• Title/Summary/Keyword: Thiazole

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Anthelmintic Efficacy of Tetramisole Against Experimental Infection of Swine Lungworm, Metastrongylus Apri (Tetramisole에 의한 돈폐충(豚肺蟲)(Metastrongylus apri) 구충(驅蟲) 효과(效果)에 대(對)하여)

  • Lee, Byung Do;Kim, Chin Bok
    • Korean Journal of Veterinary Research
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    • v.8 no.1
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    • pp.11-17
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    • 1968
  • Oral and subcutaneous administration of Tetramisole (d1-2, 3, 5, 6-tetrahydro-6-phenyl-imidazo- 2, 1-b thiazole hydrochloride) was effective in controlling the adult and immature forms of Metastrongylus apri in pigs when administered at the dose of 10-12.5 mg per kg of body weight.

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Inhibition of glutamate dehydrogenase and insulin secretion by KHG26377 does not involve ADP-ribosylation by SIRT4 or deacetylation by SIRT3

  • Kim, Eun-A;Yang, Seung-Ju;Choi, Soo-Young;Lee, Woo-Je;Cho, Sung-Woo
    • BMB Reports
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    • v.45 no.8
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    • pp.458-463
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    • 2012
  • We investigated the mechanisms involved in KHG26377 regulation of glutamate dehydrogenase (GDH) activity, focusing on the roles of SIRT4 and SIRT3. Intraperitoneal injection of mice with KHG26377 reduced GDH activity with concomitant repression of glucose-induced insulin secretion. Consistent with their known functions, SIRT4 ribosylated GDH and reduced its activity, and SIRT3 deacetylated GDH, increasing its activity. However, KHG26377 did not affect SIRT4-mediated ADP-ribosylation/inhibition or SIRT3-mediated deacetylation/activation of GDH. KHG26377 had no effect on SIRT4 protein levels, and did not alter total GDH, acetylated GDH, or SIRT3 protein levels in pancreatic mitochondrial lysates. These results suggest that the mechanism by which KHG26377 inhibits GDH activity and insulin secretion does not involve ADP-ribosylation of GDH by SIRT4 or deacetylation of GDH by SIRT3.

Evaluation on the Biodegradability of the MBT Wastewater (MBT 폐수의 생분해성 평가)

  • Lim, Ji-Young;Park, Jung-hwan;Kim, Jin-Han
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.17 no.3
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    • pp.86-92
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    • 2016
  • The possibility of the biological treatment of MBT wastewater generated from the vulcanization accelerator manufacturing process was investigated. MBT wastewater is not biodegradable because it hinders the activity of microorganisms, and approximately 10% of the total COD can be removed after a 7 day acclimation period. The optimal conditions of the MBT wastewater for the chemical pre-treatment was pH of 3.5 and the Fenton oxidation with the addition of $Fe^{3+}$ to the wastewater after agitation for 2 hours. The Fenton-treated MBT wastewater showed approximately 20% removal of COD when treated with the activated sludge process for the mixed paper wastewater and Fenton treated wastewater.

Biotransformation of a Fungicide Ethaboxam by Soil Fungus Cunninghamella elegans

  • PARK, MI-KYUNG;KWANG-HYEON LIU;YOONGHO LIM;YOUN-HYUNG LEE;HOR-GIL HUR;JEONG-HAN KIM
    • Journal of Microbiology and Biotechnology
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    • v.13 no.1
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    • pp.43-49
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    • 2003
  • Metabolism of a new fungicide ethaboxam by soil fungi was studied. Among the fungi tested, Cunninghamelia elegans produced metabolites from ethaboxam, which were not found in the control experiments. M5, a major metabolite from ethaboxam was firmly identified as N-deethylated ethaboxam by LC/MS/MS and NMR. N-Deethylated ethaboxam has been found as a single metabolite in in vitro metabolism with rat liver microsomes. Ml was proved to be 4-ethyl-2-(ethylamino)-1,3-thiazole-5-carboxamide (ETC) by comparing with the authentic compound. In addition, M2, M3, and M4, and M6 were tentatively Identified by LC/MS/MS as hydroxylated and methoxylated ethaboxams, respectively. Production of the major metabolite, N-deethylated ethaboxam, by the fungus suggested that C. elegans would be an efficient eukaryotic microbial candidate for evaluating xenobiotic-driven mammalian risk assessment.

Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

  • Fathalla, O.A.;Zaghary, W.A.;Radwan, H.H.;Awad, S.M.;Mohamed, M.S.
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.258-269
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    • 2002
  • 2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

Analysis of Volatiles in Sesame Oil Collected by Simultaneous Distillation/Extraction(SDE) and Dynamic Headspace Sampling (DHS) (연속수증기증류법(SDE)과 동적헤드스페이스법(DHS)에 의한 참기름 중의 향기성분의 분석)

  • Ha, Jaeho
    • Analytical Science and Technology
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    • v.9 no.4
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    • pp.399-405
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    • 1996
  • The flavor compounds of the oil from roasted sesame seeds were collected by simultaneous steam distillation/ extraction(SDE) and dynamic headspace sampling(DHS) and were analyzed using a gas chromatograph equipped with a flame ionization detector and connected into a mass spectrometer. Among the flavor compounds collected by the SDE method, 46 compounds were identified. They consisted of 6 alcohols, 6 aldehydes, 5 ketones or acids, 4 furans or phenols, 12 pyrazines, 4 pyridines or thiazoles, and others. Thirty six compounds were identified by DHS and many of them were the same as those identified by the SDE method. However, some compounds such as 1-hexanol, pentanal, and dimethylsulfide were identified only by the DHS method.

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Synthesis of New 2,4-Disubstituted Thiazoles and 2-(Allylidenehydrazono)-thiazolo[5,4-b]quinoxaline Derivatives (새로운 2,4-이치환된 티아졸들과 2-(Allylidenehydrazono)-thiazolo[5,4-b]quinoxaline 유도체들의 합성)

  • Kim, Jong-Geun;Bae, Sun Kun
    • Applied Chemistry for Engineering
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    • v.20 no.2
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    • pp.134-139
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    • 2009
  • A series of allylidenethiosemicarbazone compounds (2a~2e) were obtained in 45~85% by condensing (E)-3-(aryl)acrylaldehyde (1a~1e) with thiosemicarbazide. Theses compounds on treatment of 2,4'-dibromoacetophenone and 2,3-dichloroquinoxaline yielded 2,4-disubstituted thiazoles (3a~3e) and 2-[(E)-3-(aryl)allylidenehydrazono]thiazolo[5,4-b]quinoxaline (4a~4e) in good yield respectively. The structures of all the newly synthesized compounds were identified by IR and $^1H-NMR$ spectral data.

Synthetic Studies on Penems and Carbapenems (VII). Compounds Derived by Cleavage of the $\beta$-Lactam Ring during (Alkylthio) thiocarbonylation of a 4-Mercapto-3-phenylacetamidoazetidin-2-one Derivative (Penems와 Carbapenems의 합성에 관한 연구 (제 7 보) 4-mercapto-3-phenylacetamidoazetidin-2-one 유도체의 (알킬티오) 티오카르보닐화 과정 중 $\beta$-lactam 고리가 절단되어 생성된 화합물들)

  • Han Cheol Wang;Youn Young Lee;Yang Mo Goo;Kyoo Hyun Chung
    • Journal of the Korean Chemical Society
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    • v.33 no.5
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    • pp.545-550
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    • 1989
  • When (3R,4R)-1-(1-benzyloxycarbonyl-2-methyl-1-propenyl)-4-mercapto-3-phenylacetamidoazetidin-2-one(8) was reacted with carbon disulfide and alkyl halides in the presence of triethylamine, the ${\beta}$-lactam ring was cleaved to give (Z)-and (E)-1-alkylthio-5-benzyloxycarbonyl-6-methyl-2-phenylacetamido-4-aza-1,5-heptadien-3-one (13-16) or 2-benzyl-4-(3-benzyloxycarbonyl-4-methyl-1-oxo-2-aza-3-pentenyl)thiazole(17).

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Synthesis of New Uraci1-5-Sulphonamide-p-Phenyl Derivatives and Their Effect on Biomphalaria alexandrina Snail's Nucleoproteins

  • Fathalla, O.A.;Gad, H.S.M.;Maghaby, A.S.
    • Archives of Pharmacal Research
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    • v.23 no.2
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    • pp.128-138
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    • 2000
  • In continuation of the previous work (Fathalla, 1992) on the synthesis of some heterocycles containing uracil moiety, we report herein the incorporation of uracil moiety into cyan-opyridine thione, thiosemecarbazone, semicarbazone, cyanopyridine, ami nocyano pyridine, isoxazoline, pyrazoline, pyrimidine, triazolo pyrimidine, pyran, selena and thiazole derivatives which might modify their biological activities. The biological studies revealed that the chemical compound III f showed high molluscicdal activity than other compounds. The profile of the nucleoprotein extracted from chemically (compound IIIc, e, f and g) treated or UV-irradiated B.alexandrina snails did not show appreciable differences when compared to non-treated (native) snails by using SDS-PAGE, where no obvious qualitative or quantitative differences were observed. Immunization of experimental animals with the nucleoprotein extracted from native, chemically (compound III f & g) treated or physically treated B.alexandrina snails induced significant protection against challenge with normal S.mansoni cercariae, as compared to the non-immunized challenged control. As well as , a decrease in the number of granuloma formation and the size range of granuloma was also observed in immunized animals. It is concluded that, compounds III f and g have a potent molluscicidal activity. They also induced chemical modification comparable to that induced by physical treatment in the snail's nucleoprotein, which could possibly be used in immunization against S. mansoni infection.

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Studies on the Characteristics of Humic Acid and Its Utilization (V). Manufacturing of Sulfur-dyes from Humic Acid (土炭흄산의 性狀 및 應用에 關한 硏究(第 5 報). 황化染料 製造)

  • Han Kyoungsuk;Kim Wontaik
    • Journal of the Korean Chemical Society
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    • v.19 no.1
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    • pp.65-70
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    • 1975
  • Sulfur-dyes were manufactured from humic acid, $Na_2S_{2~3}$ and other additives at $200{\sim}250^{\circ}C$ for 3∼20 hrs. Sulfur-dyes from humic acid were fundamentally brown colors and could be changed from yellowish to grayish brown according to the additives. The colorfastness to rubbing and laundering were excellent but to weather was fair. Characteristic bonds of sulfur-dyes such as -C-S-C, -C-SO-C-. -C-$SO_2$-C-, and -C-O-$SO_2$-O-C- were confirmed but thiazole bond and thiazine ring were not done by IR-spectroscopy.

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