• Title/Summary/Keyword: benzimidazole

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Adsorption of methyl 2-benzimidazole carbamate on clay minerals (점토광물(粘土鑛物)에 의(依)한 methyl 2-benzimidazole carbamate의 흡착(吸着))

  • Kim, Bark-Jung;Park, Man;Hur, Nam-Ho;Choi, Jung
    • Applied Biological Chemistry
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    • v.34 no.2
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    • pp.125-129
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    • 1991
  • This experiment was carried out to examine the MBC adsorption on clay minerals by the slurry method. The adsorption of MBC on Kaolinite nearly reached equilibrium after shaking lot 2hrs. but on Bentonite and Zeolite, 10hrs., respectively. The adsorption amount was in the order of Zeolite>Bentonite>Kaolinite, and Na-saturated clay mineral adsorbed more MBC than Mg-saturated clay mineral did. The more the amount of clay minerals, the more MBC was adsorbed by clay minerals, whereas the amount of MBC adsorbed per unit gram of clay minerals reduced and Kd value cf MBC was greatest on the Na-Zeolite. The lower the pH of the water-clay system at each concentration, the more MBC was adsorbed by clay minerals. The pH dependence of the adsorption of MBC may be due to protonation of MBC in acid solution.

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Chemical Reactions in Surfactant Solutions(Ⅲ). Nucleophilic and Micellar Catalyses on Hydrolysis of an Organic Phosphate by Sodium 2-Alkylbenzimidazole-5-sulfonates in Aqueous and CTABr Solutions (계면활성제 용액속에서의 화학반응(제3보) 유기인산 에스테르의 가수분해반응에 미치는 2-알킬벤즈이미다졸-5-술포네이트의 친핵적 및 미셀 촉매효과)

  • Hong, Yeong Seok;Park, Hui Hyeon;Park, Han Seok
    • Journal of the Korean Chemical Society
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    • v.34 no.6
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    • pp.629-636
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    • 1990
  • Dephosphorylation of p-nitrophenyldiphenylphosphate(p-NPDPP) mediated by anions of sodium 2-alkylbenzimidazole-5-sulfonate(R-BI-SO$_3$Na) in CTABr micellar solutions are obviously slower than that by anion of sodium benzimidazole-5-sulfonate(BI-SO$_3$Na), and the reation rates were decreased with increase of lengths of alkyl groups. This presents a striking contrast to the reactions in aqueous solutions without added CTABr, of which the reaction rates are on approximately same levels. It seems due to steric effect of alkyl groups of R-BI$^-$SO$_3$Na in the Stern layer of micelle, and it is supported by measured activation parameters(△H$^\neq$/TEX>, △G$^\neq$/TEX> and △S$^\neq$/TEX>) of the reactions in aqueous and micellar solutions. In addition to nucleophilic ability of benzimidazole moiety of R-BI$^-$SO$_3$Na on the reactions, these compounds with long alkyl groups(nonyl to pentadecyl) are micellized for themseleves, and increase the reaction rates due to their micellar catalyses in aqueous solutions, not including CTABr.

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MeBib Suppressed Methamphetamine Self-Administration Response via Inhibition of BDNF/ERK/CREB Signal Pathway in the Hippocampus

  • Kim, Buyun;Jha, Sonam;Seo, Ji Hae;Jeong, Chul-Ho;Lee, Sooyeun;Lee, Sangkil;Seo, Young Ho;Park, Byoungduck
    • Biomolecules & Therapeutics
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    • v.28 no.6
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    • pp.519-526
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    • 2020
  • Methamphetamine (MA) is one of the most commonly abused drugs in the world by illegal drug users. Addiction to MA is a serious public health problem and effective therapies do not exist to date. It has also been reported that behavior induced by psychostimulants such as MA is related to histone deacetylase (HDAC). MeBib is an HDAC6 inhibitor derived from a benzimidazole scaffold. Many benzimidazole-containing compounds exhibit a wide range of pharmacological activity. In this study, we investigated whether HDAC6 inhibitor MeBib modulates the behavioral response in MA self-administered rats. Our results demonstrated that the number of active lever presses in MA self-administered rats was reduced by pretreatment with MeBib. In the hippocampus of rats, we also found MA administration promotes GluN2B, an NMDA receptor subunit, expression, which results in sequential activation of ERK/CREB/BDNF pathway, however, MeBib abrogated it. Collectively, we suggest that MeBib prevents the MA seeking response induced by MA administration and therefore, represents a potent candidate as an MA addiction inhibitor.

Changes in Sensitivity Levels of Botrytis cinerea Populations to Benzimidazole, Dicarboximide, and N-Phenylcarbamate Fungicides (잿빛곰팡이병균(Botrytis cinerea)의 Benzimidazole계, Dicarboximide계 및 N-phenylcarbamate계 살균제에 대한 감수성 변화)

  • 김병섭;박은우;조광연
    • Korean Journal Plant Pathology
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    • v.14 no.6
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    • pp.693-699
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    • 1998
  • Three three hundred and ninety seven isolates of Botrytis cinerea were isolated from infected plants of strawberry, tomato and cucumber from several areas in Korea during 1994∼1996 and the resistance of these isolates against some fungicides were examined. The isolation frequency of phenotypes resistant to carbendazim, procymidone, and diethofencarb were found to be 69.9 43.7, and 31.8%, respectively. The isolates were divided into six phenotypic groups; SSR, SRR, RSS, RRS, RSR and RRR, representing sensitive (S) or resistant (R) to benzimidazole, dicarboximide, and N-phenylcarbamate fungicides in order. The percentage of six phenotypes were 28.2, 2.0, 27.2, 41.0, 0.9 and 0.8%, respectively. On the basis of the mycelial growth inhibition (%) B. cinerea isolates were divided into three classes (class 1; 0∼50%, class 2; 51-99%, class 3; 100% inhibition) on carbendazim and three classes (class 1; 0∼75%, class 2; 76∼99%, class 3; 100% inhibition) on procymidone and the mixture of carbendazim+diethofencarb, respectively. Changes in sensitivity levles to carbendazim and carbendazim+diethofencarb were affected by introduction and increasing ratio of the use of diethofencarb.

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A Simple Benzimidazole Based Fluorescent Sensor for Ratiometric Recognition of Zn2+ in Water

  • Zhong, Keli;Cai, Mingjun;Hou, Shuhua;Bian, Yanjiang;Tang, Lijun
    • Bulletin of the Korean Chemical Society
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    • v.35 no.2
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    • pp.489-493
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    • 2014
  • A phenylbenzimidazole derivatized sensor (L) that behaves as a ratiometric fluorescent receptor for $Zn^{2+}$ in water has been described. In HEPES buffer at pH 7.4, sensor L displays a weak fluorescence emission band at 367 nm. Upon addition of $Zn^{2+}$, the emission intensity at 367 nm is decreased, concomitantly, a new emission band centered at 426 nm is developed, thus facilitates a ratiometric $Zn^{2+}$ sensing behavior. Sensor L binds $Zn^{2+}$ through a 1:1 binding stoichiometry with high selectivity over other metal cations. Sensor L displays a linear response to $Zn^{2+}$ concentration from 0 to $6.0{\times}10^{-5}M$, sensor L also exhibits high sensitivity to $Zn^{2+}$ with a detection limit of $3.31{\times}10^{-7}M$.

Synthesis, Characterization and Catalytic Application of MoO3/CeO2-ZrO2 Solid Heterogeneous Catalyst for the Synthesis of Benzimidazole Derivatives

  • Rathod, Sandip B.;Lande, Machhindra K.;Arbad, Balasaheb R.
    • Bulletin of the Korean Chemical Society
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    • v.31 no.10
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    • pp.2835-2840
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    • 2010
  • A series of $MoO_3/CeO_2-ZrO_2$ catalysts with different Mo content (8 - 20 wt %) were prepared by simple co-precipitation followed by impregnation method and were characterized by X-ray diffraction (XRD), infrared spectroscopy (IR), scanning electron microscopy (SEM), energy dispersive spectroscopic (EDS) techniques. The prepared materials were tested for catalytic activity by the synthesis of benzimidazole derivatives using condensation of aromatic aldehydes and o-phenylenediamine by conventional and microwave method. Obtained results reveal that the catalytic activity increases with increase in Mo wt % loading. The best catalytic activity was obtained with 20 wt % $MoO_3/CeO_2-ZrO_2$. The particle size or crystallite size was estimated using Debye-Scherrer equation. After completion of reaction, the catalyst can be recovered efficiently and reused with consistent activity.

Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives

  • Nevade, Sidram A.;Lokapure, Sachin G.;Kalyane, Navanath V.
    • Journal of the Korean Chemical Society
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    • v.57 no.6
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    • pp.755-760
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    • 2013
  • The present study is synthesis of derivatives of N'-(4-amino-5-sulfanyl-4H-1,2,4-triazole-3-yl)-2-(1H-benzimidazole-2-ylsulfanyl) acetohydrazide (IV). Antibacterial activity tested against the E. coli and A. Substilis. Biological activities conducted by disc diffusion method. Compound $2MB_1$, $2MB_3$, $2MB_5$ inhibit the appreciable microbial growth while rest of the compound possess the moderate activities. Anti-inflammatory activity tested by reduces local edema induced in the rat paw by injection of phlogestic agent. Compound $2MB_1$, $2MB_8$, $2MB_5$, $2MB_3$ and $2MB_6$ exhibit satisfying anti-inflammatory activity while analgesic activity conducted by acetic acid induced writhing effect in mice while compound $2MB_1$, $2MB_4$ and $2MB_7$ having the good analgesic activity. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and mass spectral data.

Involvement of reactive oxygen species in the anti-cancer activity of fenbendazole, a benzimidazole anthelmintic (Fenbendazole의 항암활성에서 활성산소종의 관련성)

  • Han, Yong;Joo, Hong-Gu
    • Korean Journal of Veterinary Research
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    • v.60 no.2
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    • pp.79-83
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    • 2020
  • Fenbendazole (FBZ) is a benzimidazole anthelmintic that has been widely used in treatments for gastrointestinal parasites including pinworms and roundworms in animals. Recently, some studies demonstrated that FBZ has anti-cancer effects related to disruption of microtubule polymerization. In this study, we investigated whether FBZ has anti-cancer activity in HL-60 cells, a human leukemia cell line, and assessed its relationship with the production of reactive oxygen species (ROS). FBZ treatment at 0.25-1 μM significantly decreased the metabolic activity of HL-60 cells. The mitochondrial membrane potential of FBZ-treated HL-60 cells decreased in a concentration-dependent manner. Apoptosis analysis using annexin V-FITC/propidium iodide staining demonstrated that 1 μM FBZ increased the percentages of cells in apoptosis and necrosis. In addition, Hoechst 33342 staining showed the presence of broken nuclei in HL-60 cells treated with 0.5 and 1 μM FBZ. To investigate the anti-cancer mechanism of FBZ, HL-60 cells were treated with FBZ in the absence or presence of N-acetyl cysteine (NAC), an inhibitor of ROS production. NAC significantly recovered the decreased metabolic activity of HL-60 induced by 0.5 and 1 μM FBZ treatments. This study provides evidence that FBZ has anti-cancer activity in HL-60 cells provided, in part, via ROS production.