• Journal of the Korean Chemical Society
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• v.41 no.6
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• pp.277-283
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• 1997

Platinum(II) complexes(where, $[Pt(L)_2X_2]$; L=isoxazole(isox), 3,5-dimethylisoxazole(3,5-diMeisox), 3-methyl,5-phenylisoxazole(3-Me,5-Phisox), and 4-amino-3,5-dimethylisoxazole(4-ADI); X=Cl, Br) with planar ligands are investigated on antitumor activity by MM2 and EHMO calculations. It was found that, the net atomic charges of the halogen atoms in all of cis-, trans-isomers are greater than that of the nitrogen with planar form, indicating that ionic character of Pt-X bond is greater than that of Pt-N. Also, the ${\sigma}MO$ energy level($E{\sigma}_{(Pt-X)}$) of the interaction between $d_{x2-y2}$ orbital of Pt atom and $p_x$ orbital of X found to be higher than that of between $d_{x2-y2}$ orbital of Pt atom and $p_x$ orbital of N about all the complexes. It is found that bond strength of between Pt and X atom is weaker than that of between Pt and N atom. The ${\sigma}MO$ energy level($E{\sigma}_{(Pt-X)}$) of trans- complexes found to be higher than that of cis- complexes, as a result of bond strength of Pt-X in cis- and trans-complexes, for all the complexes. The degree of dissociation of X atom in Pt-X bond for trans-complexes are related to antitumor activity and the logIA value of inhibitory activity coefficient(IA).

• Journal of Life Science
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• v.15 no.3 s.70
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• pp.505-512
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• 2005

Excitotoxicity and epileptogenesis have often been associated with glutamate receptor activation. Accumulating evidences indicates that topiramate (TPM), an antiepileptic drug with multiple mechanisms of action has neuroprotective activity. We explored the neuroprotective effect of TPM on the status epilepticus (SE)-induced hippocampal neuronal death. After development of SE by kainite injection (15 mg/Kg), rats were treated with TPM (10mg/kg) for 1 week. The neuronal death was detected by Apop tag in situ detection kit, and the expression levels of glutamate receptors were semi-quantitatively analyzed by immunoblot. Kainate-induced SE caused a significant neuronal death and cell loss in CAI and CA3 regions of hippocampus at 1 week. However, treatment of TPM for 1 week after SE markedly reduced hippocampal neuronal death. The expression of N-methyl-D-aspartate (NMDA) receptor subunit 1, was increased by SE, but was not affected by 1 week treatment of TPM. The expressions of NMDA receptor subunit 2a and 2b were not changed by either SE or TPM. As for ${\alpha}-amino-3-hydroxy-5-methyl-4-isoxazole-propionate$ (AMPA) glutamate receptors (GluR), kainate-induced SE markedly up-regulated GluR1 expression but down-regulated GluR2 expression, leading to increased formation of $Ca^{2+}$ permeable GluR2- lacking AMPA receptors. TPM administration for 1 week attenuated SE-induced expression of both the up-regulation of GluR1 and down-regulation of GluR2, reversing the ratio of GluR1/GluR2 to the control value. In conclusion, TPM protects neuronal cell death against glutamate induced excitotoxicity in kainate-induced SE model, supporting the potential of TPM as a neuroprotective agent.

• Journal of Pharmaceutical Investigation
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• v.10 no.4
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• pp.8-22
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• 1980

In order obtain some new antibacterial agents, seven new 2-ethoxymethyl-3-(5-nitro-2-furyl) acrylamide derivatives were synthesized by condensing 2-ethoxymethyl-3-(5-nitro-2-furyl) acyloyl chloride with amino compounds namely 5-amino-3, 4-dimethyl isoxazole, sulfamonomethoxazole, d-2-amino-1-butanol, hydroxylamine hydrochloride, semicarbazide hydrochloride, thiosemicarbazide, and p, p'-diaminodiphenylsulfone, respectively. The seven synthesized compounds were 2-ethoxymethyl-3-(5-nitro-2-furyl) acryl-5-amino-3, 4-dimethylisoxazoleamide [VII], $N^4-[2-ethoxymethyl\;3-methyl\;(5-nitro-2-furyl)\;acryl]-N^1-(5-methyl-3-isoxazolyl)$ sulfanilamide [VIII], 2-ethoxyl-3-(5-nitro-2-furyl) acrylsemicarbazide [X], 2-ethoxymethyl-3-(5-nitro-2-furyl) acrylthiosemicarbazide [XI], 2-ethoxymethyl-3-(5-nitro-2-furyl) acryl-d-2-amino-1-butanolamide [XII], and 4, 4'-di[2-ethoxymethyl-3-(5-nitro-2-furyl) acryl-amido] diphenylsulfone [XIII]. These compounds, with exception of the compound XIII, showed generally effective antibacterial activity, especially in the following instances. Compound VII was shown to be effective against Bacillus subtilis ATCC 6633 compound VIII, against Bacillus cereus var. Mycoides ATCC 1778, and compound XII, against both Proteus vuglaris and Saccharomyces cerevisiae ATCC 9763.

• Korean Journal of Weed Science
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• v.30 no.4
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• pp.323-329
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• 2010

Methiozolin (5-(2,6-difluoro-benzyloxymethyl)-5-methyl-3-(3-methyl- thiophen-2-yl)- 4,5-dihydro-isoxazole) is a new turf herbicide in isoxazoline chemistry. The herbicide controls grass weeds and has a high safety to various cool and warm season turfgrasses. This paper describes basic chemical, biological, and regulatory information of methiozolin.

• Molecules and Cells
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• v.21 no.1
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• pp.34-41
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• 2006

The neuronal localization of alpha-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) glutamate receptor (GluR) subunits is vital as they play key roles in the regulation of calcium permeability. We have examined the distribution of the calcium permeable AMPA glutamate receptor subunit GluR1 in the mouse visual cortex immunocytochemically. We compared this distribution to that of the calcium-binding proteins calbindin D28K, calretinin, and parvalbumin, and of GABA. The highest density of GluR1-immunoreactive (IR) neurons was found in layers II/III. Enucleation appeared to have no effect on the distribution of GluR1-IR neurons. The labeled neurons varied in morphology; the majority were round or oval and no pyramidal cells were labeled by the antibody. Two-color immunofluorescence revealed that 26.27%, 10.65%, and 40.31% of the GluR1-IR cells also contained, respectively, calbindin D28K, calretinin, and parvalbumin. 20.74% of the GluR1-IR neurons also expressed GABA. These results indicate that many neurons that express calcium-permeable GluR1 also express calcium binding proteins. They also demonstrate that one fifth of the GluR1-IR neurons in the mouse visual cortex are GABAergic interneurons.

• Archives of Pharmacal Research
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• v.5 no.2
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• pp.79-86
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• 1982

Sulfisoxazole, $C-{11}H_{13}N_{3}S$, crystallized in the orthohombic system, space group Pbca, with a = 14.492(1), b = 11.563(1), c = 14.900(2) $\AA$ and Z = 8. Intensities for 1867(1360 observed) unique reflections were measured on a four-circle diffractometer wirh CuKa radiation ($\lambda$ = 1.5418$\AA$). The structure was solved by heavy atom methods and refined by full-matrix least-squares procedures to a final R of 0.094. The benzene ring plane makes an angle of $68^{\circ}C$ with the plane of the isoxazole ring, which is plannar. The conformational angle formed by the torsional angle C(4)-S-N(2)-C(7) is $54^{\circ}C$. There are two intermolecular hydrogen bonds in the structure. One of them is of the type N-H...H with the length 2.915$\AA$. Thus two dimensional networks of hydrogen bonds form infinite moelcular sheets parallel to the (001) plane. Adjacent sheets are bound together by van der Waals forces.

• The Korean Journal of Physiology and Pharmacology
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• v.25 no.1
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• pp.79-85
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• 2021

α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors are differentially regulated in the nucleus accumbens (NAcc) of the brain after cocaine exposure. However, these results are supported only by biochemical and electrophysiological methods, but have not been validated with immunohistochemistry. To overcome the restriction of antigen loss on the postsynaptic target molecules that occurs during perfusion-fixation, we adopted an immersion-fixation method that enabled us to immunohistochemically quantify the expression levels of the AMPA receptor GluA1 subunit in the NAcc. Interestingly, compared to saline exposure, cocaine significantly increased the immunofluorescence intensity of GluA1 in two sub-regions, the core and the shell, of the NAcc on withdrawal day 21 following cocaine exposure, which led to locomotor sensitization. Increases in GluA1 intensity were observed in both the extra-post synaptic density (PSD) and PSD areas in the two sub-regions of the NAcc. These results clearly indicate that AMPA receptor plasticity, as exemplified by GluA1, in the NAcc can be visually detected by immunohistochemistry and confocal imaging. These results expand our understanding of the molecular changes occurring in neuronal synapses by adding a new form of analysis to conventional biochemical and electrophysiological methods.

• Bulletin of the Korean Chemical Society
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• v.33 no.5
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• pp.1627-1637
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• 2012

The coupling reaction between 5-bromo-3-phenylbenzo[c]isoxazole and diphenylamine followed by further condensation with a mono-, di- or ter-acetyl aromatic compound in the presence of diphenyl phosphate at $145^{\circ}C$ gave a novel asymmetric diarylquinolines, oligoquinolines with diphenylamine endgroups, and a first generation quinoline dendrimer in 41-82% isolated yield. The electrochemical and photophysical properties of the oligoquinolines were characterized by cyclic voltammograms (CVs) and spectroscopy. All the quinolines emit bright sky blue light due to charge transfer from quinoline group to diphenly amine with very high quantum efficiency (> 90%). Organic light-emitting diodes (OLEDs) were fabricated using these quinolines as emitting materials. Among different device architectures explored, OLEDs with a structure of ITO/PEDOT (40 nm)/TAPC (15 nm)/D-A quinoline (40 nm)/TPBI (30 nm)/LiF (1 nm)/Al using TAPC as an electron blocking layer and TPBI as a hole blocking layer gave the best performance. A high external quantum efficiency in the range of 1.2-2.3% were achieved in all the quinolines with the best performance in BBQA(5). Our results indicate diarylamino-substituted oligoquinoline and dendrimer are promising materials for OLEDs applications.

• Bulletin of the Korean Chemical Society
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• v.27 no.5
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• pp.613-630
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• 2006

Nucleic acids are virtually omnipresent; they exist in every living being. These macromolecules constitute the most important genetic storage material: the genes. Genes are conserved throughout the evolution of all living beings; they are transmitted from the parents to their offspring. Many interdisciplinary research groups are interested in modifying nucleic acids for use in a wider variety of applications. These modified oligonucleotides are used in many diverse fields, including diagnostics, detection, and therapeutics. In this account, we summarize our research efforts related to modified nucleic acid systems. First, we discuss our syntheses of modified oligonucleotides containing fluorescent tags for use as molecular probes (molecular beacons) to detect single-nucleotide polymorphisim (SNP) in nucleic acids and to distinguish between the B and Z forms of DNA. We also describe our research efforts into oligonucleotides functionalized with steroid derivatives to enhance their cell permeability, and the synthesis of several calix[4]arene-oligonucleotide conjugates possessing the ability to form defined triplexes. In addition, we have performed systematic studies to have an understanding about the functional groups necessary for a given nucleoside to behave as an organo or hydrogelator. The aggregation properties of a number of nucleoside-based phospholipids have been examined in different solvents; some of these derivatives are potential candidates for use as nucleoside-based liposomes. Finally, we also describe our research efforts toward the preparation of isoxazole- and isoxazoline-containing nucleoside derivatives and the determination of their antiviral activities.

• The Korean Journal of Pain
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• v.13 no.1
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• pp.8-18
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• 2000

Background: Intraperitoneal (IP) and intrathecal (IT) administration of $\alpha$-amino-3-hydroxy-5-methyl-4-isoxazole-propionic (AMPA) and kainate (KA) receptor antagonist attenuate hyperalgesia in various models of persistent pain. The purpose of this study was to assess the effects of IP and IT LY293558, a novel AMPA/KA receptor antagonist on mechanical hyperalgesia after incision. Methods: Sprague-Dawley rats were anesthetized with halothane and underwent plantar incision. Two hours later, responses to mechanical stimuli were assessed using the response frequency to a nonpunctate mechanical stimulus and withdrawal threshold to calibrated von Frey filaments. One group of rats received vehicle, 5 or 10 mg/kg of LY293558 IP. In the other group, vehicle, 0.2, 0.5 or 2 nmol of LY293558 was administered IT. Ataxia and motor function were also evaluated. Results: Hyperalgesia was persistent in both the vehicle and 5 mg/kg group. IP administration of 10 mg/kg of LY293558 increased withdrawal threshold at 30 and 60 min after incision; deficits in rotorod performance were observed at 30, 60, 90 and 150 min. IT administration of 0.5 nmol of LY293558 increased the median withdrawal threshold at 30 and 60 min. Motor function was only impaired at 30 min. IT administration of 2 nmol produced hemiparesis. Again, inhibition of pain behaviors outlasted the effects on motor function. Conclusions: These data further suggest AMPA/KA receptors are important for the maintenance of pain behaviors caused by incisions. IT administration of LY293558 was more effective than systemic administration and reducing pain behaviors caused by a surgical incision.