• 제목/요약/키워드: 1,3,4-Triazole

검색결과 107건 처리시간 0.029초

이트라코나졸 항진균제의 효과적인 합성법 개발 (Development of the Efficient Synthetic Route for Itraconazole Antifungal Agent)

  • 백두종
    • 공업화학
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    • 제17권6호
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    • pp.633-637
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    • 2006
  • 본 연구에서는 triazole계 항진균제인 이트라코나졸의 대량합성을 위한 효과적인 합성법을 제시하였다. Janssen Pharmaceutica에 의해 발표된 기존의 의약화학적 합성경로는 2,4-dichloroacetophenone을 출발물질로 하는 직렬(linear) 합성의 14 단계로서 전체수율이 1.4%에 불과하였고 대량합성에 부적합한 위험물질로서 methanesulfonyl chloride ($CH_{3}SO_{2}Cl$)와 수소기체 및 sodium hydride (NaH)를 사용하고 있다. 또한 고가의 1-acetyl-4-(4-hydroxyphenyl)piperazine 및 팔라듐을 사용함으로써 생산 단가가 높은 문제점이 있었다. 이를 개선하기 위해서 병렬(convergent) 합성 전략을 수립하였는데, 이트라코나졸의 대략 반에 해당하는 중간체 II와 III을 각각 합성한 다음 두 부분을 결합시키는 12단계의 합성공정을 개발하였고 전체 수율은 12.0%로서 합성효율이 크게 개선되었다. 이 과정에서 공정을 간략화하고 위험물질 및 고가의 반응물의 사용을 배제함으로써 생산 원가를 크게 절감시킬 수 있었다.

Conventional and Inverted Photovoltaic Cells Fabricated Using New Conjugated Polymer Comprising Fluorinated Benzotriazole and Benzodithiophene Derivative

  • Kim, Ji-Hoon;Song, Chang Eun;Kang, In-Nam;Shin, Won Suk;Zhang, Zhi-Guo;Li, Yongfang;Hwang, Do-Hoon
    • Bulletin of the Korean Chemical Society
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    • 제35권5호
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    • pp.1356-1364
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    • 2014
  • A new conjugated copolymer, poly{4,8-bis(triisopropylsilylethynyl)benzo[1,2-b:4,5-b']dithiophene-alt-4,7- bis(5-thiophen-2-yl)-5,6-difluoro-2-(heptadecan-9-yl)-2H-benzo[d][1,2,3]triazole} (PTIPSBDT-DFDTBTz), is synthesized by Stille coupling polycondensation. The synthesized polymer has a band gap energy of 1.9 eV, and it absorbs light in the range 300-610 nm. The hole mobility of a solution-processed organic thin-film transistor fabricated using PTIPSBDT-DFDTBTz is $3.8{\times}10^{-3}cm^2V^{-1}s^{-1}$. Bulk heterojunction photovoltaic cells are fabricated, with a conventional device structure of ITO/PEDOT:PSS/polymer:$PC_{71}BM$/Ca/Al ($PC_{71}BM$ = [6,6]-phenyl-$C_{71}$-butyric acid methyl ester); the device shows a power conversion efficiency (PCE) of 2.86% with an open-circuit voltage ($V_{oc}$) of 0.85 V, a short-circuit current density ($J_{sc}$) of 7.60 mA $cm^{-2}$, and a fill factor (FF) of 0.44. Inverted photovoltaic cells with the structure ITO/ethoxylated polyethlyenimine/ polymer:$PC_{71}BM/MoO_3$/Ag are also fabricated; the device exhibits a maximum PCE of 2.92%, with a $V_{oc}$ of 0.89 V, a $J_{sc}$ of 6.81 mA $cm^{-2}$, and an FF of 0.48.

포도당을 이용하여 성장하는 Acinetobacter sp. Strain JC1 DSM 3809에 존재하는 Catalase (Catalases in Acinetobacter sp. Strain JC1 DSM 3803 Growing on Glucose)

  • 신경주;노영태;김영민
    • 미생물학회지
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    • 제32권2호
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    • pp.155-162
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    • 1994
  • 포도당을 이용하여 성장하고 있는 호기성 일산화탄소 산화 세균인 Acinetobacter sp. Strain JC1 DSM 3808애 존재하는 catalase의 활성은 지수성장기 중반에서 높게 나타났으나, 지수성장기 후반 및 정체기 초기에서 낮아졌다가 정체기 중기에서 급격히 증가한 후 다시 감소하였다. 이 세균에는 세종류(Cat1, Cat2, Cat3)의 catalase가 존재하였는데, Cat1과 Cat3의 활성은 성장시기에 따라 큰 차이를 보이지 않았으나 Cat2의 활성은 성장시기에 따라 큰 변화를 나타내었다. Cat3는 이 세균이 포도당을 이용하여 성장할 때만 생성되었고, 일산화탄소나 메탄올을 이용하여 성장할 때는 생성되지 않았다. 세포추출액을 ethanol과 chloroform으로 처리한 후 활성염색을 하였을 때 Cat1과 Cat3의 활성은 안정하였으나 Cat2는 활성을 상실하였다. 세포추출액을 20mM $H_2O_2$와 3-amino-1,2,4-triazole(AT)을 처리하였을 때 Cat1과 Cat3의 활성이 반감되었고, Cat2는 $H_2O_2$에 의해서는 불활성되었으나 AT의 영향은 받지 않았다. Cat1은 80$^{\circ}C$ 1분간 열처리후에도 활성을 나타내었으나, Cat2와 Cat3는 60$^{\circ}C$와 70$^{\circ}C$에서 1분간의 열처리 후 각각 활성을 상실하였다. Cat2는 catalase 활성외에 peroxidase의 활성도 나타내었다. 일곱단계의 과정을 거쳐 포도당에서 성장시에만 생성되는 Cat3를 정제하였다. 정제된 Cat3의 크기는 150,000이었고, 63,000의 크기를 가진 두개의 동일한 소단위로 구성되어 있었으며, $H_2O_2$에 대한 K_m값은 39mM과 58mM로 나타났다. 정제된 효소의 활성을 위한 최적 pH는 7.0이었으나 전반적으로 pH 6~9에서 비슷하게 높은 활성을 나타내었다. 정제된 효소의 최적온도는 40$^{\circ}C$이었으며 20~50$^{\circ}C$에서 비슷한 활성을 나타내었고, 30$^{\circ}C$에서는 60분동안 효소활성이 거의 상실되지 않았다. 정제된 효소는 ethanol과 chloroform 처리에는 안정하였으나 12mM AT 와 0.1mM $NaN_3$ 및 1mM KCN에 의해 90% 이상의 활성이 억제되었다.

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Phytochemical Screening and Antibacterial Activity Coix lacryma-jobi Oil

  • Diningrat, Diky Setya;Risfandi, Marsal;Harahap, Novita Sari;Sari, Ayu Nirmala;Kusdianti, Kusdianti;Siregar, Henny Kharina
    • Journal of Plant Biotechnology
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    • 제47권1호
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    • pp.100-106
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    • 2020
  • Coix lacryma-jobi (Hanjeli) is known to posses anti-microbial properties. Therefore, phytochemical compounds of C. lacryma-jobi have been studied to produce novel antimicrobial agents as treatments against antibiotic-resistant bacteria.The objective of this study was to determine the phytochemical composition and antibacterial activity of the C. lacryma-jobi oil against Escherichia coli, Staphylococcus aureus, and Bacillus subtilis. The phytochemical composition of the oil was determined via gas chromatography mass spectrophotometry (GC-MS). Moreover, agar disk and agar well diffusion were employed to screen the antibacterial activity of the oil. An agar well diffusion test was implemented to determinate MIC's (minimum inhibitory concentrations). Dodecanoic acid, tetradecanoic acid, 2,3-dihydroxypropylester, 1,3-dioctanoin, N-methoxy-N-methyl-3,4-dihydro-2H-thiopyran6-carboxamide, propanamide, 5-Amino-1-(quinolin-8-yl)-1,2,3-triazole-4-carboxamide, and pyridine were identified in the C. lacryma-jobi oil. The MIC value of the oil was 0.031 g/L and the MBC of the oil was 0.125 g/L effective in all test bacteria. Dodecanoic acid displayed inhibitory activity against gram-positive and gram-negative bacteria. Therefore, our research demonstrated C. lacryma-jobi (Hanjeli) oil exhibited antibacterial activity against E. coli, S. aureus, and B. subtilis. These research suggest that C. lacryma-jobi root oil could be used for medicinal purposes; however clinical and in vivo tests must be performed to evaluate its potential as an antibacterial agent.

Antioxidant Effect of Captopril and Enalapril on Reactive Oxygen Species-Induced Endothelial Dysfunction in the Rabbit Abdominal Aorta

  • Kim, Ji Hoon;Kim, Hyuck;Kim, Young Hak;Chung, Won-Sang;Suh, Jung Kook;Kim, Sung Jin
    • Journal of Chest Surgery
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    • 제46권1호
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    • pp.14-21
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    • 2013
  • Background: Reactive oxygen species (ROS) are known to be related to cardiovascular diseases. Many studies have demonstrated that angiotensin-converting enzyme inhibitors have beneficial effects against ROS. We investigated the antioxidant effect of captopril and enalapril in nitric oxide mediated vascular endothelium-dependent relaxations. Materials and Methods: Isolated rabbit abdominal aorta ring segments were exposed to ROS by electrolysis of the organ bath medium (Krebs-Henseleit solution) after pretreatment with various concentrations (range, $10^{-5}$ to $3{\times}10^{-4}$ M) of captopril and enalapril. Before and after electrolysis, the endothelial function was measured by preconstricting the vessels with norepinephrine ($10^{-6}$ M) followed by the cumulative addition of acetylcholine (range, $3{\times}10^{-8}$ to $10^{-6}$ M). The relevance of the superoxide anion and hydrogen peroxide scavenging effect of captopril and enalapril was investigated using additional pretreatments of diethyldithiocarbamate (DETCA, 0.5 mM), an inhibitor of Cu/Zn superoxide dismutase, and 3-amino-1,2,4-triazole (3AT, 50 mM), an inhibitor of catalase. Results: Both captopril and enalapril preserved vascular endothelium-dependent relaxation after exposure to ROS in a dose-dependent manner (p<0.0001). Pretreatment with DETCA attenuated the antioxidant effect of captopril and enalapril (p<0.0001), but pretreatment with 3AT did not have an effect. Conclusion: Both captopril and enalapril protect endothelium against ROS in a dose-dependent fashion in isolated rabbit abdominal aortas. This protective effect is related to superoxide anion scavenging.

부식 방지제에 따른 코발트의 화학 기계적 연마 특성 및 표면 분석 (Investigation on the Effect of Corrosion Inhibitor on Removal Rate and Surface Characteristic of Cobalt Chemical Mechanical Polishing)

  • 정은수;표성규
    • 한국표면공학회지
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    • 제57권3호
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    • pp.140-154
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    • 2024
  • As the trend towards miniaturization in semiconductor integration process, the limitations of interconnection metals such as copper, tungsten have become apparent, prompting research into the emergence of new materials like cobalt and emphasizing the importance of studying the corresponding process conditions. During the chemical mechanical polishing (CMP) process, corrosion inhibitors are added to the slurry, forming passivation layers on the cobalt surface, thereby playing a crucial role in controlling the dissolution rate of the metal surface, enhancing both removal rate and selectivity. This review investigates the understanding of the cobalt polishing process and examines the characteristics and behavior of corrosion inhibitors, a type of slurry additive, on the cobalt surface. Among the corrosion inhibitors examined, benzotriazole (BTA), 1,2,4-triazole (TAZ), and potassium oleate (PO) all improved surface characteristics through their interaction with cobalt. These findings provide important guidelines for selecting corrosion inhibitors to optimize CMP processes for cobalt-based semiconductor materials. Future research should explore combinations of various corrosion inhibitors and the development of new compounds to further enhance the efficiency of semiconductor processes.

Purification and Characterization of a Catalase from Photosynthetic Bacterium Rhodospirillum rubrum S1 Grown under Anaerobic Conditions

  • Kang Yoon-Suk;Lee Dong-Heon;Yoon Byoung-Jun;Oh Duck-Chul
    • Journal of Microbiology
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    • 제44권2호
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    • pp.185-191
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    • 2006
  • The photosynthetic bacterium, Rhodospirillum rubrum S1, when grown under anaerobic conditions, generated three different types of catalases. In this study, we purified and characterized the highest molecular weight catalase from the three catalases. The total specific catalase activity of the crude cell extracts was 88 U/mg. After the completion of the final purification step, the specific activity of the purified catalase was 1,256 U/mg. The purified catalase evidenced an estimated molecular mass of 318 kDa, consisting of four identical subunits, each of 79 kDa. The purified enzyme exhibited an apparent Km value of 30.4 mM and a Vmax of 2,564 U against hydrogen peroxide. The enzyme also exhibited a broad optimal pH $(5.0{\sim}9.0)$, and remained stable over a broad temperature range $(20^{\circ}C{\sim}60^{\circ}C)$. It maintained 90% activity against organic solvents (ethanol/chloroform) known hydroperoxidase inhibitors, and exhibited no detectable peroxidase activity. The catalase activity of the purified enzyme was reduced to 19 % of full activity as the result of the administration of 10 mM 3-amino-1,2,4-triazole, a heme-containing catalase inhibitor. Sodium cyanide, sodium azide, and hydroxylamine, all of which are known heme protein inhibitors, inhibited catalase activity by 50 % at concentrations of $11.5{\mu}M,\;0.52{\mu}M,\;and\;0.11{\mu}M$, respectively. In accordance with these findings, the enzyme was identified as a type of monofunctional catalase.

백서 교종 세포에서 레티노인산에 의한 카탈라제의 활성 증가가 방사선감수성에 미치는 효과 (Increased Catalase Activity by All-trans Retinoic Acid and Its Effect on Radiosensitivity in Rat Glioma Cells)

  • 김화;전하연;김원동;안희열;유재란;박우윤
    • Radiation Oncology Journal
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    • 제23권4호
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    • pp.211-216
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    • 2005
  • 목적: all-trans retinoic acid (ATRA)는 뇌종양 세포의 증식억제효과가 있으며, ATRA와 방사선의 병용은 악성 뇌종양의 치료 효과를 증진시키는 방법이 될 수 있다. 그러나 ATRA에 의해 항산화효소가 증가되며 이로 인해 방사선에 의해 생성된 reactive oxygen species (ROS)가 제거된다면 방사선의 효과는 낮아질 수 있다. 본 연구에서는 ATRA에 의해 유도되는 카탈라제(catalase)에 의한 방사선감수성의 변화를 보고자하였다. 대상 및 방법: 백서 교종세포(36B10)을 대상으로 ATRA 및 ATRA의 화학적 억제제인 3-amino-1, 2, 4-triazole (ATZ) 와 병용하여 카탈라제 활성도, 방사선감수성 및 ROS의 변화를 측정하였다. 카탈라제 활성도는 $H_2O_2$의 소멸을 자외선 분광광도계로 측정하는 방법을 이용해 정량하였으며, 방사선감수성은 단일집락군형성능력으로, ROS 는 2, 7-dichlorofluorescein diacetate 를 분광광도계로 측정하였다. 결과: 카탈라제 활성도는 ATRA의 농도(10, 25, $50{\mu}M$)에 따라 증가하였다. ATRA ($10{\mu}M$)와 방사선(4 Gy)의 병용에 의해 생존분획은 상승적(supra-auditive)으로 감소하였으며, 이 감소된 생존분획은 ATZ 동시 투여에 의해 증가하였다. ATRA $10{\mu}M$ 또는 $25{\mu}M$을 48시간 처리 후 ROS는 대조군에 비해 각각 1.5배, 2배 증가하였고, 4 Gy와 ATRA의 병용군에서는 2.5배 증가하였다. ATRA와 방사선의 병용에 의해 증가된 ROS는 ATZ에 의해 감소되었다. 결론: ATRA에 의해 유도되는 카탈라제는 방사선감수성을 감소시키지 않으며, 오히려 ROS의 증가에 의해 방사선감수성을 상승시켰다. 따라서 ATRA와 방사선의 병용은 뇌종양의 치료에 유용한 방법이 될 수 있을 것으로 보인다.

흡광광도법을 이용한 포름알데히드 확산측정기의 평가 (Evaluation of a Diffusive Sampler for the Measurement of Formaldehyde using Colorimetric Method)

  • 임봉빈;김선규;정의석;김선태
    • 대한환경공학회지
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    • 제27권6호
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    • pp.606-613
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    • 2005
  • 본 연구에서는 실내공기 중 포름알데히드를 측정하기 위해 세 가지 다른 반응의 흡광광도법(비색분석)을 응용한 뱃지형 확산측정기를 평가하였다. 흡수여지의 세척방법을 비교한 결과 사용된 세척용액의 종류에 관계없이 세척하지 않은 경우 보다 양호한 세척효과가 나타났다. 각 측정방법에서 사용될 흡수액의 농도는 시료채취율을 기준으로 정하였다. 평가된 공시험 값은 측정방법별로 15% 이내의 편차를 가진 것으로 나타나 대체적으로 안정적인 것으로 나타났다. 확산측정기의 재현성은 MBTH법이 상대표준편차 10% 이내로 가장 양호하며, 채취된 포름알데히드 양과 시간가중평균농도와의 상관관계는 세 가지 측정방법 모두 양호한 것으로 나타났다. 검출한계 및 정량한계는 시료채취율이 가장 좋은 MBTH법이 다른 측정방법과 비교하여 가장 낮게 나타나 시료채취율이 가장 크고 정량한계가 낮은 측정방법일수록 포름알데히드 측정에 요구되는 측정시간이 감소되는 것으로 나타났다.

In vitro Conidial Germination and Mycelial Growth of Fusarium oxysporum f. sp. fragariae Coordinated by Hydrogen Peroxideand Nitric Oxide-signalling

  • Do, Yu Jin;Kim, Do Hyeon;Jo, Myung Sung;Kang, Dong Gi;Lee, Sang Woo;Kim, Jin-Won;Hong, Jeum Kyu
    • 한국균학회지
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    • 제47권3호
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    • pp.219-232
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    • 2019
  • Chemicals related to hydrogen peroxide ($H_2O_2$) and nitric oxide (NO) generations were exogenously applied to Fusarium oxysporum f. sp. fragariae (Fof) causing Fusarium wilt disease in strawberry plants, and regulations of in vitro conidial germination and mycelial growth of the fungus by the chemical treatments were evaluated. $H_2O_2$ drastically reduced the conidial germination of Fof in a dose-dependent manner, and treatment with 3-amino-1,2,4-triazole (3-AT) catalase inhibitor also led to dose-dependent inhibition of conidial germination but relatively moderately. Gradual decreases in mycelial growth of Fof were found by high concentrations of $H_2O_2$, whilst exogenous 3-AT slightly increased the mycelial growth. Increasing sodium nitroprusside (SNP) NO donor, $N^G$-nitro-l-arginine methyl ester (L-NAME) NO synthase (NOS)-inhibitor and tungstate nitrate reductase (NR) inhibitor led to dose-dependent reductions in conidial germination of Fof in quite different levels. SNP conversely increased the mycelial growth but increasing L-NAME moderately decreased the mycelial growth. Tungstate strongly enhanced mycelial growth. Differentially regulated in vitro mycelial growths of Fof were demonstrated by SNP, L-NAME and tungstate with or without $H_2O_2$ supplement. Superoxide anion production was also regulated during the mycelial growth of Fof by nitric oxide. These results show that $H_2O_2$ and NO-associated enzymes can be suggested as fungal growth regulators of Fof as well as eco-friendly disease-managing agents in strawberry production fields.