• Title/Summary/Keyword: $^1H{\

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Synthesis and Biological Evaluation of Some Novel [4-(1H-Benzoimidazol-2-yl)-thiazol-2-yl]-benzylidene-amines and N-[4-(1H-Benzoimidazol-2-yl)-thiazol-2-yl]-N'-benzylidene-hydrazines

  • Mekala, Raghu Vardhan Reddy;Danda, Ravinder Reddy;Gadegoni, Hemalatha
    • Journal of the Korean Chemical Society
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    • v.57 no.1
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    • pp.94-98
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    • 2013
  • A new family of thiazole heterocycles, namely [4-(1H-benzoimidazol-2-yl)-thiazol-2-yl]-benzylidene-amines has been synthesized by the condensation of 4-(1H-Benzoimidazol-2-yl)-thiazol-2-ylamine with various aromatic aldehydes and N-[4-(1H-benzoimidazol-2-yl)-thiazol-2-yl]-N'-benzylidene-hydrazines through the cyclization of 1-(1H-benzoimidazol-2-yl)-2-bromo-ethanone with arylthiosemicarbazones. The target compounds are achieved by using 1-(1H-Benzoimidazol-2-yl)-ethanone as starting material. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and Mass spectral data. Further the compounds were used to evaluate their antimicrobial activity and found that the appreciable antimicrobial activity by some of the title compounds.

ON THE MEAN VALUES OF DEDEKIND SUMS AND HARDY SUMS

  • Liu, Huaning
    • Journal of the Korean Mathematical Society
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    • v.46 no.1
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    • pp.187-213
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    • 2009
  • For a positive integer k and an arbitrary integer h, the classical Dedekind sums s(h,k) is defined by $$S(h,\;k)=\sum\limits_{j=1}^k\(\(\frac{j}{k}\)\)\(\(\frac{hj}{k}\)\),$$ where $$((x))=\{{x-[x]-\frac{1}{2},\;if\;x\;is\;not\;an\;integer; \atop \;0,\;\;\;\;\;\;\;\;\;\;if\;x\;is\;an\;integer.}\$$ J. B. Conrey et al proved that $$\sum\limits_{{h=1}\atop {(h,k)=1}}^k\;s^{2m}(h,\;k)=fm(k)\;\(\frac{k}{12}\)^{2m}+O\(\(k^{\frac{9}{5}}+k^{{2m-1}+\frac{1}{m+1}}\)\;\log^3k\).$$ For $m\;{\geq}\;2$, C. Jia reduced the error terms to $O(k^{2m-1})$. While for m = 1, W. Zhang showed $$\sum\limits_{{h=1}\atop {(h,k)=1}}^k\;s^2(h,\;k)=\frac{5}{144}k{\phi}(k)\prod_{p^{\alpha}{\parallel}k}\[\frac{\(1+\frac{1}{p}\)^2-\frac{1}{p^{3\alpha+1}}}{1+\frac{1}{p}+\frac{1}{p^2}}\]\;+\;O\(k\;{\exp}\;\(\frac{4{\log}k}{\log\log{k}}\)\).$$. In this paper we give some formulae on the mean value of the Dedekind sums and and Hardy sums, and generalize the above results.

Effects of $H_2O_2$ and ascorbic acid on TIMP-2, Type1 collagen, and PDLs22 levels in human periodontal ligament fibroblasts (($H_2O_2$와 ascorbic acid가 사람 치주인대섬유모세포의 TIMP-2, Type 1 collagen, PDLs22 발현에 끼치는 효과)

  • Choi, Yong-Sun;Kim, So-Young;Choi, Seong-Mi;Jang, Hyun-Seon;Kim, Byung-Ock
    • Journal of Periodontal and Implant Science
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    • v.37 no.4
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    • pp.655-669
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    • 2007
  • Reactive oxygen species (ROS) have been implicated in the pathogenesis of various diseases. And vitamin C has shown a protective effect for the tissues. The aim of this study was to evaluate the effects of $H_2O_2$ and ascorbic acid on matrix metalloproteinase-1 (MMP-1), tissue inhibitor of metalloproteinase (TIMP: TIMP-1, TIMP-2), Type 1 collagen, fibronectin, and PDLs22 level in human periodontal ligament fibroblasts (hPDLF) via reverse transcription-polymerase chain reaction (RT-PCR). hPDLF was obtained from a healthy periodontium and cultured in Dulbecco's modified Eagles's medium plus 10% fetal bone serum. The concentration of ascorbic acid in hPDLF was $50{\mu}g/ml$, and that of $H_2O_2$ in hPDLF was 0.03% and 0.00003%. Ascorbic acid only, $H_2O_2$ only and mixture of ascorbic acid and $H_2O_2$ were applied with hPDLF for 1-, 3-, and 30-min. respectively. The gene expression of MMP-1-, TIMP-1-, TIMP-2-, Type 1 collagen-, fibronectin-, and PDLs22-mRNA in hPDLF was analysed via RT-PCR. The results were as follows; 1. hPDLF in response to 30-min. incubation with 0.03% $H_2O_2$ did not show any gene expression. 2. In all the experimental groups, the gene expression of fibronectin mRNA showed the decreased tendency compared to control. 3. In all the experimental groups, the gene expression of TIMP-1 mRNA showed the tendency similar to control. 4. hPDLF in response to 30-min. incubation with 0.03% $H_2O_2$ and ascorbic acid increased mRNA induction for MMP-1. 5. In all the experimental groups, hPDLF increased mRNA induction for PDLs22, collagen type 1, and TIMP-2 compared to control. Within the limited experiments, $H_2O_2$ and ascorbic acid increased mRNA induction for PDLs22, collagen type 1, TIMP-2 in hPDLF. More research will be needed in order to confirm the relative importance of the different roles of ROS and antioxidants in hPDLF from a periodontal regeneration or repair standpoint.

A DOUBLY COMMUTING PAIR OF HYPONORMAL OPERATORS

  • Kim, Yong-Tae
    • Bulletin of the Korean Mathematical Society
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    • v.36 no.2
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    • pp.351-355
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    • 1999
  • If ($H_1$, $H_2$) is a doubly commuting pair of hyponormal operators on a Hilbert spaces H, then there exists a commuting pair ($T_1$,$T_1$) of contractions on H such that $H_i$=$H_i^*$$T_i$ for each i=1,2.

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THE NEARLY $H_1$-STIELTJES REPRESENTABLE OPERATORS

  • Yoon, Ju-Han
    • The Pure and Applied Mathematics
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    • v.8 no.1
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    • pp.53-59
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    • 2001
  • In this paper, we define the $H_1$-Stieltjes representable, nearly $H_1$-Stieltjes represnetable for vector-valued function, which is the generalization of Bochner representable and than study some properties of these operators.

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Regulation of Intracellular pH by SHC1 in Saccharomyces cerevisiae (효모에서 SHC1 유전자의 이온 농도 조절에 의한 세포내 pH 항상성 유지)

  • 하승길;전준철;최의열
    • Korean Journal of Microbiology
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    • v.38 no.3
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    • pp.168-172
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    • 2002
  • Budding yeasts maintain an effective system to regulate intracellular pH in response to environmental pH fluctuation. In a previous study we reported that SHC1 plays a role in cell growth at alkaline condition, not at acid pH. We constructed a null mutant deleted an entire open reading frame for SHC1. To test whether the retardation in cell growth was caused by the absence of intracellular pH buffering capacity, we measured intracellular pH with a pH-sensitive fluorescent dye, C.SNARE. The intracellular pH of the mutant cell was much higher than that of wild-type cells, indicating that the mutant cells lack some types of buffering capacity. We also investigated the level of $Na^+ and K^+$ content with atomic mass spectroscopy after alkali shock. Wild-type cell showed a higher level of intracellular K^+$ content, whereas there was no difference in $Na^+$ level. The result suggested that K^+$ is more important in the regulation of intracellular pH in yeasts.

Gas Absorption and Release Properties of Zn(BH4)2 and MgH2-Zn(BH4)2-Ni-Ti-Fe Alloy

  • Kwak, Young Jun;Kwon, Sung Nam;Song, Myoung Youp
    • Korean Journal of Materials Research
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    • v.25 no.1
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    • pp.43-47
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    • 2015
  • $Zn(BH_4)_2$ was prepared by milling $ZnCl_2$ and $NaBH_4$ in a planetary ball mill in an Ar atmosphere, and XRD analysis, SEM observation, FT-IR analysis, DTA, and TGA were performed for synthesized $Zn(BH_4)_2$ samples. 90 wt% $MgH_2$+1.67 wt% $Zn(BH_4)_2(+NaCl)$+5 wt% Ni+1.67 wt% Ti+1.67 wt% Fe (named $90MgH_2+1.67Zn(BH_4)_2(+NaCl)$+5Ni+1.67Ti+1.67Fe) samples were also prepared by milling in a planetary ball mill in an $H_2$ atmosphere. The gas absorption and release properties of the $Zn(BH_4)_2(+NaCl)$ and $90MgH_2+1.67Zn(BH_4)_2(+NaCl)_2(+NaCl)$+5Ni+1.67Ti+1.67Fe samples were investigated. An FT-IR analysis showed that $Zn(BH_4)_2$ formed in the $Zn(BH_4)_2(+NaCl)$ samples prepared by milling $ZnCl_2$ and $NaBH_4$. At the first cycle at $320^{\circ}C$, $90MgH_2+1.67Zn(BH_4)_2(+NaCl)$+5Ni+1.67Ti+1.67Fe absorbed 2.95 wt% H for 2.5 min and 4.93 wt% H for 60 min under 12 bar $H_2$, and released 1.46 wt% H for 10 min and 4.57 wt% H for 60 min under 1.0 bar $H_2$.

Pharmaceutical Study on Clonixin Argininate (Clonixin Argininate의 약제학적 연구)

  • Jee, Ung-Kil;La, Sung-Bum
    • Journal of Pharmaceutical Investigation
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    • v.16 no.2
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    • pp.43-54
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    • 1986
  • To increase the bioavailability of clonixin, clonixin argininate was prepared and compared with clonixin by determining solubility, pKa, lipid-water partition coefficient, dissolution rate and in vivo tests. The results are summerized as followings; 1) The solubility of clonixin argininate was increased by 20 times in water, about 1.2 times in pH 1.2 and pH 8.0 buffer solution, and about 1.8 times in pH 6.8 buffer solution compared with that of clonixin. 2) pKa values of clonixin, clonixin lysinate and clonixin argininate were 6.32, 7.20 and 7.45, respectively. 3) The lipid-water partition coefficient of clonixin argininate was increased more than that of the clonixin in n-hexane, carbon tetrachloride, chloroform, methylene chloride, and n-butanol, but the partition coefficient of clonixin was increased more than that of clonixin argininate in benzene/pH 1.2 buffer solution, ether/pH 8.0 buffer solution, and 3-methylbutyl acetate/pH 1.2, pH 8.0 buffer solution. 4) The time required to dissolve 60% $(T_{60%},\;min.)$ of clonixin argininate was about 1.5 min. in water and pH 1.2 buffer solution, and about 5 min. in pH 6.8 buffer solution. $T_{60%}$ of clonixin lysinate was about 1.5 min. in water, about 1.8 min. in pH 6.8 buffer solution, and about 8 min. in pH 1.2 buffer solution. But $T_{60%}$ of clonixin was about 96 min. in pH 6.8 buffer solution, over 2 hours in water and pH 1.2 buffer solution. 5) Anti-inflammatory effect of clonixin argininate was increased more than that of clonixin over 6 hours, and that of clonixin lysinate was followed by lapse of time. 6) Analgesic effect of clonixin argininate was increased by 1.5 times more than that of clonixin and the effect of clonixin argininate was nearly identical with that of clonixin lysinate. 7) The absorption rates (Ka) of clonixin, clonixin lysinate and clonixin argininate were $0.169\;hr^{-1},\;0.652\;hr^{-1}$ and $0.723\;hr^{-1}$ in situ, respectively.

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Placental Transfer and Pharmacokinetics of a Single Oral Dose of the Fluoroquinolone Antibacterial DW-116 in Rats (랫드에서 fluoroquinolone 항균제 DW-116의 단회 경구투여에 의한 태반통과와 약물동태연구)

  • 김종춘;신호철;허정두;이종화;정문구;윤효인
    • Biomolecules & Therapeutics
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    • v.10 no.1
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    • pp.43-49
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    • 2002
  • The present study was conducted to investigate the placental transfer and pharmacokinetics of the flu-oroquinolone antibacterial DW-116 in pregnant rats. The placental transfer and pharmacokinetics of DW-116 were examined after a single oral dose of 500 mg $^{14}C$ DW-116/kg on gestational day 18. Maternal and fetal tissues were collected at 0.17 0.5,1,2,4,8, and 24 h after dosing. Maximum radioactivity was detected in maternal plasma, placenta, and whole fetus at 1 h, and in amniotic plasma at 4 h after dosing. Thereafter, radioactivity gradually disappeared from these tissues and was 16~28% of maximum levels at 24 h after dosing. Radioactivity in whole fetus were higher than those in the maternal plasma and placenta. The $T_{1/2,abs}$, $T_{1/2,{\beta}},$ AUC, $T_{max},$ and $C_{max}$ in the maternal plasma were approximately 6 min, 13.3 h, 1620 $ug^*hr/ml,$ 0.5 h, and 136 ug/ml, respectively. Those in the placenta were approximately 20 min, 12.3 h, 2150 $ug^*h/$m\ell$,$ 1.0 h, and 172 ug/ml, respectively. Those in the whole fetus were 13 min, 12.8 h,2549 $ug^*h/$m\ell$,$ 1 h, and 191 ug/ml, respectively. In the amniotic fluid of maternal uterus, the 4T_1/2,abs}$, $T1/2,{\beta},$ AUC, $T_{max},$ and $C_{max}$ were approximately 1.3 h,9.3 h,2508 $ug^*h/$m\ell$,$ 4.4 h, and 135 ug/ml, respectively. While DW-116 disappeared biphasically from maternal plasma, whole fetus and placenta, it was eliminated monophasically from amniotic fluid. In conclusion, this study demonstrated that the absorption and distribution of DW-116 in maternal plasma and placenta were extensively rapid, and that the test chemical well passed the blood-placenta barrier and was transferred to the fetus.

Development of $^1H-^{31}P$ Animal RF Coil for pH Measurement Using a Clinical MR Scanner (임상용 MR에서 pH 측정을 위한 동물 실험용 $^1H-^{31}P$ RF 코일 개발)

  • Kim, Eun Ju;Kim, Daehong;Lee, Sangwoo;Heo, Dan;Lee, Young Han;Suh, Jin-Suck
    • Investigative Magnetic Resonance Imaging
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    • v.18 no.1
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    • pp.52-58
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    • 2014
  • Purpose : To establish a pH measurement system for a mouse tumor study using a clinical scanner, to develop the $^1H$ and 31P radio frequency (RF) coil system and to test pH accuracy with phantoms. Materials and Methods: The $^1H$ and the $^{31}P$ surface coils were designed to acquire signals from mouse tumors. Two coils were positioned orthogonally for geometric decoupling. The pH values of various pH phantoms were calculated using the $^1H$ decoupled $^{31}P$ MR spectrum with the Henderson-Hasselbalch equation. The calculated pH value was compared to that of a pH meter. Results: The mutual coil coupling was shown in a standard $S_{12}$. Coil coupling ($S_{12}$) were -73.0 and -62.3 dB respectively. The signal-to-noise ratio (SNR) obtained from the homogeneous phantom $^1H$ image was greater than 300. The high resolution in vivo mice images were acquired using a $^{31}P$-decoupled $^1H$ coil. The pH values calculated from the $^1H$-decoupled $^{31}P$ spectrum correlated well with the values measured by pH meter ($R^2$=0.97). Conclusion: Accurate pH values can be acquired using a $^1H$-decoupled $^{31}P$ RF coil with a clinical scanner. This two-surface coil system could be applied to other nuclear MRS or MRI.