• Title/Summary/Keyword: B7H1

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Synthesis of Novel Pyrazolines of Medicinal Interest

  • Gol, Ravindra M.;Khokhani, Kamlesh M.;Khatri, Taslimahemad T.;Bhatt, Jyotindra J.
    • Journal of the Korean Chemical Society
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    • v.58 no.1
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    • pp.49-56
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    • 2014
  • Different pyrazoline derivatives (6a-h and 7a-h) were synthesized by cyclization of substituted chalcones with hydrazine hydrate in acidic as well as basic conditions. Both the reactions were performed under conventional heating and microwave irradiation and percentage yields were compared. All the reactions were accelerated in acidic and basic conditions under microwave irradiation, with higher yields. All the synthesized compounds were characterized by their spectral study (IR, MS, $^1H$ and $^{13}C$ NMR) and were tested for their antibacterial and antifungal activity. The compounds 6g and 7g exhibited significant activity against S. aureu, 7g against E. faecalis, 6b and 7b against E. coli and 6b, 6c, 7b, 7c against S. typhi. The compounds 6d and 7d exhibited significant activity against C. albicans and 6c against M. luteus. Rest of the synthesized compounds showed moderate to poor activity against tested species with compared to standard.

A Comparative Study of the Detectable Methods of Residual Oxytetracyeline in Muscle of Flounder (Paralichthys olivaceus) with Simplified Screening Test (넙치 근육중 잔류 옥시테트라싸이클린의 간이스크리닝 검출방법 비교연구)

  • Jung, Sung-Hee;Kim, Jin-Woo
    • Journal of fish pathology
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    • v.11 no.1
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    • pp.77-81
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    • 1998
  • By standardized method, Bacillus subtilis BGA, Bacillus cereus var. mycoides ATCC 11778, and Micrococcus luteus ATCC 9341 were seeded on the muller hinton agar (Difco) plate, and pH was adjusted to 6.0, 7.2, and 8.0. Five agar plates, B. subtilis (pH 6.0), B. cereus (pH 6.0), B. subtilis (pH 7.2), B. subtilis (pH 8.0), and M. luteus (pH 8.0), were employed as test plates of modified EEC 4-plate method. Oxytetracycline (OTC) with a diet was orally administered to flounder, Paralichthys olivaceus, at 100 mg/kg once a day. After oral administration, modified EEC 4-plate method by the three screening test using muscle-direct, extraction-disk and direct-disk methods was conducted for 3 fish at 1, 3, 5, 10, 15, 20, 25 and 30 days. Muscle-direct treatment of B. subtilis (pH 6.0) was found to be dubious positive (${\pm}$) at the 1st day after the administration; thereafter, it was found to be negative to the last day of the experiment. Extraction-disk and direct-disk treatment of B. subtilis (pH 6.0) were found to be negative from the 1st day to the last day after the administration. B. subtilis (pH 7.2), B. subtilis (pH 8.0), and M. luteus (pH 8.0) by the three screening tests, were found to be negative all the way after the administration. On the other hand, B. cereus (pH 6.0) by the three screening tests was clearly found to be positive for the first 15 days after the administration, and then muscle-direct and direct-disk treatment of B. cereus (pH 6.0) were found to be dubious positive at 20th days after the administration. However extraction-disk treatment of B. cereus (pH 6.0) was clearly found to be negative at the same stage; thereafter, the three screening tests of B. cereus (pH 6.0) were found negative to the last of the experiment. These findings showed that to have equal sensitivity to those determination for the residual detection of OTC, and also confirmed that B. cereus was effective test organism for the monitoring of OTC.

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Exploration of Essential Structure of Malloapelta B for the Inhibitory Activity Against TNF Induced $NF-{\kappa}B$ Activation

  • Luu, Chinh Van;Chau, Minh Van;Lee, Jung-Joon;Jung, Sang-Hun
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.840-844
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    • 2006
  • For the exploration of pharmacophoric moiety of malloapelta B (1) possessing the inhibitory activity of $NF-{\kappa}B$ activation, structural variation of ${\alpha},{\beta}-unsaturated$ carbonyl motif was attempted. 1 was reduced by catalytic hydrogenation, sodium borohydride, and lithium aluminumhydride. Catalytic hydrogenation with 30 psi or 15 psi of $H_2$ gas of 1 generated 8-butyl-5,7-dimethoxy-2,2-dimethylchroman (2) and 1-(5,7-dimethoxy-2,2-dimethylchroman-8-yl)butan-1-one (3), respectively. Reduction with sodium borohydride occurred at the double bond of ${\alpha},{\beta}-unsaturated$ ketone of 1 to give 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)butan-1-one (4). Reduction of 1 with lithium aluminumhydride and then quenched with methanol and water produced unexpected products, 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)-3-methoxy-1-butene (5) and 1-(5,7-dimethoxy-2,2-dimethyl-2H-chromen-8-yl)-3-hydroxy-1-butene (6). These are formed from the isomerization of initial product 9 through the continuous conjugate carbocation intermediate 11. Addition of ethylmagnesium bromide and dimethyl malonate anion to 1 gave the conjugate adducts 7 and 8. Ethylmagesium bromide and sodium borohydride reduction unusually gave the conjugate addition due to steric congestion around carbonyl group of 1. Compound 2 exhibits the reduced inhibitory activity against $NF-{\kappa}B$ activation and the others do not show the activity. Therefore ${\alpha},{\beta}-unsaturated$ carbonyl group of 1 should be important for its inhibitory activity.

Metabolism Activity of Bifidobacterium spp. by D.Ps of Konjac Glucomannan Hydrolysates (Konjac Glucomannan 가수분해 올리고당의 중합도별 Bifidobacterium spp.에 대한 대사활성)

  • 최준영;박귀근
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.33 no.7
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    • pp.1186-1191
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    • 2004
  • Bacillus sp. $\beta$-mannanase was purified by DEAE-sephadex ion exchange column chromatography. The partially purified P-mannanase exhibited maximum activity at pH 6.0 and 5$0^{\circ}C$, and was stable at a pH range of 5.5 to 7.0, and at temperature between 30 to 5$0^{\circ}C$. Konjac glucomannan was hydrolyzed by the purified $\beta$-mannanase, and then hydrolysates separated by 1st activated carbon column chromatography and 2nd sephadex G-25 gel filtration. The main hydrolysates were composed of D.P 5 and 7 glucomannooligosaccharides by TLC and FACE method. To investigate the effects of guar gum glucomannooligosaccharides on the in vitro growth of B. longum, B. bifidum, B. infantis, B. adolescentis, B. animalis, and B. breve, Bifidobacterium spp. were cultivated individually on the modified-MRS medium containing carbon SOUTce such as D.P 5, and D.P 7 glucomannooligosaccharides, respectively. B. longum grew up 4.6-fold and 5.3-fold more effectively by the replacement of D.P 5 and 7 glucomannooligosaccharides as the carbon source in a comparasion of standard MRS. Also, B. breve and B. animalis slightly grew up by the treatment of D.P 5 glucomannooligosaccharide.

The hyaluronan synthesis inhibitor 7-hydroxy-4-methylcoumarin inhibits LPS-induced inflammatory response in RAW 264.7 macrophage cells

  • Kim, Gwan Bo;Hyun, Chang-Gu
    • Journal of Applied Biological Chemistry
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    • v.64 no.3
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    • pp.263-268
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    • 2021
  • 7-Hydroxy-4-methylcoumarin (7H-4MC) inhibits hyaluronan production in multiple cell lines and tissue types both in vitro and in vivo. It is a commercially available drug approved for human use, called hymecromone, in European and Asian countries to prevent biliary spasms. Nevertheless, as the pharmacological efficacy of 7H-4MC has not yet been reported in macrophages, this study investigated its anti-inflammatory effects and mechanism of action using lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. LPS-induced RAW 264.7 cells were treated with various concentrations of 7H-4MC (62.5, 125, 250, and 500 μM). The application of 7H-4MC significantly reduced nitric oxide and prostaglandin E2 production without cytotoxic effects. Additionally, 7H-4MC strongly decreased the expression of inducible nitric oxide synthase and cyclooxygenase. Furthermore, 7H-4MC reduced the production of proinflammatory cytokines, such as tumor necrosis factor-α, interleukin (IL)-1β, and IL-6. Finally, 7H-4MC exerted its potent anti-inflammatory actions via the upregulation of IκB-α production, which led to the inhibition of nuclear factor-κB (NF-κB) activity. These results, obtained in macrophage cell lines, suggest that 7H-4MC prevents inflammatory diseases via the NF-κB signaling pathway and that its use could be beneficial for human health. Ultimately, this is the first report describing the anti-inflammatory activity of 7H-4MC in a macrophage cell line.

A Study for the Norms of Audiometric Tests in Koreans (정상한국인의 청력검사치에 관한 연구)

  • 오혜경;서장수;이근해;김희남;김영명;권영화;서옥기
    • Proceedings of the KOR-BRONCHOESO Conference
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    • 1981.05a
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    • pp.38.1-38
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    • 1981
  • Currently in the otologic field, there are various methods of special audiometric examinations, such as, tone decay, SISI, and impedance audiometry and only a few studies has been done in these fields sporadically in Korea. The purpose of this paper is to establish norms of various special audiometric tests, so we have performed the special audiometric tests on 100 male medical students in good physical condition and the follow results were obtained. 1. All cases showed over 90% of PB scores. The mean and its 2 S.D. were 98$\pm$4.9% in the right ear and 97$\pm$5.6% in the left ear. 2. The mean and its 2 S.D. of MCL(most comfortable level) were 45$\pm$15.4 dB in the right ear and 46$\pm$17.9 dB in the left ear, and its range was 12$\pm$12.2 dB in the right ear and 13$\pm$12.6 dB in the left ear. 3. The mean and its 2 S.D. of UCL (uncomfortable level) were 102$\pm$7.9 dB in the right ear and 102$\pm$7.9 dB in the left ear and about an half in cases showed over 106 dB of UCL. 4. In 95% of cases, SISIs(short increment sensitivity index) at 1, 000 Hz and 4000 Hz was below 45% in the right ear in both frequencies and below 55% and 75% in the left ear, respectively. 5. In 95% of cases, tone decays at 2, 000 Hz and 4, 000 Hz was below 10 dB in both ears. 6. The difference between SRT and PTA (speech reception threshold minus pure tone average) was 4$\pm$9.2 dB in the right ear and 4$\pm$10.0 dB in the left ear. 7. The dynamic range(uncomfortable level minus speech reception threshold) was 98$\pm$13.5 dB in the right ear and 99$\pm$13.5 dB in the left ear. We had trouble in estimating the dynamic range in about an half in cases, in which we couldn't estimate the UCL with our conventional audiometry. 8. The results of impedance audiometric tests were as follow: A. In the tympanogram, all cases were of A type with one exception of B type in the left ear. The mean and its 2 S.D. of its peak level were 22.8$\pm$32.94mm $H_2O$ in the right ear and 23.9$\pm$29. 81mm $H_2O$ in the left ear. B. The mean and its 2 S.D. of the compliance were 0.6$\pm$0.54cc in the right ear and 0.6$\pm$0.53cc in the left ear. C. The results of stapedial reflex: a. The mean and its 2 S.D. of the controlateral stapedial reflex at 500Hz, 1, 000Hz, 2, 000Hz, 4, 000Hz were 99$\pm$17.7 dB, 87$\pm$14.4 dB, 79$\pm$13.7 dB, 77$\pm$20.0 dB in the right ear and 99$\pm$15.9 dB, 88$\pm$13.9 dB, 79$\pm$13.7 dB, 77$\pm$21.3 dB in the left ear. Depending on the tested frequencies, the stapedial reflex wasn't generated in 6 cases in the right ear and 11 cases in the left ear. b. The mean and its 2 S.D. of the ipsilateral stapedial reflex at 1, 000Hz, and 2, 000Hz were 89$\pm$16.3 dB, 82$\pm$15.9 dB in the right ear and 89$\pm$18.0 dB, 83$\pm$18.9 dB in the left ear. Depending on the tested frequencies, the stapedial reflex wans't generated in 1 case in the right ear and 2 cases in the left ear. 9. Eustachian tube function using with impedance audiometry was malfunctioned in21 cases depending on the tested pressure and the range of peak level of tympanogram was 14$\pm$26.9mm $H_2O$(tested pressure:+250mm $H_2O$), 8$\pm$21.9mm $H_2O$ (tested pressure:-250mm $H_2O$) in the right ear and 11 cases depending on the tested pressure and the range of the peak level of tympanogram was 12$\pm$22.5mm $H_2O$ (tested pressure: +250 mm $H_2O$, 9$\pm$17.3mm $H_2O$(tested pressure: -250mm $H_2O$) in the left ear.

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Media Optimization for the Production of Aminopeptidase M Inhibitors MR-387A and B by Streptomyces sp. SL-387 (Streptomyces sp. SL-387에 의한 Aminopeptidase M 저해제 MR-387A 및 B의 생산 배지 최적화)

  • Chung, Myung-Chul;Chun, Hyo-Kon;Lee, Ho-Jae;Lee, Choong-Hwan;Kim, Su-Il;Kho, Yung-Hee
    • Applied Biological Chemistry
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    • v.38 no.2
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    • pp.100-105
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    • 1995
  • Media optimization for the production of MR-387A and B, novel aminopeptidase M inhibitors by Streptomyces sp. SL-387 isolated from a soil was studied. Optimized medium was consisted of 1% glucose, 3% soybean meal, 0.2% yeast extract, 0.1% beef extract, 0.3% NaCl, 0.01% $K_2HPO_4$, 0.3% $CaCO_3$, 0.001% $MnCl_2{\cdot}4H_2O$, 0.001% $ZnCl_2{\cdot}7H_2O$, and 0.0005% $MgSO_4{\cdot}7H_2O$, and adjusted to pH 7.0 before autoclaving. When the optimized medium was used as a fermentation medium, maximum productivity of MR-387 was reached at 120 hours of fermentation, and total productivity was 909.1 U/ml.

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The Crystal and Molecular Structure of Ethylenediammonium bis (P-Methylbenzenesulfonate) Monohydrate (에티렌디암모늄 비스(파라-메틸벤젠슬폰네이트) 수화물의 결정 및 분자구조)

  • Choong Tai Ahn;Eul-San Kim
    • Journal of the Korean Chemical Society
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    • v.29 no.4
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    • pp.335-340
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    • 1985
  • The crystal structure of ethylenediammonium bis (p-methylbenzenesulfonate) monohydrate, $C_2H_{10}N_{22}^{+2}{\cdot}(C_7O_3H_7S^-){\cdot}H_2O$ has been determined by X-ray diffraction techniques. The space group is P21, in 2 unit cell with a = 12.649 (2) ${\AA}$, b = 7.727 (1) ${\AA}$, c = 11.295 (2) ${\AA}$, ${\beta}$ =111.8(1)$^{\circ}$, and z = 2. The structure was solved by direct methods and refined to R = 0.060 for 1134 reflections measured with Mo-K${\alpha}$ radiation. Two p-methylbenzenesulfonates, fragment A and B, from a pair through the hydrogen bonds to the ethylenediammonium ion. The sulfonate group in the fragment B are disordered. There are six unique hydrogen bonds, of which four are between the ethylenediammonium ion and the sulfonate groups and remaining two involve the water molecule.

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Synthes is of 9,10-difluoro-5,6,6a,7,11b-pentahydroindano [2,1-c]isoquinoline (9,10- 디플루오르 -5,6,6a,7,11b- 펜타하이드로인다노[2,1-c] 이소퀴놀린의 합성)

  • Ma, Eun-Sook;Kim, Min-Jung
    • YAKHAK HOEJI
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    • v.44 no.6
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    • pp.505-510
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    • 2000
  • The synthesis of pentahydroindanoisoquinoline (4) compound has been achieved via the cyclization of 2-(N-benzylamino)-5,6-difluoro-1-indanol (10a, 10b), which was prepared by condensation and reduction of 2-amino-1-indanol and benzaldehyde in ethanol. The stereochemistry of $H_{6a}$ and $H_{11b}$ of 9,10-difluoro-5,6,6a,7,11b-pentahydroindano[2,1-c]isoquinoline (4) was the trans B/C ring fusion.

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Synthesis of Adriamycin-related System (1) -Synthesis of the Derivative of Tetrahydrobenzo(b)phenazine as a Potential Isostere of Anthracyclinone- (아드리아마이신의 유사제제 합성 (1) -안트라싸이클리논의 Isostere 로서 Tetrahydrobenzo(b)phenazine 유도체의 합성-)

  • Jahng, Yurng-Dong;Chang, Sun-Young
    • YAKHAK HOEJI
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    • v.34 no.4
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    • pp.219-223
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    • 1990
  • 7,8-Dihydro-6,11-dihydroxy-9(10H)benzo(b)phenazinone was prepared from 1,2,3,4-tetra-hydrophenazine as a potential isostere of anthracyclinone. The attempts to functionalize at $C_9$ were not successful due to the unstability of the above ketone.

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