• Journal of the Korean Chemical Society
• /
• v.54 no.4
• /
• pp.429-436
• /
• 2010

A series of some biologically active halogenopurines were synthesized from commercially available guanine (1). The reaction of guanine with acetic anhydride yielded 2,9-diacetylguanine (2-1) by acetylation reaction. Further treatment of 2-1 with $POCl_3$ by PEG-2000 phase transfer catalysis furnished the important compound 3a, then 2-amino-6-halogenopurines (3b-d) were obtained through chlorine-exchange halogenations between KX and 3a by TPPB phase transfer catalyst. Further, 2-halogenopurines (2-2a-d, 4-2a-d, 5a-d) were efficiently prepared from 2-amino-6-substituted purines (1, 3a, 4-1) via a diazotization catalyzed by their corresponding CuX, and some new compounds 2-2a, 2-2c, 2-2d, 4-2c, 4-2d, 5b, 5c and 5d have been discovered. The structures of synthesized compounds were mainly established on the basis of their elemental analysis, $^1H$ NMR, as well as their mass spectral data. All the title compounds were screened for their antifungal activities, and some of the compounds showed promising activity.

• Journal of Microbiology and Biotechnology
• /
• v.32 no.6
• /
• pp.740-748
• /
• 2022

As circ_UBE2D2 has been confirmed to have targeted binding sites with multiple miRNAs involved in septic acute kidney injury (SAKI), efforts in this study are directed to unveiling the specific role and relevant mechanism of circ_UBE2D2 in SAKI. HK-2 cells were treated with lipopolysaccharide (LPS) to construct SAKI model in vitro. After sh-circ_UBE2D2 was transfected into cells, the transfection efficiency was detected by qRT-PCR, cell viability and apoptosis were determined by MTT assay and flow cytometry, and expressions of Bcl-2, Bax and Cleaved-caspase 3 were quantified by western blot. Target genes associated with circ_UBE2D2 were predicted using bioinformatics analysis. After the establishment of SAKI rat model, HE staining and TUNEL staining were exploited to observe the effect of circ_UBE2D2 on tissue damage and cell apoptosis. The expression of circ_UBE2D2 was overtly elevated in LPS-induced HK-2 cells. Sh-circ_UBE2D2 can offset the inhibition of cell viability and the promotion of cell apoptosis induced by LPS. Circ_UBE2D2 and miR-370-3p as well as miR-370-3p and NR4A3 have targeted binding sites. MiR-370-3p inhibitor reversed the promoting effect of circ_UB2D2 silencing on viability of LPS-treated cells, but shNR4A3 neutralized the above inhibitory effect of miR-370-3p inhibitor. MiR-370-3p inhibitor weakened the down-regulation of NR4A3, Bax and Cleaved caspase-3 and the up-regulation of Bcl-2 induced by circ_UB2D2 silencing, but these trends were reversed by shNR4A3. In addition, sh-circ_UBE2D2 could alleviate the damage of rat kidney tissue. Circ_UBE2D2 mitigates the progression of SAKI in rats by targeting miR-370-3p/NR4A3 axis.

• YAKHAK HOEJI
• /
• v.48 no.4
• /
• pp.254-260
• /
• 2004

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 2,4-difluorophenyl( 2a-5a), 2,5-difluorophenyl(2b-5b), 4-ethylphenyl(2c-5c), 2-hydroxyphenyl(2d-5d) and 2-methylnaphthyl(2e-5e) instead of naphthyl group with hydrogen(3a-3e), methyl(4a-4e), and ethyl(5a-5e) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds( 3a, 4a, 5a, 3d, 4d, 4d, 5d, 3e, and 4e) showed significant anti-fungal activity against T. mentagroPhytes. (E)-N-(3-Phenyl-2-propenyl)-2- hydroxy-benzenemethaneamine( 3d) displayed moderate antifungal activity against all five different fungi.

• Korean Journal of Weed Science
• /
• v.16 no.1
• /
• pp.36-41
• /
• 1996

The experiments were conducted to identify the herbicidal effect of 2,4-D{ (2,4-dichlorophenoxy) acetic acid}, 2,4-D ethylester {ethyl 2,4- dichlorophenoxy acetate} and bentazon{3- isopropyl-1H-2,1,3- benzothiazin- 4-(3H)one 2,2-dioxide} on Sagittaria trifolia. Both 2,4-D and 2,4-D ethylester could completely control S. trifolia when applied before 80 days after transplanting of the tubers (DAT), but the weeding effect by bentazone decreased when applied after 60 DAT. 2,4-D and 2,4-D ethylester were effectively translocated from the treated parts to growing point. They killed S. trifolia completely when applied at 80 DAT under 3cm standing water depths, but the controlling effect by bentazone decreased at deeper than 1cm standing water depth. Formation of S. trifolia tuber was effectively suppressed with 2,4-D at 7g ai/10a and 2,4-D ethylester at 6g ai/10a when applied 60 DAT.

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

• Journal of Oriental Neuropsychiatry
• /
• v.28 no.3
• /
• pp.157-164
• /
• 2017

Objectives: The purpose of this study is the research of the 2D:4D ratio and its correlation with the Sasang constitution and the MBTI preference types. Methods: A measurement of the 2D:4D ratios of 101 South Korean medical students was performed, the QSCC-II and PSSC-2004 were used to diagnose the Sasang constitution, and MBTI testing was performed to classify the preference types. Results: In the relationship between the Sasang constitution and the 2D:4D ratios, a statistically significant difference is absent in the 2D:4D ratios of the group comprising both sexes in the order of Taeumin, Soyangin, and Soeumin. A statistically significant difference is also lacking in the 2D:4D ratios of the male-only group in the order of Taeumin, Soyangin, and Soeumin. The 2D:4D ratios are higher in the female group only, but again a statistically significant difference is absent. In the 2D:4D ratios according to the MBTI preference type, the 2D:4D ratios of the I, S, F, and P types are higher in the unisex group, but a significant difference is not evident. The 2D:4D ratios of the E, N, F, and P types are higher in the male-only group, but again a significant difference is not evident. In the female-only group, the mean of the 2D:4D ratios of the I, S, F, and P types is higher, but a significant difference is not identifiable. Conclusions: The Sasang constitution and the MBTI preference types did not show statistically significant differences regarding the 2D:4D ratios of the male, female, and unisex groups.

• Bulletin of the Korean Chemical Society
• /
• v.14 no.2
• /
• pp.188-191
• /
• 1993

The reaction between methyl 2,3-di-O-benzyl-4,6-di-O-mesyl-${\alpha}$-D-glucopyranoside (1b) and potassium superoxide resulted in hydrolysis, and gave methyl 2,3-di-O-benzyl-${\alpha}$-D-glucopyranoside (1) as a sole product. When the reaction was performed with a vicinal dimesylate, methyl 4,6-O-benzylidene-2,3-di-O-mesyl-${\alpha}$-D-altropyranoside (4b), again the hydrolysis product, methyl 4,6-O-benzylidene-${\alpha}$-D-altropyranoside (4) was obtained. However, the reaction of potassium superoxide with another vicinal dimesylate, methyl 4,6-O-benzylidene-2,3-di-O-mesyl-${\alpha}$-D-glucopyranoside (3b), nucleophilic displacement took place to afford methyl 4,6-O-benzylidene-${\alpha}$-D-altropyranoside (4). Apparently different results from two trans vicinal dimesylates, 3b and 4b are explained by the transient formation of epoxides, methyl 2,3-anhydro-4,6-O-benzylidene-${\alpha}$-D-allopyranoside (8) and methyl 2,3-anhydro-4,6-O-benzylidene-${\alpha}$-D-mannopyranoside (9) by $KO_2$. The reaction between the allo epoxide 8 and $KO_2$ gave altro 4. The manno epoxide 9 also afforded altro 4 as the major product. Facile epoxide formation by the reaction of a vicinal dimesylate and superoxide was also observed with 3-O-benzyl-1,2-O-isopropylidene-5,6-di-O-mesyl-${\alpha}$-D-glucofuranose: 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-${\beta}$-L-idofuranose was obtained.

• KOREAN JOURNAL OF CROP SCIENCE
• /
• v.34 no.4
• /
• pp.422-427
• /
• 1989

Weeds may compete detrimentally with the ginseng for moisture and nutrients but hand weeding is the only practical means of eliminating weeds after crop establishment. To define the effects of 2, 4-D herbicide application on the plant growth and root yield of Korean ginseng (Panax ginseng C. A. Meyer). the herbicide 2, 4-D was applied as a foliar spray with the rates of 0.5. 1.0. 1.5 and 2.0 times of the recommended herbicide dosage 70ml/l0a. The Korean ginseng treated with 2, 4-D in the rate of two times concentration was indistinguishable from nontreated plants in visual rating for foliar symptoms. There were no significant differences of the leaf length and width as well as the stem length and diameter in check plants and those recieving 2, 4-D treatments. The. berry maturing in 3 and 4-years old ginseng was not inhibited with 2, 4-D treatment. The root weight of the 4-years old ginseng plant was not reduced by 2, 4-D application of 2 times dosage. However. when the ginseng seedling was treated with 2, 4-D. detrimental phenomena as stem bending and dicoloration of marginal part of seedling leaf were occured but stem bending was recovered in a few days.

• Applied Biological Chemistry
• /
• v.3
• /
• pp.25-48
• /
• 1962

The polysaccharide C prepared from gum tragacanth powder (U. S. P. grade) by the precipitation method with 85% ethanol was a neutral polysaccharide, $[{\alpha}]^{30}_D-72.2$. The polysaccharide C consisted of L-rhamnose, D-xylose, L-arabinose and D-galactose in the molar ratio 2:1:17:9 (Table 1, 2, 3, ). The polysaccharide C was methylated with dimethylsulphate and 40% NaOH, and Purdies regent. The hydrolyzate of fully methlated product ($[{\alpha}]^{22}_D-102$ in chloroform, the methoxy content 40.6%) was composed of 2, 3, 5-tri-O-methyl-L-arabofuranose (I), 3,4-di-O-methyl-L-rhamnopyranose (II), 2,3-di-O-methyl-D-xylose (III), 2,3,4-tri-O-methyl-D-galactopyranose (IV), 2,4-di-O-methyl-L-arabopyranose (?), 2,4-di-O-methyl-D-galactose(VI), 2-O-methyl-D-arabinose (VII), and L-arabopyranose(VIII) (Table 4, 5, and Fig. 4). The first partial hydrolysis (A) of the polysaccharide C with 0.05N-HCl for 4.5 hours at $80-85^{\circ}C$ released only L-arabinose: the second hydrolysis (B) with 0.1N-HCl for 5 hours at $80-85^{\circ}C$, L-arabinose and D-galactose; and the third hydrolysis (C) with 0.3N-HCl at $90-95^{\circ}C$ in sealed tube, L-rhamnose, D-xylose, L-arabinose and D-galactose. From the unhydrolyzate A' were found L-rhamnose, D-xylose, L-arabinose, and D-galactose; from B' L-rhamnose, d-xylose, L-arabinose and D-galactose; and from C' D-xylose and D-galactose respectively (Table 6). The periodate consumption and formic acid production of the polysaccharide C were measured at various time intervals. After 120 hours periodat was consumed by 1.23 mole per $C_5H_8O_4$ and formic acid was produced 0.78 mole per $C_5H_8O_4$ (Table 7). Although a definite chemical structure for this polysaccharide C may not be formulated, experimental data, especially, from methylation, partial hydrolysie and determination of its molar ratio, and periodate analysis showed that the polysaccharide C is a highly branched polysaccharide and would be constructed of galactoaraban as a main chain residue and L-arabofuranose, D-galactopyranosyl $(1{\rightarrow}1)$-L-arabofuranose, D-xylopyranosyl $(1{\rightarrow}2)$-L-rhamnopyranosyl $(1{\rightarrow}1)$-L-arabofuranose, and L-rhamnopyranosyl $(1{\rightarrow}1)$-arabofuranose, and D-galactopyranosyl-$(1{\rightarrow}2)$-L-arabopyranosyl-$(1{\rightarrow}1)$-I-arabofuranose as a branch chain or end group (page 21).

• Journal of Advanced Navigation Technology
• /
• v.13 no.1
• /
• pp.48-53
• /
• 2009

The CMOS RF front-end for Global Positioning System(GPS)are implemented in 1P8M CMOS $0.13{\mu}m$ process. The LNAs consist of LNA1 with high gain and low NF, and LNA2 with low gain and high IIP3 for supporting operation with active and passive antenna. the measured performances of both LNAs are 16.4/13.8 dB gain, 1.4/1.68 dB NF, and -8/-4.4 dBm IIP3 with 3.2/2 mA form 1.2 V supply, respectively. The quadrature downconversion mixer is followed by transimpedance amplifier with gain controllability from 27.5 to 41 dB. The front-end performances in LNA1 mode are 39.8 dB conversion gain, 2.2 dB NF, and -33.4 dBm IIP3 with 6.6 mW power consumption.