• 제목/요약/키워드: active agents

검색결과 658건 처리시간 0.026초

화학요법제 합성연구 II N,N'-disubstituted thiourea derivatives의 합성및 그 항균성과 항인결핵성 (Synthetic studies on chemothe-rapeutic agents (II) : synthesis and antibacterial and antitubercular activity of N,N'-disubstituted thiourea derivatives)

  • 조윤성;고광호
    • 약학회지
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    • 제15권3_4호
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    • pp.87-92
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    • 1971
  • Fourteen novel N,N'-disubstitued thiourea derivatives were synthesized by Hugershof reaction. Antitubercular activities of ten compounds against Mycobacterium tuberculosis H$_{37}$ Rv were tested and was found tat 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was considerably active at 1mg/ml and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea was slightly active at 1mg/ml. Antibacterial activity of the newly synthesized compounds against E. coli, Sta. aureus and Streptococcus hemolyticus were also tested. 1-cyclohexyl-3-(4-benzenesulfonepiperidide)-2-thiourea was makedly active against E. coli, Sta, aureus and Streptococcus hemolyticus; Phenol coefficients against E. coli, Sta, aureus and Streptococcus hemolyticus were 30,17.5 and 21.3, respectively. 1,1'-p-phenylene-3,3'bis[N-(2-thiazolyl)-sulfamylphenyl]-2,2'-dithiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were considerably active against E. coli: phenol coefficients, 18.8 and 37.5 respectively. 1-(4-ethoxyphenyl)3-(4-sulfamylphenyl)-2-thiourea was active against Streptococcus hemolyticus: phenol coefficients, 22.5. 1-$\alpha$-naphthyl-3-(4-sulfamylphenyl)-2-thiourea, 1-$\betha$-naphthyl-3-[4-N-(2-thiazolyl)-sulfamylphenyl]-2-thiourea and 1-$\alpha$-naphthyl-3-(4-benzenesulfonepiperidide)-2-thiourea were active against Sta. aureus: phenol coefficients, 17.5, 20.0 and 18.8 respectively.

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온도 변화에 따른 압전체 센서 자가진단법 및 접합제의 영향에 대한 실험적 고찰 (The Effect of Temperature Variations and Bonding Agents on Piezoelectric Sensor Diagnostics)

  • 조혜진;박통일;박규해
    • 한국소음진동공학회:학술대회논문집
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    • 한국소음진동공학회 2013년도 추계학술대회 논문집
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    • pp.799-804
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    • 2013
  • The sensor/actuator active sensor diagnostics procedure, where the sensors/actuators are confirmed to be functioning properly during operation, is a critical component to successfully complete the structural health monitoring (SHM) process with large numbers of active sensors typically installed in a structure. The basis of this process is to track the changes in the capacitive value of piezoelectric materials, which shows up in measured admittance. Due to the temperature dependent nature of piezoelectric materials, we investigated the effects of temperature variations on sensor diagnostic process. The effect of temperature variations found to be remarkable, modifying the measured capacitive values significantly. In addition we analyzed the effect of bonding agents between a PZT patch and a host structure. This paper summarizes considerations needed to develop such sensor diagnostic processes, experimental procedures and results, and additional issues that can be used as guidelines for future investigations.

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수종 골형성 증진재의 골형성능에 관한 조직형태계측학적 연구 (A STUDY OF THE EFFECTS OF SEVERAL BONE-ENHANCING AGENTS)

  • 신민철;류동목
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제29권5호
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    • pp.282-292
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    • 2003
  • Several agents are in use to promote new bone formation during bone graft procedures in maxillofacial region. Among them, we have used crude BMP, PRP, and P-15 for experimentally created defects with accompanying graft materials in the rabbit model. The aim of this study is to analyze the effect of above mentioned agents on bone formation using histologic and histomorphometrical methods, thus to provide experimental support for clinical application of these agents. Six rabbits were used as experimental animals. Four surgical defects were created on the distal femoral heads of each animal using trephine drill. The defects were filled with each agents with accompaning graft materials as experimental groups and particulate corti-co-cancellous autogenous graft as control. For histomorphometric analysis, fluorescent dye was injected at 2week and 1week before sacrifice. Then, the animals were sacrificed at 2, 4 and 8weeks after surgery and histologic and histomorphometric examinations were achieved. At two weeks after bone graft, bone formation and active remodeling process were examined in all experimental groups and the control. But the intensity of such activities of the experiments were somewhat weaker than that of the control. In BMP group, the amount of newly formed osteoid was increased constantly and the amount was preserved constantly in PRP group. But in P-15 group, the amount of newly formed osteoid was decreased with time to 8week after surgery. Histologic findings showed superior bony quantity and quality in PRP group than that of P-15 group. MAR(Mineralization Apposition Rate) of all experimental groups were slower than that of control group. In P-15 group, constant foreign body reaction was observed at all periods and the graft material showed inwardly destroyed characteristics rather to mature. The data from this study provide the basis for future studies for evaluating the long-term remodeling process and foreign body reactions observed in P-15 group and clinical study for predictable use of these agents.

IBM Aglets를 기반으로 하는 가상 병렬 컴퓨팅 시스템에서 작업 할당 기법과 성능 비교 (Work Allocation Methods and Performance Comparisons on the Virtual Parallel Computing System based on the IBM Aglets)

  • 김경하;김영학;오길호
    • 한국정보과학회논문지:컴퓨팅의 실제 및 레터
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    • 제8권4호
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    • pp.411-422
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    • 2002
  • 최근에 다중 에이전트를 기반으로 하는 가상 병렬 컴퓨팅 시스템에 관한 적극적인 연구가 이루어지고 있다. 가상 병렬 컴퓨팅 시스템은 많은 계산을 요구하는 복잡한 문제들을 해결하기 위해 고비용수퍼 컴퓨터를 사용하는 대신에, 인터넷상에 산재되어 있는 개인용 컴퓨터 혹은 워크스테이션을 사용한다. 가상 병렬 컴퓨팅 시스템은 인터넷상에 이용 가능한 자원에 의존하여 동질 혹은 이질형의 컴퓨터들로 구성될 수 있다. 본 논문에서는 IBM Aglets를 기반으로 하는 가상 병렬 컴퓨팅 환경에서 작업자 에이전트와 작업 패키지를 효율적으로 분산하는 새로운 방법을 제안한다. 기존의 방법들은 작업자 에이전트와 작업 패키지를 분산하기 위해서 주로 마스터/슬레이브 유형을 사용한다. 그러나 이러한 방법에서 에이전트의 수가 증가하게되면 중앙 마스터에서 작업부하가 급속하게 증가된다. 이러한 문제에 대한 해결로서 본 논문에서는 작업자 에이전트와 작업 패키지의 분산을 작업자 에이전트에게 위임하는 방법을 사용한다. 제안된 방법은 가상 병렬 컴퓨팅 시스템에서 다양한 방식으로 평가되었으며, 그 결과는 기존의 방법에 비해서 괄목할 만한 수준으로 개선되었다.

작물 보호제로서 살균제와 살충제의 활성 성분에 대한 물리-화학 파라미터의 범위 (The Range of Physicochemical Parameters for the Active Ingredients of Fungicides and Insecticides as Crop Protection Agents)

  • 송선섭;성낙도
    • Applied Biological Chemistry
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    • 제46권4호
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    • pp.280-284
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    • 2003
  • 농업용 살균제와 살충제로서의 활용성 진단과 예측평가 자료로 사용하기 위하여 상용화 된 살균제 133품목과 살충제 152품목의 활성 성분들에 대하여 소수성(LogP), 쌍극자능율(DM), HOMO 및 LUMO 에너지, molar refractivity(MR), polarizability(Pol), van der Waals 분자 표면적 및 부피(Vol), 분자량 및 수화 에너지(hydralion energy) 등, 10 가지의 다양한 물리-화학 파라미터들을 계산하였다. 그리고 살균제와 sterol 생합성 저해제 (DMI: demethylation inhibitor) 및 살충제와 acetylcholine esterase 저해제(AChE)이 가지는 특정한 물리-화학 파라미터들의 범위 값을 설정하였다. 그 결과에 기초하여 다양한 화합물들이 작물 보호제로서 살균제와 살충제로의 활용 가능성이 예측될 것으로 판단되었다.

점액세균 Sorangium cellulosum이 생산하는 약제내성 암세포의 증식억제물질 (Isolation of Antibiotics Effective to Multidrug-Resistant Cancer Cells from Sorangium cellulosum(Myxobacteria).)

  • 안종웅;이정옥
    • 한국미생물·생명공학회지
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    • 제32권1호
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    • pp.47-51
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    • 2004
  • 암세포가 특정 항암제에 의해 내성을 획득하면 구조가 상이한 타 항암제에도 교차내성을 나타내는 이른바 암세포의 다약제 내성이 암 화학요법에 있어서 가장 심각한 문제가 되고 있다. 본 연구에서는 다약제 내성 암세포주인 CL02 세포를 이용하여 cellulose 용해성 점액세균인 Sorangium cellulosum의 60여종의 균주를 대상으로 다약재 내성 암세포에 유효한 항암물질을 탐색하는 과정에서, 균주 JW1006의 대사산물에서 강한 증식억제 활성을 발견하고 그 활성 본체로서 macrolide계 화합물인 Disorazoles $A_1$$A_2$를 분리하였다 Disorazoles $A_1$$A_2$는 인체기원의 암세포에 대해 모두 강한 세포독성($IC_{50}$ <0.04 ng/$m\ell$)을 나타낼 뿐 아니라 다약제내성 세포주인 CL02와 cisplatin내성 세포주인 CP70에 대해서 감수성 세포주와 동일한 활성을 나타내어 다약제 내성을 극복하는 우수한 활성 물질임을 확인하였다

Use of Bioluminescent Indicator Acinetobacter Bacterium for Screening and Characterization of Active Antimicrobial Agents

  • Haleem Abd-El;A.M. Desouky;Zaki Sahar A.
    • Journal of Microbiology and Biotechnology
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    • 제16권11호
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    • pp.1706-1712
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    • 2006
  • Because of the need for new antimicrobial substances with novel mechanisms of action, we report here the use of an Acinetobacter reporter system for high-throughput screening of active antimicrobial agents. The bioreporter Acinetobacter strain DF4/PUTK2 carrying luciferase genes luxCDABE was chosen because of its ecological importance and it is widespread in nature. This bioreporter is genetically engineered to emit light constitutively that can be measured in real time by luminometry. Hence, this reporter system was employed to determine the bacteriostatic actions of spent-culture supernatants derived from twelve bacterial isolates. Out of the results, the strongest bioluminescence inhibitory effect of the supernatants was recorded with Bacillus cereus strain BAC (S5). Subsequently, ethyl acetate extracts of extracellular products of strain BAC (S5) were separated by a thin-layer chromatography (TLC). Based on the bioluminescence inhibitory assay, three fractions were found to have antimicrobial activity. One fraction (C) having the strongest antimicrobial activity was further purified using TLC and characterized by IR, $^1H$ NMR, mass spectrometry, SDS-PAGE, and amino acid composition analysis. The results predicted the presence of 2-pyrrolidone-S-carboxylic acid (PCA) and the octadeconic-acid-like fatty acid. Fraction C also demonstrated a broad inhibitory activity on several Gram-negative and Gram-positive bacteria. In conclusion, the Acinetobacter reporter system shows great potential to be a reliable, sensitive, and real-time indicator of the bacteriostatic actions of the antimicrobial agents.

LPS로 활성화된 U937세포에서 Prostaglandin $E_2\;(PGE_2)$ 생성 및 Cyclooxygenase-2 (COX-2) 활성 억제에 대한 한약제의 평가 (Evaluation of Korean Phytomedicinal Plants on inhibition of Prostaglandin $E_2\;(PGE_2)$ Production and Cyclooxygenase-2 (COX-2) in LPS-stimulated U937 Cells)

  • 장선일;전창수;곽경철;배문성;이정호;김기영;윤용갑;채규윤
    • 동의생리병리학회지
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    • 제20권2호
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    • pp.455-459
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    • 2006
  • The inhibitors of prostaglandin $E_2\;(PGE_2)$ production and cyclooxygenase-2 (COX-2) activity have been considered as potential anti-inflammatory agents. In this study, we evaluated 9 compounds isolated from 5 Korean phytomedicinal plants (Spirea prunifolia, Paeonia suffruticosa, Salvia miltiorrhiza, Scutellaria baicalensis, and Artemisia capillaris) for the inhibition of $PGE_2$production and COX-2 expession in lipopolysaccharide (LPS)-stimulated human macrophages U937 cells. As a result, several compound such as prunioside A, penta-O-galloyl-beta-D-glucose, tanshinone IIA, baicalin, baicalein, wogonin, scopolatin, scoparone and decursinol showed potent inhibition of $PGE_2$production (50-70% inhibition at the test concentration of $10\;{\mu}M$). In addition, these compounds were also considered as potential inhibitors of COX-2 activity (45-73% inhibition at the test concentration of $10\;{\mu}M$). These active compound mediating COX-2 inhibitory activities are warranted for further elucidation of active principles for development of anti-inflammatory agents and these properties may contribute to the anti-atopic dermatitis activity.

丹參의 methicillin 내성 황색포도구균에 대한 효과 (Antibacterial Activity of Salvia Miltiorrhiza against Methicillin-resistant Staphylococcus aureus)

  • 서명원;정승일;신철균;주영승;김홍준;고병섭
    • 한방안이비인후피부과학회지
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    • 제16권1호
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    • pp.94-99
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    • 2003
  • Objectives : Gram-positive bacteria have became increasing resistant to antibacterial agents, and hence multi-drug-resistant bacterial pathogens are now a major problem in clinical medicine. There is, therefore, a need for new antibacterial agents. In the course of our screening program for potent antibacterial agent from medicinal plants, the extract of Salvia miltiorrhiza (S. miltiorrhiza) showed antibacterial activity against methcillin resistant Staphylococcus aureus (MRSA) and antibiotic-resistant S. aureus. Methods : S. miltiorrhiza was extracted with 80$\%$ EtOH. The extract was suspended in H2O and fractionated successively with hexane chloroform, ethyl acetate, and n-buthanol. The chloroform fraction, which showed the highest antibacterial activity(MICs, 78㎍/ml) against MRSA, was chromatographed on a silica gel column and recycling prep-LC to give the pure antibacterial component. Results and Conclusions : The second fraction among the chloroform soluble portion of an aqueous EtOH extract of S. miltiorrhiza root showed outstanding antibacterial activity against MRSA and antibiotic-resistant S. aureus compared to the other fraction. An active compound was isolated from the second fraction using silica gel column chromatoraphy and recycling prep-LC. Based on these data together with the IH-, 13C-NMR, mass and mp, the active compounds were identified tanshinone Ⅰ, dehydrotanshinone Ⅰ and cryptotanshinone. Among tanshinones, cryptotanshinone and dihydrotanshinone Ⅰ MICs against MRSA and antibiotics-resistant S. aureus were 12.5, 12.5 and 6.3㎍/ml, respectively.

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