• Archives of Pharmacal Research
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• v.10 no.1
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• pp.50-59
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• 1987

(E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

• Molecules and Cells
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• v.20 no.1
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• pp.1-16
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• 2005

The peptidyl transferase center (PTC) is located in a protein free environment, thus confirming that the ribosome is a ribozyme. This arched void has dimensions suitable for accommodating the 3'ends of the A-and the P-site tRNAs, and is situated within a universal sizable symmetry-related region that connects all ribosomal functional centers involved in amino-acid polymerization. The linkage between the elaborate PTC architecture and the A-site tRNA position revealed that the A-to P-site passage of the tRNA 3'end is performed by a rotatory motion, which leads to stereochemistry suitable for peptide bond formation and for substrate mediated catalysis, thus suggesting that the PTC evolved by genefusion. Adjacent to the PTC is the entrance of the protein exit tunnel, shown to play active roles in sequence-specific gating of nascent chains and in responding to cellular signals. This tunnel also provides a site that may be exploited for local co-translational folding and seems to assist in nascent chain trafficking into the hydrophobic space formed by the first bacterial chaperone, the trigger factor. Many antibiotics target ribosomes. Although the ribosome is highly conserved, subtle sequence and/or conformational variations enable drug selectivity, thus facilitating clinical usage. Comparisons of high-resolution structures of complexes of antibiotics bound to ribosomes from eubacteria resembling pathogens, to an archaeon that shares properties with eukaryotes and to its mutant that allows antibiotics binding, demonstrated the unambiguous difference between mere binding and therapeutical effectiveness. The observed variability in antibiotics inhibitory modes, accompanied by the elucidation of the structural basis to antibiotics mechanism justifies expectations for structural based improved properties of existing compounds as well as for the development of novel drugs.

• Bulletin of the Korean Chemical Society
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• v.33 no.5
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• pp.1547-1550
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• 2012

Second-order rate constants ($k_N$) have been measured spectrophotometrically for the reactions of benzyl 2-pyridyl carbonate $\mathbf{3}$ and $t$-butyl 2-pyridyl carbonate $\mathbf{3}$ with a series of alicyclic secondary amines in MeCN at $25.0{\pm}0.1^{\circ}C$. Substrate $\mathbf{4}$ is much less reactive than $\mathbf{3}$ and the steric hindrance exerted by the bulky $t$-Bu group in $\mathbf{4}$ has been attributed to its decreased reactivity. The Br${\o}$nsted-type plots for the reactions of $\mathbf{3}$ and $\mathbf{4}$ are linear with ${\beta}_{nuc}=0.57$ and 0.45, respectively. Thus, the reactions have been concluded to proceed through a concerted mechanism, although the current reactions were expected to proceed through a stepwise mechanism with a zwitterionic tetrahedral intermediate $T^{\pm}$. It has been proposed that the rate of leaving-group expulsion is accelerated by the intramolecular H-bonding interaction in $T^{\pm}$ and the "push" provided by the RO group through the resonance interaction. Thus, the enhanced nucleofugality forces the reactions to proceed through a concerted mechanism. The reactivity-selectivity principle (RSP) is not applicable to the current reaction systems, since the reaction of the less reactive $\mathbf{4}$ results in a smaller ${\beta}_{nuc}$ than that of the more reactive $\mathbf{3}$. Steric hindrance exerted by the bulky $t$-Bu group in $\mathbf{4}$ has been suggested to be responsible for the failure of the RSP.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.335-335
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• 1994

Possibility whether lead ingestion can cause selective toxicity to central serotonergic nervous system in rats was tested. Three groups of wistar rats; 1)Control, 2) Low dose and 3) High dose groups, were prepared. In prenatally lead-exposed rats, until parturition from dams, rat pups were intoxicated via placenta of mother rats having received drinking water containing either 0%(control ), 0.05%(low dose) or 0.2%(high dose) of lead acetate respectively, In postnatally lead-exposed rats, right after parturition from dams rat pups received drinking water containing either 0％ (control), 0.05%(low dose) or 0.2％(high dose) of lead acetate. At 2, 4, 6 and 8 weeks of age, tryptophan hydroxylase (TPH) activity and Na$\^$+//K$\^$+/-ATPase activity were measured in 4 areas of rat brain; Telencephalon, Diencephalon, Midbrain and Pons/Medulla. TPH activities were assayed by modified method of Beevers et al. (1983) using L-(5-$^3$H)-tryptophan as substrate. TPH activity was determined as a criterion of lead poisoning to central serotonergic nervous system and Na$\^$+//K$\^$+/-ATPase activity as a criterion of non specific lead poisoning to any kinds of tissues. Selective toxicity of lead poisoning to central serotonergic nervous system was evaluated by the changes of TPH activities without concomitant changes of Na$\^$+//K$\^$+/-ATPase activities. In prenatally lead-exposed rats. this selectivity was found in Telencephalon (2 weeks of age), Diencephalon/Midbrain (2 weeks of age), Midbrain (4 and 6 weeks of age), Pons/Medulla (2, 4 and 6 weeks of age) In rats exposed to low dose of lead and Pons/Medulla (2 weeks of age) to high dose of lead. In postnatal Iy lead-exposed rats, this selectivity was found in Telencephalon (8 weeks of age), Diencephalon(8 weeks of age), Pons/Medulla (6 and 8 weeks of age) in rats exposed to low dose of lead and Pons/Medulla (8 weeks of age) to high dose of lead. These results suggest that lead poisoning may exhibit selective toxicity to central serotonergic nervous system.

• Proceedings of the KIEE Conference
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• 2008.07a
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• pp.1295-1296
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• 2008

Hydrogen peroxide ($H_2O_2$) biosensor is one of the most developing sensors because this kind of sensors is highly selective and responds quickly to the specific substrate. Hemoglobin (Hb) has been used as ideal biomolecules to construct hydrogen peroxide biosensors because of their high selectivity to $H_2O_2$. The direct electron transfer of Hb has widely investigated for application in the determination of $H_2O_2$ because of its simplicity, high selectivity and intrinsic sensitivity. An electrochemical detection for hydrogen peroxide was investigated based on immobilization of hemoglobin on DNA/Fe(pyterpy)$^{2+}$ modified gold electrode. The pyterpy monolayers were firstly an electron deposition onto the gold electrode surface of the quartz crystal microbalance (QCM). It is offered a template to attach negatively charged DNA. The fabrication process of the electrode was verified by quartz crystal analyzer (QCA). The experimental parameters such as pH, applied potential and amperometric response were evaluated and optimized. Under the optimized conditions, this sensor shows the linear response within the range between $3.0{\times}10^{-6}$ to $9.0{|times}10^{-4}$ M concentrations of $H_2O_2$. The detection limit was determined to be $9{\times}10^{-7}$ M (based on the S/N=3).

• Korean Journal of Materials Research
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• v.10 no.6
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• pp.450-455
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• 2000

For further scaling down of the silicon devices, the application of low dielectric constant materials instead of silicon oxide has been considered to reduce power consumption, crosstalk, and interconnection delay. In this paper, the effect of $O_2/SF_6$ plasma chemistry on the etching characteristics of polyimide-one of the promising low-k interlayer dielectrics-has been studied. The etch rate of polyimide decreases with the addition of $SF_6$ gas due to formation of nonvolatile fluorine compounds inhibiting reaction between oxygen and hydrocarbon polymer, while applying substrate bias enhances etching process through physical attack. However, addition of small amount of $SF_6$ is desirable for etching topography. $SiO_2$ hard mask for polyimide etching is effective under $O_2$plasma etching(selectivity~30), while $O_2/SF_6$ chemistry degrades etching selectivity down to 4. Based on the above results, $1-2\mu\textrm{m}$ L&S PI2610 patterns were successfully etched.

• Proceedings of the Korean Vacuum Society Conference
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• 2011.02a
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• pp.472-472
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• 2011

The capacitive coupled plasma (CCP) has been extensively used in the semiconductor industry because it has not only good uniformity, but also low electron temperature. But CCP source has some problems, such as difficulty in varying the ion bombardment energy separately, low plasma density, and high processing pressure, etc. In this reason, dual frequency CCP has been investigated with a separate substrate biasing to control the plasma parameters and to obtain high etch rate with high etch selectivity. Especially, in this study, we studied on the etching of $SiO_2$ by using the pulse-time modulation in the dual-frequency CCP source composed of 60 MHz/ 2 MHz rf power. By using the combination of high /low rf powers, the differences in the gas dissociation, plasma density, and etch characteristics were investigated. Also, as the size of the semiconductor device is decreased to nano-scale, the etching of contact hole which has nano-scale higher aspect ratio is required. For the nano-scale contact hole etching by using continuous plasma, several etch problems such as bowing, sidewall taper, twist, mask faceting, erosion, distortions etc. occurs. To resolve these problems, etching in low process pressure, more sidewall passivation by using fluorocarbon-based plasma with high carbon ratio, low temperature processing, charge effect breaking, power modulation are needed. Therefore, in this study, to resolve these problems, we used the pulse-time modulated dual-frequency CCP system. Pulse plasma is generated by periodical turning the RF power On and Off state. We measured the etch rate, etch selectivity and etch profile by using a step profilometer and SEM. Also the X-ray photoelectron spectroscopic analysis on the surfaces etched by different duty ratio conditions correlate with the results above.

• Archives of Pharmacal Research
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• v.11 no.1
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• pp.33-40
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• 1988

Two new nitro analogs of tranylcypromine, (E)-2-(p-nitrophenyl)cyclopropylamine ((E)-p-NTCP) and (E)-2-(m-nitrophenyl)cyclopropylamine ((E)-m-NTCP) were synthesized in order to examine the effect of aromatic nitro substitution on the MAO-inhibitory activity of 2-phenylcyclopropylamines. The compounds were obtained by treating t-butyl (E)-2-(p-nitrophenyl) cyclopropanecarbamate and t-butyl (E)-2-(m-nitrophenyl)cyclopropanecarbamate with p-toluenesulfonic acid in $CH_3$CN. Inhibitions of rat brain mitochondrial MAO-A and B by the compounds were examined using serotonin and benzylamine as the substrate at both in vitro and ex vivo levels. It was found from in vitro measurements that (E)-p-NTCP at $6.0{\times}10^{-5}M$ elicited merely 22.5% inhibition against MAO-B without any effect on MAO-A. In contrast, (E)-m-NTCP showed fair degrees of inhibitions of MAO-A and B with $IC_{50}$ values, $2.5{\times}10^{-7}M\;and\;1.4{\times}10^{-6}M$, respectively. It was also noted from (E)-m-NTCP that m-nitro substitution caused a shift of selectivity of the inhibition toward MAO-A. According to ex vivo measurements at 1.5, 3, 6, and 12 hr following the administration of a dose of 0.015 mmol/kg, i.p. to the rats, the inhibition percents of MAO-A by (E)-m-NTCP were 58.6, 63.7 63.6, and 46.6%, slightly lower than those observed by tranylcypromine. Whereas, (E)-m-NTCP at the same dose level did not show significant inhibitions against both MAO-A and MAO-B. Possible reasons for the difference in potencies between (E)-m-NTCP and (E)-p-NTCP were sought in relation to differing electron withdrawing effects of m- and p-substituents which will influence electron density of the side chain amino functions and the partitions.

• KSBB Journal
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• v.19 no.2
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• pp.164-167
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• 2004

Cyclodextrin glucanotransferase (EC 2.4.1.19, abbreviated as CGTase) is one of the most applied industrial enzymes that produces cyclodextrins from starch and related ${\alpha}$-1,4-glucans by intramolecular transglycosylation reaction upon Ca$\^$2＋/ dependent manner. The reaction of CLEC, ${\alpha}$-CGTases from Bacillus macerans with the soluble starch as a substrate reveals that the surfactants (SDS, N-octyl-${\beta}$-D-glucoside) significantly affect not only the overall products of CDs but also their selectivity. The surfactants (SDS, Lubrol PX) trigger the increase of ${\alpha}$-CD production, but Triton x-100 and Tween 80 suppress ${\alpha}$-CD specificity. Organic solvents (dimethyl sulfoxide, formamide, 2-methyl-2,4-pentandiol, and ethylene glycol) also cause changes of total product and product selectivity.

• Bulletin of the Korean Chemical Society
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• v.25 no.9
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• pp.1371-1378
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• 2004

A porous stainless steel (SUS) as a substrate of silica composite membranes for hydrogen purification was used to improve mechanical strength of the membranes for industrial application. The SUS support was successfully modified by using submicron Ni powder, $SiO_2$ sols with particle size of 500 nm and 150 nm in turns. Silica top layer was coated on the modified supports under various preparation conditions such as calcination temperature, dipping time and repeating number of dipping-drying process. The calcination temperature for proper sintering was between H ttig temperature and Tamman temperature of the coating materials. Maximum hydrogen selectivity was investigated by changing dipping time. As repeating number of dipping-drying process increased, permeances of nitrogen and hydrogen were decreased and $H_2/N_2$ selectivity was increased due to the reduction of non-selective pinholes and mesopores. For the silica membrane prepared under optimized conditions, permeance of hydrogen was about $3\;{\times}\;10^{-5}\;cm^3{\cdot}cm^{-2}{\cdot}s^{-1}{\cdot}cmHg^{-1}$ combined with $H_2/N_2$ seletivity of about 20.