• 제목/요약/키워드: Biological Synthesis

검색결과 1,242건 처리시간 0.025초

Synthesis and Antibacterial Activity of Novel [3-(4-substitutedphenylamino)-8-azabicyclo [3.2.1] oct-8yl]-phenyl-methanone Derivatives

  • Reddy, B. Surendra;Reddy, A. Babul;Reddy, G. Ramachandra;Reddy, P. Raveendra
    • 대한화학회지
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    • 제55권6호
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    • pp.969-973
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    • 2011
  • The synthesis, as well as spectroscopic and biological studies of a novel class of [3-(4-substitutedphenylamino)-8-azabicyclo [3.2.1] oct-8yl]-phenyl-methanone derivatives are described. All the synthesized compounds were characterized by elemental analysis FTIR, $^1H$-NMR, $^{13}C$ NMR, and Mass spectral data. All the synthesized compounds were exhibit in vitro antibacterial activity.

Synthesis of Diblock Codendrimer by Double Click Chemistry

  • Lee, Jae Wook;Han, Seung Choul;Ji, Won Ho;Jin, Sung-Ho;Kim, Ji Hyeon
    • Bulletin of the Korean Chemical Society
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    • 제33권12호
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    • pp.4103-4108
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    • 2012
  • Efficient double click methods for the synthesis of diblock codendrimers were developed. The synthetic strategy involved the sequential click reactions between an alkyne and an azide. The short core building block, 1,4-diazidobutane, was chosen to serve as the azide functionalities for dendrimer growth via click reactions with the alkyne-functionalized PAMAM dendrons as hydrophilic dendron and alkyne-functionalized Fr$\acute{e}$chet-type dendrons as hydrophobic dendron. The structure of diblock codendrimers was confirmed by $^1H$ and $^{13}C$ NMR spectroscopy, IR spectroscopy, mass spectrometry, and GPC analysis.

Fibrostatins의 부분 합성 (Partial Synthesis of Fibrostatins)

  • 이관희
    • 대한화학회지
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    • 제47권1호
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    • pp.47-58
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    • 2003
  • 알킬화제로 작용할 수 있는 naphthoquinones인 fibrostatin이 Streptomyces catanulae subsp. griseospora 배양액으로부터 추출되었다. 이들 quinone 화합물의 합성은 이 화합물들의 생물학적 반응성 연구에 매우 중요하다. 본 논문에서는 효과적으로 치환체들의 위치를 조절할 수 있는 방법인 Hooker oxidation을 이용하여 fibrostatin B를 합성하였다.

Acyclic Anhydrides를 이용한 피리다진아민의 아실레이션; N-치환된 3-아미노-6-클로로피리다진 유도체의 합성 (Acylation of Pyridazinylamines by Acyclic Anhydrides; Synthesis of N-Substituted 3-Amino-6-chloropyridazines)

  • 박은희;박명숙
    • 약학회지
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    • 제49권1호
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    • pp.56-59
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    • 2005
  • We synthesized new N-substituted 3-amino-6-chloropyridazine derivatives which were expected to retain biological activity. All synthetic process from pyridazine to 3-aminopyridazines could be carried out conveniently in high yield. N-Substituted 3-amino-6-chloropyridazine derivatives were prepared through amination and acylation from 3,6-dichloropyridazine. 3-Amino-6-chloropyridazine was prepared from the reaction of 3,6-dichloropyridazine with liquid ammonia under autoclave for 6 hrs. The refluxing of 3-amino-6-chloropyridazine and the corresponding acid anhydride for $1{\sim}2$ hrs afforded the N-substituted 3-amino-6-chloropyridazines. Alkyl chain of N-substituent was prolonged to six carbon (hexanoic acid).

Synthesis and Evaluation of Biological Properties of Benzylide-neacetophenone Derivatives

  • Oh, Sei-Kwan;Jang, So-Yong;Kim, Dong-Hyun;Han, Inn-Oc;Jung, Jae-Chul
    • Archives of Pharmacal Research
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    • 제29권6호
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    • pp.469-475
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    • 2006
  • A series of yakuchinone B 1f and its analogs 1a-e was synthesized and evaluated for free radical scavenging, suppression of LPS-induced NO generation, cytotoxicity and anti-excitotoxicity in vitro. Compound 1c exhibited potent anti-excitotoxicity, while all compounds 1a-f showed considerable effects of free radical scavenging, suppression of LPS-induced NO generation, and cytotoxicity in microglia.

Synthesis and Anti-HIV Activity of Sulfonated Amino Ribofuranans

  • Kang, Byoung-Won
    • Archives of Pharmacal Research
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    • 제26권6호
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    • pp.441-445
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    • 2003
  • New sulfonated amino ribofuranans were synthesized to elucidate the relationship between structure and specific biological activities such as anti-HIV and blood anticoagulant activities. The synthesis was performed by sulfonation of copolymers having various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranosidic unit. The sulfonation with piperidine N-sulfonic acid produced the sulfonated amino ribofuranans in high yield. The anti-HIV activity of sulfonated 3-amino-3-deoxy-(1$\rightarrow5)-\alpha$-D-ribofuranan showed more potent by increasing the degree of sulfonation and the average molecular weights. This activity was almost equal to the activities of sulfonated ribofuranans and ribopyranans reported before in spite of low molecular weight. The blood anticoagulant activities was observed at 36-48 mg/units, more potent than standard dextran sulfonate, 22.7 mg/units. In addition, the blood anticoagulant activities of sulfamide-copolysaccharide consisting various proportion of (1$\rightarrow5)-\alpha$-D-ribofuranan units were potentiated by increasing sulfonated amino-ribofuranan units from 13 to 21 mg/units.

A Study of a Biodegradale Inorganic-Organic Composite Artificial Bone Substitute -Part 1. Synthesis of an Apatite with Similar Crystallinity to Bone-

  • Choon Ki Lee;Hwal Suh
    • 대한의용생체공학회:의공학회지
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    • 제15권2호
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    • pp.195-200
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    • 1994
  • To develop an artificial bone substitute that is gradually degraded and replaced by the regenerated natural bone, the authors designed a composite that consists consisted of calcium phosphate and collagen according to the natural bone's main composition. The crystallinity of the synthesized apatite was shown to depend on the synthesis temperature. Carbonate apatite synthesized at $58{\circ}C$ demonstrated crystallinity very similar to that of the natural bone. By sintering the apatite over $700{\circ}C$ in vacuum, porous carbonate apatite could be obtained, and the pore extent was controllable according to the additive hydrogenperoxide volume.

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Synthesis and Biological Investigations of New Thiazolidinone and Oxadiazoline Coumarin Derivatives

  • Abd Elhafez, Omaima Mohamed;El Khrisy, Ezz El Din Ahmed Mohamed;Badria, Farid;Fathy, Alaa El Din Mohamed
    • Archives of Pharmacal Research
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    • 제26권9호
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    • pp.686-696
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    • 2003
  • Ethyl (coumarin-4-oxy)acetate 1 was prepared through the reaction of 4-hydroxycoumarin with ethyl bromoacetate. Compound 1 was allowed to react with hydrazine hydrate to produce coumarin-4-oxyacetic hydrazide 2. The synthesis of N-(arylidene and alkylidene)-coumarin-4-oxyacetic hydrazones 3-20 was performed. The preparation of 2-substituted-3-[(coumarin-4-oxy) acetamido]thiazolidinones 21-26 and 2-[(coumarin-4-oxy )methyl]-4-acetyl-5-substituted-$\Delta^2$-1,3,4-oxadiazolines 27-33 was performed by the reaction of the hydrazones 3, 4, 7, 9, 12, 14 with mercaptoacetic acid and the hydrazones 3, 4, 5, 7, 12, 15, 16 with acetic anhydride, respectively. The antiviral activities, cytotoxicities and structure-activity relationship (SAR) towards different microorganisms of the prepared compounds were studied.

Asymmetric Synthesis of 12(S)-HETE

  • Suh, Young-Ger;Kim, Jin-Kwan;Min, Kyung-Hoon;Seo, Seung-Yong;Lee, Bo-Young;Han, Young-Taek
    • 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.364.2-364.2
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    • 2002
  • (S) and (R) 12-HETE. endogenous eicosanoids. have recently been discovered to be implicated in a number of important biological activities. In particular. it has recently been reported by us that both the capsaicin-activated channel of sensory neurons and the cloned capsaicin receptor (VR1) are activated by the eicosanoids including these metabolites. We report herein a novel and efficient asymmetric synthesis of highly enantiomerically enriched 12(S)-HETE via enzymatic kinetic resolution of the key allylic alcohol synthon. (omitted)

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GSK3${\beta}$의 선택적 저해제인 Kenpaullone의 B16 멜라노마 및 인간 멜라노사이트에서의 영향 (Effect of Kenpaullone, a Specific Inhibitor of GSK3${\beta}$, on Melanin Synthesis in B16 Melanoma and Human Melanocytes)

  • 김해종;이유리;호앙구엔;이향복;김은기
    • 대한화장품학회지
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    • 제37권3호
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    • pp.211-218
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    • 2011
  • Glycogen synthase kinase 3 beta (GSK3${\beta}$)의 선택적 저해제인 Kenpaullone가 B16 멜라노마 및 사람의 멜라노사이트에 미치는 멜라닌 합성능을 조사하였다. Kepaullone은 B16 멜라노마 및 사람의 멜라노사이트에 대하여 세포증식에는 영향이 없는 범위 내에서 농도 의존적으로 멜라닌 합성을 촉진시켰다. B16 멜라노마 세포에 Kenpaullone을 첨가 48 h 후 tyrosinase 활성이 증가하였으며, 농도별 처리에 대하여 tyrosinase 단백질의 발현 및 tyrosinase mRNA양이 증가함을 관찰하였다. 결론적으로 Kenpaullone는 B16 멜라노마 세포에서 tyrosinase 효소의 발현을 증가시켜 멜라닌 합성을 촉진하는 것으로 판단되어진다. 따라서 GSK3${\beta}$ 저해제가 멜라닌 합성을 촉진시키는 결과는 백반증과 같은 저색소관련 질병의 치료제 개발의 가능성을 갖고 있는 소재로서 응용가능하리라고 판단되어진다.