• Archives of Pharmacal Research
• /
• 제19권4호
• /
• pp.312-316
• /
• 1996

A series of N-Cbz${alpha}$-aminosucinimides (1), combining common moieties of various anticonvulsants such as N-CO-C-N and cyclic imide in a single molecule, were synthesized from the corresponding (R)- and (S)-N-Cbz-aspartic acid (2). And their in vivo anticonvulsant evaluations in MES and PTZ test were investigated. And also the rotorod test for neurotoxicity was investigated. All the tested compounds (1), except 1c and 1f, showed significant anticonvulsant activities in both MES and PTZ test. And the most active compound among them in MES test was (R)-N-Cbz-${alpha}$-amino-N-methylsuccinimide (1b) $(ED_50/=52.5 mg/kg)$ and (S)-N-Cbz-aminosuccinimide((1d) was most active in PTZ test $(ED_50/=78.1 mg/kg)$. And the $TD_50$ values of the tested compounds were above 117.5 mg/kg. These pharmacological data were comparable to those of currently available anticonvulsants. And also we found that the pharmacological effects were dependent on their N-substituted alkyl chains and their stereochemistry.

• Journal of Microbiology and Biotechnology
• /
• 제27권6호
• /
• pp.1065-1070
• /
• 2017

This study aimed to examine the anti-candidal efficacy of a novel ketone derivative isolated from Diaporthe sp. ED2, an endophytic fungus residing in medicinal herb Orthosiphon stamieus Benth. The ethyl acetate extract of the fungal culture was separated by open column and reverse phase high-performance liquid chromatography (HPLC). The eluent at retention time 5.64 min in the HPLC system was the only compound that exhibited anti-candidal activity on Kirby-Bauer assay. The structure of the compound was also elucidated by nuclear magnetic resonance and spectroscopy techniques. The purified anti-candidal compound was obtained as a colorless solid and characterized as 3-hydroxy-5-methoxyhex-5-ene-2,4-dione. On broth microdilution assay, the compound also exhibited fungicidal activity on a clinical strain of Candida albicans at a minimal inhibitory concentration of $3.1{\mu}g/ml$. The killing kinetic analysis also revealed that the compound was fungicidal against C. albicans in a concentration- and time-dependent manner. The compound was heat-stable up to $70^{\circ}C$, but its anti-candidal activity was affected at pH 2.

• Archives of Pharmacal Research
• /
• 제20권2호
• /
• pp.155-157
• /
• 1997

An attempt to estabilish the relationship between anti-cell adhesive action of phenylacetylshikonin analogues and their cytotoxicity against A549 cells was done. In the one hour incubation with A549 cells,${\alpha}$-methoxyphenylacetyl-(9), ${\alpha}$-acetoxyphenylacetyl-(13), 3,4-methylenedioxyphenylacetyl-(15) and 4-(N,N-dimethylamino)-phenylacetylshikonin (17) analogues showed a high anti-cell adhesive activity $(IC_100; value, 4-8{\mu}g/ml)$, while halophenylacetyl- and dimethoxy- or trimethoxyphenylacetyl analogues expressed no activity at $40{\mu}g/ml$, indicating that the presence of a bulky group at $ C^I-{\alpha}$ and a polar group at C-4 of phenylacetyl moiety may be important. A similar structure activity relationship exists for the 48 hr cytotoxocity $(ED_{50})$ of phenylacetylshikonin analogues in A 549 cells, but not in either K562 or L1210 cells. Furthermore, the difference between $IC_{100}$ values for anti-cell adhesive activity and$ED_{50}$ values for cytotoxicity of potent compound in A549 cells was not so great (1.5 to 3 times). Based on these observations, it is proposed that the anti-cell adhesive action of phenylacetylshikonins might be responsible for their cytotoxicity in A549 cells.

• Archives of Pharmacal Research
• /
• 제21권2호
• /
• pp.198-206
• /
• 1998

Fourty eight derivatives of 2-(1-oxyalkyl)-1,4-dioxy-9,10-anthraquinone were synthesized, and their antitumor activity was evaluated. On the whole, 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinones (DHAQ=1,4-dihydroxy-9,10-anthraquinone) showed stronger cytotoxic activity against L1210 cells than 2-(l-hydroxyalkyl)-1,4-dimethoxy-9,10-anthraquinones(DMAQ =1,4-dimethoxy-9,10-anthraquinone), implying that free hydroxy groups at C-1 and C-4 of the anthraquinone structure are necessary for the cytotoxic activity. The bioactivity of 2-(lhydroxyalkyl)-DHAQ derivatives differed according to the size of alkyl group at C-1;while the elongation of alkyl group over 7 carbon atoms failed to enhance the bioactivity, the derivatives possessing alkyl moiety of 1-6 carbon atoms showed an increase in the cytotoxicity and the antitumor activity in Sarcoma-180; 2-hydroxymethyl-DHAQ ($ED_{50}$, $15\mu\textrm{g}$/ml; T/C, 125%), 2-(1 -hydroxyethyl)-DHAQ($1.9{\mu}g/ml;139.2%)$;, 2-(1-hydroxypropyl)-DHAQ ($7.2{\mu}g$/ml; 135.1%), 2-(1-hydroxybutyl)-DHAQ ($10.2{\mu}g/ml; 125.3%)$, 2-(1-hydroxypentyl)-DHAQ ($23.7{\mu}g/ml; 110.1%$). and 2-(1-hydroxyhexyl)-DHAQ ($58{\mu}g/ml;108%$). Next, 2-(1-Hydroxyalkyl)-DHAQ derivatives were acetylated to produce 2-(1-acetoxyalkyl)-DHAQ analogues. Although the acetylation somewhat enhanced the cytotoxicity, but not the antitumor action. In addition, the presence of phenyl group at $C-1^{l}$ enhanced the cytotoxicity and the T/C value, compared to alkyl groups of same size; 2-(1-hydroxy-1-phenyl)-DHAQ ($ED_{50}$, $5.6{\mu}g$, T/C, 137%).

• 대한전기학회:학술대회논문집
• /
• 대한전기학회 2006년도 춘계학술대회 논문집 전기기기 및 에너지변환시스템부문
• /
• pp.158-160
• /
• 2006

The structure of interior permanent magnet type brushless DC motor (IPM type BLDC motor) has high saliency ratios that produce additional reluctance torque. But this structure has a significant cogging torque that may cause acoustic noise and vibration. In this paper describes an optimization of flux barrier in order to reduce cogging torque and torque ripple in IPM type BLDC motor using the Taguchi methods. The optimal design consider- ed noises such as manufacturing tolerances of permanent magnet size. So, optimal design ensures that torque performance is insensitive to noise.

• 한국자동차공학회논문집
• /
• 제13권2호
• /
• pp.16-21
• /
• 2005

The performance of reciprocating internal combustion engine is a strong function of the air intake system configuration. In order to improve engine power, it is essential to optimize the air induction system. In this study, a numerical investigation has been carried out for the three-dimensional flow and pressure characteristics in air intake system of a large-sized commercial bus. CFD simulations using STAR-CD were also perform ed to evaluate effects of intake duct geometry and structure variation inside air cleaner on the negative pressure distribution of overall intake system. Studies for improving the back pressure distribution have been proposed and quantitatively examined based on intensive case studies.

• Bulletin of the Korean Chemical Society
• /
• 제29권2호
• /
• pp.319-322
• /
• 2008

The viability of acetylene addition in each step of aromatic formation initiated by vinyl radical and acetylene also with its competition with structure rearrangement is investigated by determining optimal geometries and barrier and reaction energies using quantum mechanical methods. In principle, the addition reaction has more difficult in term of free energy and enthalpy compared to geometry arrangement. Under combustion conditions, i.e. T = 1200 K, acetylene addition is unfavorable mechanism as the barrier energy values rise much higher than that of geometry arrangement. However, in longer chain hydrocarbon case, e.g. n-CxHx+1 where x ³ 8, C-C bond rotation is rather difficult and requires high energy to form a ring structure, elongation chain is preferable.

• 대한기계학회논문집
• /
• 제16권3호
• /
• pp.506-513
• /
• 1992

본 연구에서는 복합재 구조물에 대하여 유한요소해석법에 현상학적 모델인 전 단지연해석을 도입하여 강성저하와 모재파손을 예측하고 변형률을 매개변수로 한 Wei- bull 함수를 섬유파손해석에 도입하여 초기파손후의 거동을 묘사하고자 한다. 그리 고 면내전단하중이 작용하는 경우에 대해 전단지연해석을 수행할 수 있도록 모델링을 확장했다. 모재균열의 존재로 인한 단층의 강성변화는 실험으로 측정이 불가능하므 로 유한요소해석을 수행하여 비교하였다. 이 모델로부터 전단강성의 저하를 평가하 는 방법을 사용하였으며, 모재파손의 밀도 예측도 평균변형률 개념으로 전단효과를 고 려할 수 있도록 수정하였다. 그리고 초기파손후의 거동을 점진적으로 해석하기 위해 비선형 유한요소프그램을 작성하고, 상기의 모델을 도입하여 초기파손후의 거동을 보 다 정확히 묘사할 수 있는 방법을 제시하고 예로서 평시편에 대해 해석하고 실험치 및 타방법의 결과와 비교하였다.

• Coupled systems mechanics
• /
• 제8권2호
• /
• pp.111-127
• /
• 2019

In this paper, we present a 2D multi-scale coupling computation procedure for localized failure. When modeling the behavior of a structure by a multi-scale method, the macro-scale is used to describe the homogenized response of the structure, and the micro-scale to describe the details of the behavior on the smaller scale of the material where some inelastic mechanisms, like damage or plasticity, can be defined. The micro-scale mesh is defined for each multi-scale element in a way to fit entirely inside it. The two scales are coupled by imposing the constraint on the displacement field over their interface. An embedded discontinuity is implemented in the macro-scale element to capture the softening behavior happening on the micro-scale. The computation is performed using the operator split solution procedure on both scales.

• Applied Microscopy
• /
• 제21권2호
• /
• pp.67-75
• /
• 1991

[ $C_{60}$ ] molecule, the Buckminsterfullerene, has generated great interest because of its unique molecular structure and of superconductivity exhibited in its alkali-doped solids. We have investigated the molecular stacking and crystal structure of $C_{60}$ thin crystals formed on amorphous carbon film. The $C_{60}$ powder which was chromatographically purified was dissolved in benzene. The thin crystals of $C_{60}$ were observed with a 300 keV transmission electron microscope. Electron diffraction analysis and direct imaging of its molecular stacking were carried out. It was found from this work that the molecules of $10.0{\AA}$ diameter are arrayed hexagonally on substrate surface and $8.7{\AA}$ lattice planes are quite often found in several types of ED patterns, which can never be explained with a fcc model. Therefore the structure of $C_{60}$ thin crystals is hcp, although we cannot fully exclude the possibility of co-existence of hcp and fcc.