• Title/Summary/Keyword: benzimidazole

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Ultra High Molecular Weight Polyethylene Nanocomposite Films : Thermomechanical Property, Morphology, and Gas Permeability (초고분자량 폴리에틸렌 나노복합체 필름 : 열적-기계적 성질, 모폴로지 및 기체 투과도)

  • Jung, Min-Hye;Kim, Jeong-Cheol;Chang, Jin-Hae
    • Polymer(Korea)
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    • v.31 no.5
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    • pp.428-435
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    • 2007
  • The thermomechanical property, morphology, and gas permeability of nanocomposites of ultra high molecular weight polyethylene (UHMWPE) with two different organoclays are compared. Hexamethylene benzimidazole-mica ($C_{16}BIMD-Mica$) and Cloisite 25A were used as reinforcing fillers in the formation of UHMWPE hybrid films. Dispersions of organoclays with UHMWPE were carried out by using the solution intercalation method at different organoclay contents to produce nano-scale composites. Transmission electron microscopy (TEM) micrographs show that some of the clay layers are dispersed homogeneously within the polymer matrix on the nano-scale, although some clay particles are agglomerated. We also found that the addition of only a small amount of organoclay is enough to improve the thermomechanical property and gas barrier of the UHMWPE hybrid films. In general, Cloisite 25A is more effective than $C_{16}BIMD-Mica$ in increasing both the thermomechanical property and the gas barrier in a UHMWPE matrix.

A Solid-Contact Indium(III) Sensor based on a Thiosulfinate Ionophore Derived from Omeprazole

  • Abbas, Mohammad Nooredeen;Amer, Hend Samy
    • Bulletin of the Korean Chemical Society
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    • v.34 no.4
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    • pp.1153-1159
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    • 2013
  • A novel solid-contact indium(III)-selective sensor based on bis-(1H-benzimidazole-5-methoxy-2-[(4-methoxy-3, 5-dimethyl-1-pyridinyl) 2-methyl]) thiosulfinate, known as an omeprazole dimer (OD) and a neutral ionophore, was constructed, and its performance characteristics were evaluated. The sensor was prepared by applying a membrane cocktail containing the ionophore to a graphite rod pre-coated with polyethylene dioxythiophene (PEDOT) conducting polymer as the ion-to-electron transducer. The membrane contained 3.6% OD, 2.3% oleic acid (OA) and 62% dioctyl phthalate (DOP) as the solvent mediator in PVC and produced a good potentiometric response to indium(III) ions with a Nernstian slope of 19.09 mV/decade. The constructed sensor possessed a linear concentration range from $3{\times}10^{-7}$ to $1{\times}10^{-2}$ M and a lower detection limit (LDL) of $1{\times}10^{-7}$ M indium(III) over a pH range of 4.0-7.0. It also displayed a fast response time and good selectivity for indium(III) over several other ions. The sensor can be used for longer than three months without any considerable divergence in potential. The sensor was utilized for direct and flow injection potentiometric (FIP) determination of indium(III) in alloys. The parameters that control the flow injection method were optimized. Indium(III) was quantitatively recovered, and the results agreed with those obtained using atomic absorption spectrophotometry, as confirmed by the f and t values. The sensor was also utilized as an indicator electrode for the potentiometric titration of fluoride in the presence of chloride, bromide, iodide and thiocyanate ions using indium(III) nitrate as the titrant.

Improved On-off Property of SiO2 Embedded Polyfluorene Polymer-OLED (SiO2의 첨가를 통한 Polyfluorene계 Polymer-OLED의 발광 동작 개선 가능성)

  • Jeon, Byung Joo;Kim, Hyo Jun;Kim, Jong Su;Jeong, Yong Seok
    • Journal of the Semiconductor & Display Technology
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    • v.16 no.1
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    • pp.40-44
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    • 2017
  • The effect of weak dielectric silicone dioxide($SiO_2$) embedded in polyfluorene(PFO) emitting layer of polymer-based multi structure OLED was investigated. Indium tin oxide(ITO)/poly(3,4-ethylenedioxythiophene)-poly(styrenesulfonate) (PEDOT:PSS)/poly(9,9-di-n-octylfluorenyl-2,7-diyl)(PFO)/2,2,2"-(1,3,5-benzinetriyl)-tris(1-phenyl-1-H-benzimidazole) (TPBi)/aluminum(Al) structure OLED was fabricated by spin-coating method. Applied electric field causes some effect on $SiO_2$ in PFO layer. Thus, interaction between polymers and affected $SiO_2$ might generate electrical and luminance properties change. Experimental results, show the reduced threshold voltage of 6 V(from 23 V to 17 V). The maximum current density was rather increased from $71A/m^2$ to $610A/m^2$ and maximum brightness was also increased from $7.19cd/m^2$ to $41.03cd/m^2$, 9 and 6 times each. Additionally we obtained colour broadening result due to the increasing of blue-green band emission. Consequently we observed that electrical and luminance properties are enhanced by adding $SiO_2$ and identified the possibility of controlling the emission colour of OLED device according to colour broadening.

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Investigation of Degradation Mechanism of Rabeprazole with Solid State Pharmaceutical Excipients

  • Ren, Shan;Tran, Thao Truong-Dinh;Tran, Phuong Ha-Lien;Rhee, Yun-Seok;Lee, Beom-Jin
    • Journal of Pharmaceutical Investigation
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    • v.40 no.6
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    • pp.367-372
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    • 2010
  • Rabeprazole sodium (RPN) is known to be very unstable at acidic condition or some acidic pharmaceutical excipients such as acrylic acid polymer (carbomer 934) with carboxylic acids. Thus, degradation mechanism of binary blends of rabeprazole with pharmaceutical excipients in a solid state without using solvents at three different ratios (3:1, 1:1 and 1:3) was investigated using Fourier transform infrad (FTIR) spectroscopy. Alkalizer (MgO), neutral hydroxypropymethylcellulose (HPMC 4000) were also tested for comparison. The binary blends were stored under accelerated conditions ($40^{\circ}C$/75% relative humidity) for two weeks. The concentration of thioether rabeprazole from the binary blends with acidic carbomer 934 increased as the rabeprazole concentration decreased. In addition, the degradation half-life of rabeprazole as well as the relative peak area ratios obtained from FTIR spectra of S=O stretching at $1094.1\;cm^{-1}$ decreased consistently as the fraction of carbomer 934 increased due to its sensitivity between the basic benzimidazole nitrogen and carboxylic acid group of carbomer 934. The physical appearance also turned into strong brown color in the presence of carbomer 934. In contrast, there were no significant changes in the degradation kinetics of rabeprazole with MgO and HPMC 4000 in a solid state. This present study demonstrated that the solid-state compatibility test with the aid of HPLC chromatographic and FTIR spectral analyses could offer a valuable methodology to select suitable pharmaceutical excipients and to elucidate the degradation mechanism of RPN for drug formulations at the early formulation stages.

In silico Analysis on hERG Channel Blocking Effect of a Series of T-type Calcium Channel Blockers

  • Jang, Jae-Wan;Song, Chi-Man;Choi, Kee-Hyun;Cho, Yong-Seo;Baek, Du-Jong;Shin, Kye-Jung;Pae, Ae-Nim
    • Bulletin of the Korean Chemical Society
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    • v.32 no.1
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    • pp.251-262
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    • 2011
  • Human ether-a-go-go related gene (hERG) potassium channel blockade, an undesirable side effect which might cause sudden cardiac death, is one of the major concerns facing the pharmaceutical industry. The purpose of this study is to develop an in silico QSAR model which uncovers the structural parameters of T-type calcium channel blockers to reduce hERG blockade. Comparative molecular similarity indices analysis (CoMSIA) was conducted on a series of piperazine and benzimidazole derivatives bearing methyl 5-(ethyl(methyl)amino)-2-isopropyl-2-phenylpentanoate moieties, which was synthesized by our group. Three different alignment methods were applied to obtain a reliable model: ligand based alignment, pharmacophore based alignment, and receptor guided alignment. The CoMSIA model with receptor guided alignment yielded the best results : $r^2$ = 0.955, $q^2$ = 0.781, $r^2_{pred}$ = 0.758. The generated CoMSIA contour maps using electrostatic, hydrophobic, H-bond donor, and acceptor fields explain well the structural requirements for hERG nonblockers and also correlate with the lipophilic potential map of the hERG channel pore.

Dephosphorylation of Diphenyl-4-Nitrophenyl Phosphinate(DPNPIN) onto 2-Alkylbenzimidazolide Anion in TTABr Micellar Solution (TTABr 미셀 용액속에서 2-알킬벤즈이미다졸 음이온에 의해 추진되는 디페닐-4-니트로페닐 포스페네이트(DPNPIN)의 탈인산화반응)

  • Kim, Jeung-Bea
    • Journal of Environmental Science International
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    • v.24 no.8
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    • pp.981-992
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    • 2015
  • This study is mainly focused on micellar effect of tetradecyltrimethyl ammonium bromide(TTABr) solution including alkylbenzimidazole(R-BI) on dephosphorylation of diphenyl-4-nitrophenylphosphinate(DPNPIN) in carbonate buffer(pH 10.7). Dephosphorylation of DPNPIN is accelerated by $BI^{\Theta}$ ion in $10^2$ M Carbonate buffer(pH 10.7) of $4{\times}10^{-4}$ M TTABr solution up to 80 times as compared with the reaction in Carbonate buffer by no benzimidazole(BI) solution of TTABr. The value of pseudo first order rate constant($k_{\psi}$) of the reaction in TTABr solution reached a maximum rate constant increasing micelle concentration. The reaction mediated by $R-BI^{\Theta}$ in micellar solutions are obviously slower than those by $BI^{\Theta}$, and the reaction rate were decreased with increase of lengths of alkyl groups. It seems due to steric effect of alkyl groups of $R-BI^{\Theta}$ in Stern layer of micellar solution. The surfactant reagent, TTABr, strongly catalyzes the reaction of DPNPIN with R-BI and its anion($R-BI^{\Theta}$) in Carbonate buffer(pH 10.7). For example, $4{\times}10^{-4}$ M TTABr in $1{\times}10^{-4}$ M BI solution increase the rate constant($k_{\psi}=99.7{\times}10^{-4}1/sec$) of the dephosphorylation by a factor ca. 28, when compared with reaction($k_{\psi}=3.5{\times}10^{-4}1/sec$) in BI solution(without TTABr). And no TTABr solution, in BI solution increase the rate constant($k_{\psi}=3.5{\times}10^{-4}1/sec$) of the dephosphorylation by a factor ca. 39, when compared with reaction ($k_{\psi}=1.0{\times}10^{-5}1/sec$) in water solution(without BI).

Albendazole and Mebendazole as Anti-Parasitic and Anti-Cancer Agents: an Update

  • Chai, Jong-Yil;Jung, Bong-Kwang;Hong, Sung-Jong
    • Parasites, Hosts and Diseases
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    • v.59 no.3
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    • pp.189-225
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    • 2021
  • The use of albendazole and mebendazole, i.e., benzimidazole broad-spectrum anthelmintics, in treatment of parasitic infections, as well as cancers, is briefly reviewed. These drugs are known to block the microtubule systems of parasites and mammalian cells leading to inhibition of glucose uptake and transport and finally cell death. Eventually they exhibit ovicidal, larvicidal, and vermicidal effects on parasites, and tumoricidal effects on hosts. Albendazole and mebendazole are most frequently prescribed for treatment of intestinal nematode infections (ascariasis, hookworm infections, trichuriasis, strongyloidiasis, and enterobiasis) and can also be used for intestinal tapeworm infections (taeniases and hymenolepiasis). However, these drugs also exhibit considerable therapeutic effects against tissue nematode/cestode infections (visceral, ocular, neural, and cutaneous larva migrans, anisakiasis, trichinosis, hepatic and intestinal capillariasis, angiostrongyliasis, gnathostomiasis, gongylonemiasis, thelaziasis, dracunculiasis, cerebral and subcutaneous cysticercosis, and echinococcosis). Albendazole is also used for treatment of filarial infections (lymphatic filariasis, onchocerciasis, loiasis, mansonellosis, and dirofilariasis) alone or in combination with other drugs, such as ivermectin or diethylcarbamazine. Albendazole was tried even for treatment of trematode (fascioliasis, clonorchiasis, opisthorchiasis, and intestinal fluke infections) and protozoan infections (giardiasis, vaginal trichomoniasis, cryptosporidiosis, and microsporidiosis). These drugs are generally safe with few side effects; however, when they are used for prolonged time (>14-28 days) or even only 1 time, liver toxicity and other side reactions may occur. In hookworms, Trichuris trichiura, possibly Ascaris lumbricoides, Wuchereria bancrofti, and Giardia sp., there are emerging issues of drug resistance. It is of particular note that albendazole and mebendazole have been repositioned as promising anti-cancer drugs. These drugs have been shown to be active in vitro and in vivo (animals) against liver, lung, ovary, prostate, colorectal, breast, head and neck cancers, and melanoma. Two clinical reports for albendazole and 2 case reports for mebendazole have revealed promising effects of these drugs in human patients having variable types of cancers. However, because of the toxicity of albendazole, for example, neutropenia due to myelosuppression, if high doses are used for a prolonged time, mebendazole is currently more popularly used than albendazole in anti-cancer clinical trials.

Chemical Reactions in Surfactant Solution (I). Substituent Effects of 2-Alkylbenzimidazolide ions on Dephosphorylation in CTABr Solutions (계면활성제 용액속에서의 화학반응 (제1보). 미셀용액속에서의 탈인산화 반응에 미치는 2-알킬벤즈이미다졸음이온들의 치환기효과)

  • Young-Seuk Hong;Chan-Sik Park;Jung-Bae Kim
    • Journal of the Korean Chemical Society
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    • v.29 no.5
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    • pp.522-532
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    • 1985
  • The reactions of p-nitrophenyldiphenylphosphate (p-NPDPP) with anions of benzimidazole (BI) and its 2-alkyl derivatives (R-BI) are strongly catalyzed by the micelles of cetyltrimethyl ammonium bromide (CTABr). On the other hand, the first order rate constants $(k'_{R-BI^-})$ and the second order rate constants $(k_{m(R-BI^-)})$ of the reactions mediated by R-$BI^-$in the micellar pseudophase are much smaller than those mediated by $BI^-$. In order to explain the slower rates of the micellar reactions mediated by R-$BI^-$, we compared the concentration-ratios ([R-$BI^-$]/[$BI^-$]) with the first order rate constant-ratios $(k'_{R-BI^-}/k'_{BI^-})$ and the second order constant-ratios $(k_{m(R-BI^-)}/k_{m(BI^-)})$ for the reactions taking place in the micellar pseudophase. The rate constant-ratios were much smaller than the concentration-ratios. For example in a 5 ${\times}10^{-4}$M butyl-BI solution, the two ratios were 0.089 and 0.430 (for the first order) respectively, and in a $10^{-4}$M butyl-BI solution the former was 0.100 (for the second order). This predicts that the reactivities of R-$BI^-$ in the micellar pseudophase are much smaller than that of $BI^-$. Based on the values of several kinetic parameters measured for dephosphorylation of p-NPDPP mediated by R-$BI^-$, a schemetic model is proposed. Due to the hydrophobicity and the steric effect of the alkyl substituents, these groups would penetrate into the core of the micelle for stabilization by van der Waals interaction with long cetyl groups of CTABr. Consequently, the movements of R-$BI^-$ bound to the micelle should be restricted, leading to decreased collison frequencies between the nucleophiles and p-NPDPP. We refer this as an "anchor effect". This effect became more predominent when a larger alky group in R-BI was employed and when a greater concentration of R-BI was used.

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Control Effects of Several Fungicides on Jujube Anthracnose and Fungicide Resistance Monitoring (몇 종류 살균제의 대추 탄저병균에 대한 방제효과 및 살균제 저항성 모니터링)

  • Lee, Kyeong Hee;Choi, Jiyoung;Park, Subin;Kim, Heung Tae
    • Research in Plant Disease
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    • v.25 no.4
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    • pp.188-195
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    • 2019
  • Among 6 fungicides, fluazinam, which had an excellent inhibitory effect on mycelial growth and spore germination, was also effective in controlling jujube anthracnose in the field. While EC50 values of metconazole and tebuconazole ranged from 0.2 to 0.9 ㎍/ml and from 0.4 to 1.1 ㎍/ml against the mycelial growth, respectively, each inhibitory effect on spore germination was low by 7.4% and 11.1% at 50.0 ㎍/ml. In the field test, they showed the control value of 80.5% and 77.0%, respectively. The protective fungicides, as mancozeb and folpet, which had a low inhibitory effect on the mycelial growth, but had a high inhibitory effect of spore germination, showed excellent disease control activities by 87.6% and 92.0% in the field. Showing a result of resistance monitoring conducted with the isolates of Colletotricum gloeosporioides, the resistance against carbendazim was already generated in the field, but it was thought that there was no resistance to pyraclostrobin, fluazinam and tebuconazole. However, if the resistance factor value of the population of C. gloeosporioides isolates to pyraclostrobin was high by 160.4, the diversity of the response to the fungicide in the population was high, so it should be taken more attention to the resistance management.

Poly(ethylene terephthalate) Nanocomposite Fibers with Thermally Stable Organoclays (내열성 유기화 점토를 이용한 폴리(에틸렌 테레프탈레이트) 나노복합체 섬유)

  • Jung, Min-Hye;Chang, Jin-Hae
    • Polymer(Korea)
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    • v.31 no.6
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    • pp.518-525
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    • 2007
  • The thermomechanical properties and morphologies of nanocomposite fibers of poly(ethylene terephthalate)(PET) incorporating thermally stable organoclays are compared. Dodecyltriphenyl-phosphonium-mica($C_{12}PPh-Mica$) and 1-hexadecane benzimidazole-mica ($C_{16}BIMD-Mica$) were used as reinforcing fillers in the fabrication of PET hybrid fibers. Dispersions of organoclays with PET were studied by using the in-situ polymerization method at various organoclay contents to produce nano-scale composites. The thermo-mechanical properties and morphologies of the PET hybrid fibers were determined using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), wide angle X-ray diffraction (XRD), electron microscopy (SEM and TEM), and a universal tensile machine (UTM). Transmission electron microscopy (TEM) micrographs show that some of the clay layers are dispersed homogeneously within the polymer matrix on the nano-scale, although some clay particles are agglomerated. We also found that the addition of only a small amount of organoclay is enough to improve the thermal stabilities and mechanical properties of the PET nanocomposite fibers. Even polymers with low organoclay content (<5 wt%) were found to exhibit much higher thermo-mechanical values than pure PET fibers.