• Archives of Pharmacal Research
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• v.19 no.3
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• pp.248-250
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• 1996

In conclusion, a series of N-Cbz-.alpha.-amono-glutarimides (1a-f), combining common structures such as N-CO-C-N and cyclic imide in a single molecule, were prepared from the (R)- or (S)-N-Cbz-glutamic acid and evaluated for their anticonvulsant activities in MES and PTZ tests in order to develope new and broad spectrum anticonvulsant. In this study, N-Cbz-.alpha.-aminoglutarimides (1) except ac and af, showed significant anticonvulsant activity in both MES and PTZ tests enough to be recommended as promising new anticonvulsant drug candidates. Now we are continuing to investigate further anticonvulsant test (quantification)for these compounds and synthesize their analogues in order to develop more active anticonvulsant and define the structure activity relationship more precisely.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.759-763
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• 1998

In connection with the development of new anticonvulsant agents with a broad spectrum, we found that N-Cbz-alpha-amino-alkylsuccinimides showed significant anticonvulsant activities, and the pharmacological activities of these compounds were dependent on their stereochemistry and N-substituted alkyl group. These results prompted us to define the effects of other functional group on the anticonvulsant activities of these compounds. Therefore a series of N-alkoxycarbonyl-alpha-amino-N-methylsuccinimide were prepared from N-Cbz-aspartic acid and were evaluated with their anticonvulsant activities againt the MES and PTZ tests, in order to define the effect of N-substituted alkoxy carbonyl group with the anticonvulsant activities. From these studies, it was found that all the tested N-alkoxycarbonyl-alpha-amino-N-methylsuccinimides exhibited significant anticonvulsant activities in the PTZ test and were not active in the MES test. The most active compound in the PTZ test was (S) N-ethoxycarbonyl-alpha-amino-N-methyl-succinimide. We found that the pharmacological activities in the PTZ test were dependent on their N-alkoxycarbonyl groups. They follow as such: The order of anticonvulsant activities for (R) series as evaluated by $ED_{50}$ was N-phenoxycarbonyl=N-4-nitrobenzyloxycarbonyl > N-ethoxycarbonyl > N-allyloxycarbonyl > N-tert. butoxycarbonyl compound: For the (S) series N-ethoxycarbonyl > N-phenoxycarbonyl > N-allyloxycarbonyl compound. From the above results, it was conceivable that N-substituted alkoxycarbonyl group had certain effects on the anticonvulsant activities of N-alkoxycarbonyl-${\alpha}$-amino-N-methylsuccinimides.

• Journal of Environmental Health Sciences
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• v.23 no.4
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• pp.115-120
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• 1997

The purpose of thesis was to investigate the removal efficiency of surfactants and commercial detergents by Oenanthe javanica that is one of aquatic plants in Korea. The experiment is concerned with measuring the concentrations of surfactants and commercial detergents in different media: 1) in pure water, 2) in water containing Oenanthe javanica, 3) in water containing Oenanthe javanica and commercial nutrients. The surfactants used in this research include linear alkylbenzene sulfonates (LAS), $\alpha$-sulfo fatty acid methyl esters(MES), and alkylbenzene sulfonates(ABS). Two commercial detergents designated as A and B were in the forms of power and liquid. The results showed that LAS and MES were more effectively removed by Oenanthe javanica probably because these have a chain of linear carbon than on ABS with a branched carbon structure. In the case of commercial detergents, when the except was performed on the basis of surfactants proportion, the removal trends were similar to LAS and MES. The 5-day cultivating test with initial concentration of 0.5-1.0 ppm surfactants showed that less than 10% was removed if no nutrients an Oenanthe javanica were added. When Oenanthe javanica was added into the sample solution containing surfactants, the removal efficiency was increased 100% for the solution containing 0.5-1.0 ppm 60-70% for 5-10 ppm. In addition, chlorisis on Oenanthe javanica was observed due to surfactants and commercial detergents for all three cases. To test the dependence of population density on nutrients, the initial population density was made 300 g/0.4 m$^2$. Throughout the 5-day experiment, the on Oenanthe javanica grew 20-25% with 0.5-1.0 ppm without the synthetic nutrients but by 5% with a high concentrations of 5-10 ppm. The population density was appeared to be independent of synthetic nutrients. The leaves were to be grown with synthetic nutrients, while roots were grown without synthetic nutrients. Based on this research, the fundamental data concerning cultivation and an adequate adjustment of the water condition can provide for the utilization of Oenanthe javanica in real water treatment system.

• Bulletin of the Korean Chemical Society
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• v.26 no.11
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• pp.1757-1760
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• 2005

A series of 6-alkyloxyl-3,4-dihydro-2(1H)-quinoliones (5a-5n) were synthesized through nitration, reduction, diazotization, hydrolysis and alkylation from 3,4-dihydro-2(1H)-quinolione. Their structures were characterized by IR, $^1H$-NMR and MS. The anticonvulsant activity was evaluated by the Maximal electroshock test (MES) and the subcutaneous pentylenetetrazole (Metrazole) test (sc-Met). The neurotoxicity was measured by the Rotarod test (Tox). The result showed that 6-hexyloxy-3,4-dihydro-2 (1H)-quinolinone (5c) was potent in anti-MES and anti-scMet test with $ED_{50}$ of 24.0 mg/kg and 21.2 mg/kg, respectively, albeit its $TD_{50}$ (67.6 mg/kg) revealed the high neurotoxicity. 6-Benzyloxy-3,4-dihydro-2(1H)-quinolinone (5f) was less effective against MES induced seizure with $ED_{50}$ of 29.6 mg/kg, but no neurotoxicity was observed even under 300 mg/kg. Its Protective index (PI) was greater than 10 preferable to Phenytoin, Carbamazepin, Phenobarbital and Valproate.

• Proceedings of the Korean Society of Precision Engineering Conference
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• 2002.10a
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• pp.1070-1073
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• 2002

The biomechanical interaction between the stump and the prosthetic socket is critically important to achieve close-to-normal ambulation. Many investigators suggested that the pressure changes during gait of transfemoral amputees are closely related to the prosthetic alignment, the socket shape, the stump size, and the residual muscle activity. The effects of the prosthetic alignment, the socket shape, and the stump size on the interface pressure were investigated previously. However, there is no report how the residual muscle activities in the transfemoral stump affect the socket interface pressure characteristics during gait. Since designs of socket fur lower limb amputees need to consider the socket interface pressure characteristics, the interface pressure patterns by the residual muscle activities during gait should be investigated. In this study, myoelectric signals (MES) and socket interface pressure in residual limb of transfemoral amputees were measured during the stance and swing phases of gait. For the purpose, specially designed quadrilateral sockets that MES electrodes could be instrumented were fabricated. A total of two transfemoral amputees were participated in the experiments. The measured temporal MES amplitude and interface pressure in knee flexor (biceps femoris) and extensor (rectus femoris) had significant correlations (P ＜ 0.05). Based on the test results, It was suggested that the residual muscle activity of transfemoral amputees stump is an important factor affecting socket pressure changes during walk.

• Membrane and Water Treatment
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• v.12 no.2
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• pp.75-82
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• 2021

This study aimed to prepare a W/O nonionic microemulsion system(MEs) consisting of OP-4[polyoxyethylene(4) nonylphenol], OP-7[polyoxyethylene(7) nonylphenol], 1-hexanol, D2EHPA, kerosene and HCl solution and applied to the extraction of La(III) from chloride aqueous solution within the polysulfone hollow fiber contactor (HFC),laboratory-scale experiments were carried out to investigate the recovery of La(III) using as-prepared microemulsion from the simulation wastewater containing La(III),Al(III) and Fe(III). The right weight ratio(Rs) of OP-4 to OP-7 was firstly confirmed through determination of the solubilization capacity of HCl solution(W0,HCl) in microemulsion, the effect of several factors such as the HCl concentration, temperature and effective extraction time on the extraction efficiency of La(III) was discussed. Results showed that the acceptable Rs was 4:6 to prepare the W/O MEs. The extraction yield of La(III) increased with the increasing of HCl concentration, temperature and effective extraction time and reaches to 97.3% while using five-stage modules. The recovery yield of La(III) from simulation La-bearing wastewater was 90.6%.

• Bulletin of the Korean Chemical Society
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• v.31 no.2
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• pp.447-452
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• 2010

A series of 5-alkoxy-tetrazolo[1,5-a]quinolines were synthesized to evaluate their anticonvulsant and antidepressant effects. Anticonvulsant effects and neurotoxicity of the compounds when injected intraperitoneally to mice were determined by a maximal electroshock (MES) test and a rotarod test, respectively. Only three of the synthesized compounds (4a, 4b, 4c) displayed anticonvulsant activity at a dose of 300 mg/kg. Most of the compounds significantly reduced immobility times during the forced swimming test (FST) at a dose of 100 mg/kg, indicative of antidepressant activity. Among the compounds, 5-(2-fluorobenzyloxy)tetrazolo[1,5-a]quinoline (4k) reduced immobility time by 66.85% at 30 mg/kg compared with the same dose of Fluoxetine, which reduced immobility time by 52.30%. According to the results of the 5-Hydroxytryptophan induced head-twitch test and yohimbine toxicity potentiation test, the noradrenergic system seems not to be involved in the antidepressant-like effect of compound 4k while the serotonergic system seems a little to be involved.

• Journal of Life Science
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• v.14 no.1
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• pp.91-97
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• 2004

As a part of our study on the improvement of anticonvulsant, here we report the synthesis of N-acyl-$\alpha$-aminosuc-cinimides 1 and N-acyl-$\alpha$-aminoglutarimides 2. (R)-Benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-ylester 6a, (R)-4-nifro-benzoic acid 4-benzyloxycarbonylamino-2- oxo-pyrrolidin-1-yl ester 6b, (R) -4-nitro-benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6c, and (R)-propionic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6d were synthesized from (R)-2-benzyloxy carbonylamino-succinic acid 3 as a starting meterial. (R)-(3- Benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)-acetic acid methyl ester 10a, (R)-(3-benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)-acetic acid ethy1 ester 10b, an d (R)-2-(3-benzyloxycarbonylamino-2,6- diox o-piperidin-1-yl oxy)-propionic acid methyl ester l0c were synthesized from (R)- 3-carbobenzyloxy-amino-glutarmic acid 7 as a starting meterial. The yield, mp, IR, $^1H-NMR,\; and^{13}C$- NMR spectra of the products 6a, 6b, 6c, 6d, 10a, l0b, l0c are summarized in footnote. The biological studies of these compounds are in progress and will be reported in future.

• Computers and Concrete
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• v.23 no.1
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• pp.25-36
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• 2019

In this paper, an algorithm is presented to simulate numerically the reinforced concrete (RC) columns having any geometric form of section, loaded eccentrically along one or two axes. To apply the algorithm, the columns are discretized into two macro-elements (MEs) globally and the critical sections of columns are discretized into fixed rectangular finite elements locally. A proposed triple simultaneous dichotomy convergence method is applied to find the equilibrium state in the critical section of the column considering the three strains at three corners of the critical section as the main characteristic variables. Based on the proposed algorithm a computer program has been developed for simulation of the nonlinear behavior of the eccentrically-loaded columns. A good agreement has been witnessed between the results obtained applying the proposed algorithm and the experimental test results. The simulated results indicate that the ultimate strength and stiffness of the RC columns increase with the increase in axial force value, but large axial loads reduce the ductility of the column, make it brittle, impose great loss of material, and cause early failure.

• Tuberculosis and Respiratory Diseases
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• v.52 no.5
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• pp.463-474
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• 2002

Background : This study was designed to examine how glutathione, one of the nucleophilic sulfur compounds, effects the cisplatin cellular toxicity in the non-small cell lung cancer cell lines and normal lung epithelial cell line. Materials and Methods : Three cultured cell lines, the lung adenocarcinoma cell(NCL-H23), the lung squamous carcinoma cell(SK-MES-1) and the normal lung epithelial cell(L-132) line were exposed to various concentrations of cisplatin with or without glutathione. The relative viability was estimated as a means of measuring the cisplatin cellular toxicity using the MTT method. Results : In NCI-23, the response to cisplatin was sensitive but glutathione markedly increased the relative survival of the tumor cells by removing the antitumor effect of cisplatin. In both SK-MES-1 and L-132, the responses to cisplatin were less sensitive, and the chemoprotective effect of glutathione compared to and equal cisplatin dose was significantly higher in L-132 than in SK-MES-1(p<0.05). Conclusion : The protective effectes of of glutathione on cisplatin-induced cellular toxicity is more significant in normal lung epithelial cells than in squamous carcinoma cells.