• Title/Summary/Keyword: CH2150

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Comparative Activities of CH2150 and Sulbactam as ${\beta}$-Lactamase Inhibitors Against Escherichia coli and Staphylococcus Aureus Resistant to Ampicillin/Sulbactam (암피실린/설박탐에 내성을 갖는 대장균과 포도상구균에 대한 베타-락타메이즈 억제제 CH2150과 설박탐의 항균효과 비교)

  • Park, Su-Hyun;Kim, Hong-Jin;Kim, Ki-Ho
    • YAKHAK HOEJI
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    • v.41 no.1
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    • pp.126-131
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    • 1997
  • To overcome the problems of the resistance to clavulanic acid, many researchers are developing novel inhibitors that are not sensitive to new mutant ${\beta}$-lactamases. In order to evaluate newly synthesized compound CH2150 (Sodium (3S.5R)-6(Z)-[1-{1-(2-{2-benzoxazoly}thioethyl)-l.2,3-txiazol-4-yl}methylene] penicillanate-1,1-dioxide) as a ${\beta}$-lactamase inhibitor, we examined inhibitory activity of CH2150 against ${\beta}$-lactamases of clinical isolates resistant to ampicillin/sulbactam(12 strains of Escherichia coli and 13 strains of Staphylococcus aureus), and compared with that of sulbactam. Nitrocefin was used as substrate for ${\beta}$-lactamases, and the increase of absorbance was measured spectrophotometerically at 482 nm. ${\beta}$-Lactarnase inhibition of CH2150 against ${\beta}$-lactamases was 73 ~ 96% in E. coli and 76 ~ 79% in S. aureus. Comparatively, that of sulbactam was 96 ~ 100% and 96 ~ 100%, respectively. The inhibitory activity of CH2150 was slightly lower than that of sulbactam. The MIC values of ampicillin combined with CH2150 (2:1) for the clinical isolates were 4~512 ${\mu}$g/ml for E. coli and 1.0 ~ 64 ${\mu}$g/ml for S. aureus, whereas 0.5~16 ${\mu}$g/ml for E. coli and 0.25~8 ${\mu}$g/ml for S. aureus when combined with sulbactam (2:1).

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Comparison of the Activities of Novel ${\beta}$-Lactamase Inhibitors, 6-Exomethylene Penamsulfones, with Other ${\beta}$-Lactamase Inhibitors as Combined with ${\beta}$-Lactam Antibiotics (I) (6위치 엑소 메칠렌 치환 페남계 베타락타마제 억제제의 베타락탐항생제와 병용시 활성비교(I))

  • Park, Kye-Whan;Kim, Ki-Ho;Kim, Mee-Young;Im, Chae-Uk;Yim, Chul-Bu
    • YAKHAK HOEJI
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    • v.41 no.4
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    • pp.462-472
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    • 1997
  • In this approach, the antimicrobial activities of the compounds were compared with the ${\beta}$-lactam antibiotics against ${\beta}$-lactamase producing strains in vitro. Heteroc yclyl exomethylenepenam derivatives were several numbers of 6-exomethylenepenam sodiums (CH1240, CH1245, CH1250, CH2140, CH2145, CH2150). The inhibitory concentraion assay of six compounds were compared with clavulanic acid, sulbactam, tazobactam. Clavulanic acid, sulbactam and tazobactam are used as inhibitors of a variety of plasmid-mediated beta-lactamases. In vitro ${\beta}$-lactamase inhibitory assay, CH1240 and CH2140 were more active than clavulanic acid, sulbactam and tazobactam against ${\beta}$-lactamases overally. And in vitro comparative antimicrobial susceptibility test of six inhibitors were performed with mixed forms of ampicillin, cefotaxime, amoxicillin, ticarcillin, piperacillin, cefoperazone against ${\beta}$-lactamase producing 31 species strains. Consequently CH2140 and CH1240 among the six compounds enhanced the activity of the ${\beta}$-lactams for 31 ${\beta}$-lactamase producing strains.

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Synthesis and $\beta$-lactamase inhibitory activity of 6-exomethylene penamsulfone derivatives-IV (In Vitro Comparative Susceptibility test of 6-exomethylene penamsulfone derivatives)

  • Yim, Chul-Bu;Youm, Jeong-Rok;Im, Chae-Uk;Kim, Ki-Ho;Park, Kye-Whan
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.162-162
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    • 1996
  • 새로 합성된 6-exomethylene penamsulfone derivatives 7종에 대해 In Vitro antibacterial activities를 Broth Microdilution법으로 Sulbactam-Na(SAM), Clavulanic acid-K(CLA)와 Cefotaxime-Na(CFT), Ampicillin Trihydrates(AMP), Amoxicillin-Na(AMX), Cefoperazone(CFZ)을 병용투여하여 $\beta$-lactamase 생성 균주(30 여종)에 실시, MIC를 구하였다. 균주에 따라 SAM, CLA에 비해 CH1145, CH1155 등이 우수한 효과를, CH1140, CH2150등이 유사한 효과를 보였다.

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Self-Aggregation of Synthetic Magnesium Bacteriochlorins as a Photosynthetic Antenna Model

  • Kunieda, Michio;Mizoguchi, Tadashi;Tamiaki, Hitoshi
    • Journal of Photoscience
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    • v.9 no.2
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    • pp.353-355
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    • 2002
  • We prepared 3-(1-hydroxyethyl)-bacteriopyrochlorophy11-a (3) possessing magnesium atom and phytyl ester from modification of natural bacteriochlorophyll(BChl)-a. A dichloromethane solution of (3$^1$R) and (3$^1$S)-3 was diluted with 100~1000 fold volume of cyclohexane to give new species absorbing near-infrared lights. The resulting Q, maximum of (3$^1$R)-3 was 860 nm and red-shifted by 2150 $cm^{-1}$ / from the monomeric. In the nonpolar organic solvent, epimeric (3$^1$S)-3 showed a 1ess red-shifted peak at 798 nm as well as a residual monomeric band. Such visible spectra indicated that 3 diastereose1ectively aggregated in cyclohexane to afford oligomers possessing a simi1ar supramolecular structure with chlorosomal aggregates of natural BChl-d, 7,8-dehydro-form of 3.

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Distribution of Glutathione S-Transferase Omega Gene Polymorphism with Different Stages of HBV Infection Including Hepatocellular Carcinoma in the Egyptian Population

  • Shaban, Nadia Z;Salem, Halima H;Elsadany, Mohamed A;Ali, Bahy A;Hassona, Ehab M;Mogahed, Fayed AK
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.4
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    • pp.2145-2150
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    • 2016
  • Background: Infection with hepatitis B virus (HBV) is a major global public health problem, with a wide spectrum of clinical manifestations. Human cytosolic glutathione-S-transferases (GSTs) include several classes such as alpha (A), mu (M), pi (P), sigma (S), zeta (Z), omega (O) and theta (T). The present study aimed to investigate the role of GST omega genes (GSTO1 and GSTO2) in different groups of patients infected with HBV. Materials and Methods: HBV groups were classified according to clinical history, serological tests and histological analysis into normal carriers (N), acute (A), chronic (CH), cirrhosis (CI) and hepatocellular carcinoma (HCC) cases. The study focused on determination of the genotypes of GST omega genes (GSTO1 and GSTO2) and GST activity and liver function tests. Results: The results showed that GSTO1 (A/A) was decreased in N, A, CH, CI and HCC groups compared to the C-group, while, GSTO1 (C/A) and GSTO1(C/C) genotypes were increased significantly in N, A, CH, CI and HCC groups. GSTO2 (A/A) was decreased in all studied groups as compared to the C-group but GSTO2(A/G) and GSTO2(G/G) genotypes were increased significantly. In addition, GST activities, albumin and TP levels were decreased in all studied groups compared to the C-group, while the activities of transaminases were increased to differing degrees. Conclusions: The results indicate that GSTO genetic polymorphisms may be considered as biomarkers for determining and predicting the progression of HBV infection.