• Archives of Pharmacal Research
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• v.14 no.4
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• pp.359-363
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• 1991

2,6-Dimethyl-4-(3'-nitrophenyl)1,4-dihydropyridine-3,5-dicarboxylic acid 5-(2'-cyanoethyl) ester 10a reacted with chloromethyl methylsulfide to give 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-methylthiomethyl 5-(2'-cyanoethyl) ester 11a in 88.1% yield. The synthesis of 2,6-dimethyl-4-(3'-nitrophenyl)-1,4-dihydropyridine-3,5-dicrboxylic acid 3-methylthiomethyl ester 2a was achieved in 83% yield by alkaline hydrolysis of compound 11a in aqueous EtOH.

• Elastomers and Composites
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• v.58 no.1
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• pp.26-31
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• 2023

Aromatic diamine containing ortho catenation and methyl group was synthesized from 4-methyl catechol and 4-nitrobenzoyl chloride. Subsequently, a poly(amic acid) was prepared by reacting 4-methyl-1,2-phenylene bis(4-aminobenzoate) with 4,4'-hexafluoroisopropylidenediphthalic anhydride (6FDA). The resulting poly(amic acid) was transformed into a polyimide through chemical imidization. The polyimide formed was soluble in N-methyl-2-pyrrolidone (NMP) and could be cast into a flexible, transparent film. Furthermore, the polyimide exhibited a 5% weight loss at 380 ℃ in the nitrogen atmosphere.

• Korean Journal of Biological Psychiatry
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• v.7 no.2
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• pp.152-158
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• 2000

Background : No association between schizophrenia and dopamine D4 receptor polymorphisms have been reported. Despite these results, it is premature to exclude the association. It has been suggested that the susceptibility to develop schizophrenia could result from variation at a number loci which may interact or coact with each other. Therefore, we investigated a possible association of combinations of exon III 48bp polymorphism[D4E3] and exon I 12bp polymorphism of the DRD4 gene [D4E1] with schizophrenia. Methods : 207 unrelated Korean schizophrenic patients and 191 healthy controls were recruited. DRD4 genotype was established using the polymerase chain reaction. Statistical analysis consisted of ${\chi}^2$ tests for Hardy-Weinberg proportions and genotypic and allelic frequencies in the patients and control groups. Results : There were no statistically significant differences in the each polymorphisms between schizophrenics and controls. And all genotype frequencies were within Hardy-Weinberg expectations. When the combinations of the polymorphism in schizophrenia and controls were compared, however, there were significant differences at $A1A2^*2/4$ in the distributions of the combinations of D4E1 and D4E3(p<0.01). Conclusions : These findings suggest that the certain combination of D4E1 and D4E3($A1A2^*2/4$) has the protective role to a susceptibility for schizophrenia.

• Journal of the Korean Chemical Society
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• v.55 no.4
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• pp.638-643
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• 2011

The synthesis of biologically active 1H-1,4-diazepines 4a-d and 3H-1,5-benzodiazepines 5a-d in good yields, from the heterocyclization reaction of 2-(4-methylthio benzenesulfonyl)-1,3-dimethyl/1-methyl-3-phenyl/1,3-diphenyl/1-methyl-3-ethoxy propane-1,3-dione 3a-d with ethylenediamine (EDA) and o-phenylenediamine (o-PDA), respectively, in the presence of silica sulfuric acid (SSA) is described. The novel ${\beta}$-diketones/${\beta}$-ketoesters 3a-d were synthesized by the condensation reaction of 4-methylthiobenzenesulfonyl chloride 1 with various ${\beta}$-diketones/${\beta}$-ketoesters 2a-d. All structures of the newly synthesized compounds were elucidated by elemental analysis and spectral studies. The compounds 4a-d and 5a-d have been screened for antimicrobial, antifungal and anthelmintic activity.

• YAKHAK HOEJI
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• v.49 no.4
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• pp.299-305
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• 2005

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 3,4-difluorophenyl (2a-5a), 4-hydroxyphenyl (2b-5b), 3-nitro­phenyl (2c-5c), 4-chlorobenzothiazoly (2d-5d) and 5-methylfurfural (2e-5e) instead of naphthyl group, and with hydrogen (3a-3e), methyl (4a-4e) and ethyl (5a-5e) in the place of methyl in naftifine were synthesized and tested for their in vitro anti-fungal activities against five different fungi. Fourteen compounds (3a, 4a, 5a, 3b, 4b, 5b, 3c, 4c, 5c, 3d, 4d, 3e, 4e and 5e) showed significant anti-fungal activities against T. mentagrophytes. (E)-N-(3-Phenyl-2-propenyl)-3,4-difluoro-ben­zenemethaneamine(3a), (E)_N_(3_phenyl_2_propenyl)_4_hydroxy_benzenemethaneamine(3b) and (E)-N-ethyl-N-(3-phenyl­2-propenyl)-3-nitro-benzenemethaneamine (5c) displayed moderate anti-fungal activities against all five different fungi.

• Journal of the Korean Chemical Society
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• v.35 no.5
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• pp.575-579
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• 1991

Reaction of 6${\beta}$-bromopenicillanic acid(4a) with p-nitrobenzylbromide, 3-bromophthalide, chloromethylpivalate and 1-chlorodiethylcarbonate afforded 6${\beta}$-bromopenicillanates(4b~4e). New ${\beta}$-lactam compound, 6-(carboxymethylthio)penicillanic acid(5a) and the other esters(5b~5e) were prepared by nucleophilic substitution reaction of 6${\beta}$-bromopenicillanic acid(4a) and the other esters(4b~4e) with thioglycolic acid.

• BMB Reports
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• v.31 no.1
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• pp.83-88
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• 1998

Recently a B cell surface molecule, CD40, has emerged as a receptor mediating a co-stimulatory signal for B cell proliferation and differentiation. To investigate the mechanism of synergy between interleukin-4 (IL-4) and CD40 ligation in B cell activation, we have examined the effect of CE40 cross-linking on the IL-4 receptor expression in human B cells using anti-CE40 antibody. We observed that IL-4 and anti-CD40 both induce IL-4 receptor gene expression with a rapid kinetics resulting in a noticeable accumulation of IL-4 receptor mRNA within 4 h. While IL-4 caused a dose-dependent induction of surface IL-4 receptor expression, the inclusion of anti-CD40 in the IL-4-treated culture, further up-regulated the IL-4-induced IL-4 receptor expression as analyzed by flow cytometry. Pretreatment of B cells with inhibitors of protein tyrosine kinase (PTK) resulted in a significant inhibition of both the IL-4- and anti-CD40-induced IL-4 receptor mRNA levels, while protein kinase C (PKC) inhibitors had no effects. These results suggest that IL-4 and CD40 ligation generate B cell signals, which via PTK-dependent pathways, lead to the synergistic induction of IL-4 receptor gene expression. The rapid induction of IL-4 receptor gene expression through the tyrosine kinase-mediated signal transduction by B cell activating stimuli, would provide cells capacity for an efficient response to IL-4 in the early phase of IL-4 action, and may in part constitute the molecular basis of the reported anti-CD40 co-stimulatory effect on the IL-4-induced response.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2003.11a
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• pp.88-88
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• 2003

Cytochrome P-450 3A4 (CYP3A4) is major enzyme in human liver, the role of this is detoxification and metabolizing more than 50% clinical drugs in use. Expression of CYP3A4 is transciptionally regulated by the Pregnenolone X receptor (PXR), of which human form is Steroid and Xenobiotics receptor (SXR). SXR is activated by wide range of endogenous and exogenous compounds, and then induces CYP3A4 gene expression. In the previous study, it has been known that proximal promoter (-864 to +64) does not response to chemical inducers such as pregnenolone 16a-carbonitrile (PCN), Rifampicin, Estrogen in terms of transcription of CYP 3A4 in cultured cells. Here, we developed luciferase reporter gene assay system to detect SXR-based CYP 3A4 transcriptional activity. We have used CYP3A4-Luc plasmid that contains proximal promoter of human CYP3A4 gene upstream of the luciferase gene. We did transient transfection of 3A4-luciferase gene and SXR. In the HepG2 cells transfected with CYP3A4-Luc, when rifampicin treatment was combined with histone deacetylase inhibitor (HDAC Inhibitor), such as Trichostatin A, Hc-toxin and IN 2001 of the luciferase activity was induced 10-20 fold over control.

• Proceedings of the Korea Society of Environmental Toocicology Conference
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• 2003.10a
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• pp.178-178
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• 2003

Cytochrome P-450 3A4 (CYP3A4) is major enzyme in human liver, the role of this Is detoxification and metabolizing more than 50% clinical drugs in use. Expression of CYP3A4 is transciptionally regulated by the Pregnenolone X receptor (PXR), of which human form is Steroid and Xenobiotics receptor (SXR). SXR is activated by wide range of endogenous and exogenous compounds, and then induces CYP3A4 gene expression. In the previous study, it has been known that proximal promoter (-864 to ＋64) does not response to chemical inducers such as pregnenolone 16a-carbonitrile (PCN), Rifampicin, Estrogen in terms of transcription of CYP 3A4 in cultured cells. Here, we developed luciferase reporter gene assay system to detect SXR-based CYP 3A4 transcriptional activity. We have used CYP3A4-Luc plasmid that contains proximal promoter of human CYP3A4 gene upstream of the luciferase gene. We did transient transfection of 3A4-luciferase gene and SXR. In the HepG2 cells transfected with CYP3A4-Luc, when rifampicin treatment was combined with histone deacetylase inhibitor (HDAC Inhibitor), such as Trichostatin A, Hc-toxin and IN 2001 of the luciferase activity was induced 10-20 fold over control.

• Journal of applied mathematics & informatics
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• v.39 no.5_6
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• pp.859-882
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• 2021

In the proposed paper, a new algorithm based on Nonlinear Feedback Shift Register (NLFSR) and modified RC4A (Rivest Cipher 4A) cipher is introduced. NLFSR is used for image pixel scrambling while modified RC4A algorithm is used for pixel substitution. NLFSR used in this algorithm is of order 27 with maximum period 2^27-1 which was found using Field Programmable Gate Arrays (FPGA), a searching method. Modified RC4A algorithm is the modification of RC4A and is modified by introducing non-linear rotation operator in the Key Scheduling Algorithm (KSA) of RC4A cipher. Analysis of occlusion attack (up to 62.5% pixels), noise (salt and pepper, Poisson) attack and key sensitivity are performed to assess the concreteness of the proposed method. Also, some statistical and security analyses are evaluated on various images of different size to empirically assess the robustness of the proposed scheme.