• Title/Summary/Keyword: Imidazole

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Synergistic Effect of Polygodial with Imidazole Drugs on the Antifungal Activity (천연물 Polygodial과 Imidazole계 화합물의 병용에 의한 항진균 활성의 증진)

  • 이상화;이재란;김창진
    • YAKHAK HOEJI
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    • v.43 no.2
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    • pp.221-227
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    • 1999
  • The fungistatic and fungicidal activities of amphotericin B, fluconazole, miconazole, econazole, and 5-fluorocytosine against Saccharomyces cerevisiae were estimated in the presence of 1/2 minimum inhibitory concentration (MIC) and 1/2 minimum fungicidal concentration (MFC) of polygodial, respectively. Among them, the antifungal activities of miconazoles by polygodial was still shown against several yeast-like fungi including Candida albicans, Candida utilis, Cryptococcus neoformans, except for Candida krusei. The combination of polygodial with imidazole drugs against Saccharomyces cerevisiae was further examined using the macrobroth dilution checkerboard method. The fractional inhibitory concentration (FIC) and the fractional fungicidal concentration (FFC) index between polygodial and miconazole were 0.16 and 0.19, while the combination of polygodial with econazole exhibited the FIC index of 0.19 and the FFC of 0.25, respectively. These results suggest that polygodial and the imidazoles on the fungistatic and fungicidal action are highly synergistic.

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Synthesis and Antiinflammatory Activity of 1.5- and 4.5-Disubstituted Imidazoles

  • Tuyen, Truong-Ngoc;Sin, Kwan-Seog;Kim, Hyun-Pyo;Park, Hae-Il
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.347.4-348
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    • 2002
  • Recently it has been demonstrated that selective cyclooxygenase-2 (COX-2) inhibitors retain the antiinflammatory effect but with markedly reduced GI toxicity compared to non selective inhibitors such as traditional NSAIDs. As a consequence, intense efforts have been made to develop selective COX-2 inhibtors during the last decade. Two compounds in this class. celecoxib and rofecoxib. are already in the market and are proved as potent and selective COX-2 inhibitors with much better gastric tolerance. However. there are still strong domands for a COX-2 inhibitor with improved efficacy and safety profiles. Here we report the synthesis and biological profiles of 1.5- and 4.5-disubstituted imidazole analogues as structural equivalents of cefecoxib and refecoxib. The imidazole analogues are overlapped well whth the 3D srructures of celecoxib and rofecoxib.

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Surface Analysis of LB Films and Monolayer for IMI-O Polymer (IMI-O 고분자의 단분자막과 LB막에 대한 표면분석)

  • Jung, Sang-Burm;Yoo, Seung-Yeop;Park, Jae-Chul;Kwon, Young-Soo
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2000.05b
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    • pp.265-268
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    • 2000
  • We fabricated an IMI-O polymer containing an imidazole group that could form a complex structure between the monolayer and the metal ions at the air-water interface. Also. the monolayer behavior at the air-water interface and the surface morphology of metal-complexed Langmuir-Blodgett(LB) films were investigated by using Brewster angle microscopy(BAM) and Scanning Maxwell-stress Microscopy(SMM). The difference in the BAM and SMM images between the pure water and the aqueous metal ions is attributed to the interactions of the copolymers with the metal ions at the interface and the consequent change of the monolayer organization.

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Acid and Base Catalyzed Intramolecular Cyclizations of N-Benzoylthiocarbamoyl-acetals

  • Lee, Bong-Yong;Kim, Choong-Sup;Lee, Jong-Wook
    • Archives of Pharmacal Research
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    • v.23 no.2
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    • pp.99-103
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    • 2000
  • Acid and base catalyzed intramolecular cyclizations of N-benzoylthioureidoacetal, contain-ing four functional groups adjacent to thiourea such as benzocarbamoyl, acetal, thioure and amide, were investigated. The condensation reaction of N-benzoyl thiocarbamoylgly-cine amide in the presence of 10% aqueous NaOH provided 1-(2,2-dimethoxy)ethyl-imi- dazolidine-2-thione exclusively. In the presence of pyridine, it was transformed to 2- thiohydantoin. N-Benzoyl thiocarbamoyl glycine amide was completely transformed to an iminothiazolidine exclusively in the presence of Lewis acid such as borontrifluoride ether-ate or trimethylsilyl iodide. 1-(2,2-Dimethoxy)ethyl-imidazolidine-2-thione was transformed to imidazole[2,1-b]thiazole and pyrazino[5,1-a]imidazole in the presence of $BF_3$.$ET_2$O and formic acid, respectively.

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Electronic Structure and Bonding Configuration of Histidine on Ge(100)

  • Lee, Han-Gil;Youn, Young-Sang;Yang, Se-Na;Jung, Soon-Jung;Kim, Se-Hun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3217-3220
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    • 2010
  • The electronic structures and bonding configuration of histidine on Ge(100) have been investigated with various sample treatments using core-level photoemission spectroscopy (CLPES). Interpretation of the Ge 3d, C 1s, N 1s, and O 1s core level spectra being included in these systems revealed that both the imino nitrogen in the imidazole ring and the carboxyl group in the glycine moiety concurrently participate in the adsorption of histidine on a Ge(100) surface at 380 K. Moreover, we could clearly confirm that the imino nitrogen with a free lone pair in the imidazole group adsorbs on Ge(100) more strongly than the carboxyl group in the glycine moiety by examining systems annealed at various temperatures.

An Efficient Synthesis of 2,4,5-Triaryl-1H-Imidazole Derivatives Catalyzed by Boric Acid in Aqueous Media Under Ultrasound-Irradiation

  • Shelke, Kiran F.;Sapkal, Suryakant;Sonal, Swapnil;Madje, Balaji R.;Shingate, Bapurao B.;Shingare, Murlidhar S.
    • Bulletin of the Korean Chemical Society
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    • v.30 no.5
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    • pp.1057-1060
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    • 2009
  • Boric acid ($BO_3H_3$) is an inexpensive, efficient and mild catalyst for the synthesis of 2,4,5-triaryl-1H-imidazoles in excellent yields from the one-pot three-component condensation of benzil/benzoin, an aldehydes and ammonium acetate in aqueous media under ultrasound at room temperature. The remarkable advantages offered by this method are green catalyst, mild reaction conditions, simple procedures, much faster reactions and excellent yield of products.

Convenient One-Pot Synthesis of 2,4,5-Triaryl-1H-imidazoles from Arylaldehydes, Benzyl Alcohols, or Benzyl Halides with HMDS in the Presence of Molecular Iodine

  • Veisi, Hojat;Khazaei, Ardashir;Heshmati, Leila;Hemmati, Saba
    • Bulletin of the Korean Chemical Society
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    • v.33 no.4
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    • pp.1231-1234
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    • 2012
  • A one-pot efficient procedure for the synthesis of 2,4,5-triaryl-1H-imidazole derivatives in good to excellent yields by reaction between hexamethyldisilazane and arylaldehydes, benzyl alcohols, benzyl halides in the presence of molecular iodine has been developed. The remarkable advantages of this method are the simple workup procedure, high yields of products, and the availability of reagents.

Synthesis and Biological Evaluation of 4-Heteroaryl-2-amino-5-methylimidazole Analogs as NHE-1 Inhibitors

  • Lee, Sun-Kyung;Yi, Kyu-Yang;Lee, Byung-Ho;Yoon, Boo-Soon
    • Bulletin of the Korean Chemical Society
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    • v.30 no.11
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    • pp.2621-2625
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    • 2009
  • To identify a non-acylguanidine NHE-1 inhibitor, an acylguanidne group was replaced with an imidazole group in the potent NHE-1 inhibitors with furan or benzothiphene core template, found from our previous studies. We synthesized and biologically evaluated 4-heteroaryl-2-amino-5-methylimidazole derivatives. All those imidazole compounds (16-18) represented the potent NHE-1 inhibitory activities, similar to the corresponding acylguanidine compounds.