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Synthesis of Some Novel N7-tetrazolo[5,1-f]-1,2,4-triazin-8-(7H)-one Compounds as Potential Antimicrobial Agents

  • El-Badry, Susan M.;Taha, Mamdouh A.M.
    • Journal of the Korean Chemical Society
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    • v.58 no.4
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    • pp.381-387
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    • 2014
  • A series of new $N^7$-tetrazolo[5,1-f ]-1,2,4-triazin-8-(7H)-one derivatives 4-16 were designed and synthesized from 3 with different reagents. The newly prepared compounds were characterized by spectral data and screened for their antimicrobial activities against various bacteria and fungi strains.

One Pot Synthesis of Bioactive Novel Cyanopyridones

  • Khokhani, Kamlesh;Khatri, Taslimahemad;Patel, Praful
    • Journal of the Korean Chemical Society
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    • v.57 no.4
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    • pp.476-482
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    • 2013
  • Cyanopyridone was prepared by the condensation of cyanoacetamide, substituted arylaldehydes and malononitrile in presence of pipyridine. The structure of the synthesized compound CP 1-20 was assigned on the basis of elemental analysis, IR, $^1H$-NMR and mass spectroscopy. These compounds were also screened for antimicrobial activity. The Minimum Inhibitory Concentration (MIC) of all the synthesized compounds was compared with standard drugs.

Synthesis and Antimicrobial Activity of Glycyl Norfloxacin Derivatives (Glycyl Norfloxacin 유도체의 합성과 항균작용)

  • 이현수;임채욱;임철부
    • YAKHAK HOEJI
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    • v.43 no.4
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    • pp.442-446
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    • 1999
  • The synthesis and antimicrobial activity of N-substituted glycyl derivatives of Norfloxacin were described. Norfloxacin was treated with chloroacetyl chloride to yield chloroacetyl norfloxacin (1). This compounds was treated with alkylamines to obtain quinolone carboxylic acids (2-6), which were reacted with pivaloyloxymethyl chloride to get pivaloyloxymethyl quinolone carboxylates (7-11). Free carboxylic quinolones (2-6) showed little stronger activities to their pivaloyloxymethyl esters (7-11). In quinolone analogues, longer alkyl chain compounds showed stronger activities than shorter one.

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Purification of Antimicrobial Substance for the Extract from the Root Bark of Morus alba (상백피 추출물로부터 향균성 물질의 분리정제)

  • 박욱연;김신희;김지회;김용관;장동석
    • Journal of Food Hygiene and Safety
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    • v.10 no.4
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    • pp.225.1-230
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    • 1995
  • The ethanol extract from the root bark of Morus alba showed the strongest antimicrobial activity on the growth of almost all the tested microorganisms which were food-borne pathogens and food-related microorganisms. 1) In order to isolate and purify of antimicrobial substance extracted from the root bark of Morus alba, the antimicrobial substance from the ethanol extract which exhibited a strong antimicrobial activity was purified by solvent fractionation, silica gel column chromatography, TLC and HPLC. Among the fractions fractionated by 4 kind of solvents from the ethanol extract, the antimicrobial activity of ethyl acetate fraction had the strongest antimicrobial activity against B. subtilis. Unknown compound were isolated from the ethyl acetate fraction by silica gel column chromatography, TLC and HPLC and the compounds showed strong absorbance at 207, 217 and 285 nm, therefore, it was supposed to be a kinds of aromatic compound.

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Antimicrobial Activity of Newly Synthesized 2,5-Disubstituted 1,3,4-Thiadiaozle Derivatives

  • Ramiz, Mahmoud M.M.;Abdel-Rahman, Adel A.H.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.12
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    • pp.4227-4232
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    • 2011
  • A number of new 2,5-disubstituted 1,3,4-thiadiazole and their S- or N-substituted derivatives as well as the corresponding sugar hydrazone derivatives were synthesized and tested for their antimicrobial activity against Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes). The synthesized compounds displayed different degrees of antimicrobial activities or inhibitory actions.

Synthesis and In-vitro Activity of Some New Class of Thiazolidinone and Their Arylidene Derivatives

  • Seelam, Nareshvarma;Shrivastava, S.P.
    • Bulletin of the Korean Chemical Society
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    • v.32 no.11
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    • pp.3996-4000
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    • 2011
  • In an attempt to find a new class of anti microbial agents, a series of thiazolidinone and their 5-arylidene derivatives containing 4-(4-methyl benzamido)-benzoyl moiety were synthesized via the reaction of benzocaine with appropriate chemical reagents. These compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Bacillus thuringiensis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and antifungal activity against Botrytis fabae, Fusarium oxysporan and Candida albicans. On the other hand the synthesized compounds were also screened for their anti tubercular activity. IR, $^1H$ NMR, $^{13}C$ NMR and MS spectral analyses established the structures of the newly synthesized compounds. The results revealed that some of these compounds have shown promising antimicrobial and anti tubercular activity in comparison with standard drugs.

Synthesis of certain N-Aryl-N'-(2-pyrimidinyl)guanidine derivatives as potential antimicrobial agents

  • Eisa, H.M.;Tayel, M.A.;Yousif, M.Y.;El-Kerdway, M.M.
    • Archives of Pharmacal Research
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    • v.13 no.1
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    • pp.78-81
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    • 1990
  • N-Aryl-N'(4-hydroxy-6-methyl-2-pyrimidinyl)guanidines (IIa-c) were prepared by cyclization of N-arybiguanides (Ia-c) with ethyl acetoacetate. Coupling of compounds (IIa-c) with the appropriate diazotized arylamine gave N-aryl-N'-(5-arylhydrazono-6-methyl-4-oxopyrimidin-2-yl) guanidines (IIIa-f). Whereas, their chlorination with phosphorus oxychloride followed by treatment of N-aryl-N'-(4-Chloro-6-methyl-2-pyrimidinyl)guanidimes (IVac) with the appropriate arylamine afforded the corresponding 4-arylamino derivatives (Vaf). Compounds (IIa-f) were also formed when compounds (1a-c) were treated with ethyl 2-arylhydrazono-3-oxobutyrates. The antimircobial testing of some of the prepared compounds against some pathogenic microorganisms revealed that only two have a marked effect against Escherichia coli.

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Eco-friendly Solventless Synthesis of 5-Indolylpyrimido[4,5-d]pyrimidinones and Their Antimicrobial Activity

  • Gupta, Ragini;Jain, Anshu;Joshi, Rahul;Jain, Meenakshi
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.899-904
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    • 2011
  • A series of 5-indolylpyrimido[4,5-d]pyrimidinones (4a-h) were obtained by multi-component reaction of 3-formylindole (1), thiobarbituric acid/barbituric acid (2) and thiourea/urea (3) under microwave irradiation in dry media. Secondly, grinding together neat reactants also gave the titled compounds in good yields. All the synthesized compounds have been characterized on the basis of elemental analyses and spectral data (IR, $^1H$ NMR and Mass). Representative compounds were also evaluated for their antimicrobial activity against Rhizopus stolonifer, Fusarium oxysporum, Escherichia coli, and Pseudomonas aeruginosa at different concentrations. Some of the compounds showed promising activity.

Synthesis and Biological Evaluation of Some Novel [4-(1H-Benzoimidazol-2-yl)-thiazol-2-yl]-benzylidene-amines and N-[4-(1H-Benzoimidazol-2-yl)-thiazol-2-yl]-N'-benzylidene-hydrazines

  • Mekala, Raghu Vardhan Reddy;Danda, Ravinder Reddy;Gadegoni, Hemalatha
    • Journal of the Korean Chemical Society
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    • v.57 no.1
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    • pp.94-98
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    • 2013
  • A new family of thiazole heterocycles, namely [4-(1H-benzoimidazol-2-yl)-thiazol-2-yl]-benzylidene-amines has been synthesized by the condensation of 4-(1H-Benzoimidazol-2-yl)-thiazol-2-ylamine with various aromatic aldehydes and N-[4-(1H-benzoimidazol-2-yl)-thiazol-2-yl]-N'-benzylidene-hydrazines through the cyclization of 1-(1H-benzoimidazol-2-yl)-2-bromo-ethanone with arylthiosemicarbazones. The target compounds are achieved by using 1-(1H-Benzoimidazol-2-yl)-ethanone as starting material. The chemical structures of all newly synthesized compounds were confirmed by their IR, $^1H$ NMR and Mass spectral data. Further the compounds were used to evaluate their antimicrobial activity and found that the appreciable antimicrobial activity by some of the title compounds.

Studies on the synthesis of mannish bases of 2,2'-methylene bis(3,4,6-trichlorophenoxyacetic acid) and their antimicrobial activities (2,2'-methylene bis(3,4,6-trichlorophenoxyacetic acid)의 mannich bases합성및 항균작용에 관한 연구)

  • 김종호
    • YAKHAK HOEJI
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    • v.16 no.2
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    • pp.97-107
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    • 1972
  • Thirty-three Mannich bases of 2,2'-methylene bis(3,4,6-trichlorophenoxyacetic acid) were synthesized as potential antimicrobial agents and tested against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Trichophyton rubrum, Microsporum gypseum, Epidermophyton floccosum, Aspergillus niger and Aspergillus oryzae in vitro. It was found that: 1) Compounds 24 and 22 were active against Staphylococcus aureus and Bacillus subtilis at the concn. of 1 $\mu$g/ml respectively; 2) Compounds 9 and 29 were active against Trichophyton rubrum at the concn. of 2 $\mu$g/ml respectively; 3) Compouns 9 and 30 were active against Microsporum gypseum at the concn. of 2 $\mu$g/ml respectively; 4) Compounds 6,9,13,15,21,28,29,31,33 and 34 were active against Epidermophyton floccosum at the concn. of 1 $\mu$g/ml respectively; 5) Compounds 6,9,18 and 28 were active against Aspergillus niger and Aspergillus oryzae at the concn. of 1 $\mu$g/ml respectively.

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