature solid oxide fuel cells. Conventional synthesis routes of (Sr,Mg)-doped $LaGaO_3$ compounds based on solid state reaction have some problems such as the formation of impurity phases, long sintering time and Ga loss during high temperature sintering. Phase stability problem especially, the formation of additional phases at the grain boundary is detrimental to the electrical properties of the electrolyte. From this point of view, we focused to synthesize single phase (Sr,Mg)-doped $LaGaO_3$ electrolyte at the stage of powder synthesis and to apply relatively low heat-treatment temperature using novel synthesis route based on combustion method. The synthesized powder and sintered bulk electrolytes were characterized by XRD, TG-DTA, FT-IR and SEM. AC impedance spectroscopy was used to characterize the electrical transport properties of the electrolyte with the consideration of the contribution of the bulk lattice and grain boundary to the total conductivity. Finally, relationship between synthesis condition and electrical properties of the (Sr, Mg)-doped $LaGaO_3$ electrolytes was discussed with the consideration of phase analysis results.

Solid-phase Parallel Synthesis of a Novel N-[Alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted Amide and Amine Drug-like Libraries

  • Kim, Ji-Hye;Gong, Young-Dae;Lee, Gee-Hyung;Seo, Jin-Soo
    • Bulletin of the Korean Chemical Society
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    • 제33권1호
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    • pp.128-136
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    • 2012
  • We report the solid-phase library construction of 222 number of a novel N-[alkyl sulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B derivatives. The polymer-bound N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 9 and amine 10 derivatives were obtained by first diversity generation with various acid chlorides and alkyl halides. Further reactions on the resins 9 and 10 with substituted sulfonyl chlorides produced the desired N-[alkylsulfonamido-spiro(2H-1-benzopyran-2,4-piperidine)-6-yl] substituted amide 1A and amine 1B analogues.

Solid-phase Synthesis and Preliminary Evaluation of 1,6,8-Trisubstituted Tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as a NF-kB Inhibitor

  • Kim, Jin-Woong;Cho, Jung-Hyuck;Han, Tae-hee;Lee, Jong-Baek;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • 제27권4호
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    • pp.484-488
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    • 2006
  • The solid-phase synthesis of new series of 1,6,8-trisubstituted tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones as bicyclic $\beta$-turn mimetics is described. Their NF-kB inhibition activities were tested and the effect of substituents on bicyclic ring was investigated. Among the prepared compounds, the fluorobenzyl and methoxybenzyl group substituted compounds 26 and 27 at C-1 and C-8 position showed more inhibitory activities than the others. Tested at a concentration of 10 uM, these two compounds showed a 60% inhibition against the target NF kB 549.

$WS_2$ 고체 윤활제의 합성 (Synthesis of $WS_2$ Solid Lubricant)

  • 신동우;윤대현;황영주;김성진;김인섭
    • Tribology and Lubricants
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    • 제13권4호
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    • pp.60-65
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    • 1997
  • The tungsten disulfide $(WS_2)$ solid lubricant was synthesized by two different reaction processes, i.e., the reaction between $CS_2$ gas phase and solid $WO_3$powder, and the vapour phase transport method of tungsten and sulfur in a high vacuum. The chemical and physical characteristics of synthesized $WS_2$powder were analyzed in terms of the average particle size, morphology, crystalline phase etc. in comparison with those of commercial $WS_2$powder. The solid $WO_3$ powder with the average size of 0.2 ${\mu}{\textrm}{m}$ was reacted with $CS_2$gas flowed with$N_2$or 96%$N_2{\times}4%H_2$forming gas for 36 h and 24 h at 90$0^{\circ}C$ respectively. $WS_2$ crystalline phase was then formed through the intermediate phase of .$W_{20}O_{58}$ In the case of vapour phase transport method, the 3.5 wt% iodine was added as a vapour transport reagent into the composition of tungsten and sulfur powders maintaining a constant molar ratio of W:S=1:2.2. The mixture was then heat treated at 85$0^{\circ}C$ for 2 weeks in vacuum. The reaction product obtained showed the average size of 12 ${\mu}{\textrm}{m}$ and the hexagonal plate shape of typical solid lubricant with 2H-$WS_2$crystalline phase.