• Title/Summary/Keyword: triazoles

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Design, Synthesis and Biological Activity of Certain 3,4-Disubstituted-5-mercapto-1,2,4-triazoles and Their Hydrazino Derivatives

  • Udupi, R.H.;Sudheendra, Sudheendra;Bheemachari, Bheemachari;Srinivasulu, N.;Varnekar, Rajesh;Purushottamachar, Puranik
    • Bulletin of the Korean Chemical Society
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    • v.28 no.12
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    • pp.2235-2240
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    • 2007
  • 3-Aryloxy methyl-4-(N-pyrazin-2'yl carboxamido)-5-mercapto-1,2,4-triazoles (3a1-a14) were prepared starting from potassium dithio carbazinates (2a1-a14). These triazoles were then employed in the synthesis of 3-aryloxy methyl-4-(N-pyrazin-2'yl carboxamido)-5-hydrazino-1,2,4-triazoles (4a1-a14). All the newly synthesized compounds were characterized by analytical, IR, NMR spectral studies. The compounds were screened for their antibacterial, antifungal, anti-inflammatory and analgesic properties. Most of the compounds have shown significant antifungal activity while few have shown excellent anti-inflammatory and analgesic activity. An attempt is made to study the structure activity relationship (SAR).

2-Benzothiazolylhydrazones with Cation Radicals in Nitrile Solvents. Formations of 1,2,4-Triazoles and Triazolo[3,4-b]benzothiazoles

  • Park, Gun Ha;Jeon, Geon;O, Si Hwa
    • Bulletin of the Korean Chemical Society
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    • v.21 no.4
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    • pp.425-428
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    • 2000
  • Arenealdehyde 2-benzothiazolylhydrazone in thianthrene cation radicalafforded triazolo[3,4-b]benzothiazoles and 1,2,4-triazoles as major and minor product, respectively. On the contrary the similar reaction in tris(2,4-dibromophenyl)aminium hexachloroantimonate gave 1,2,4-triazoles and triazolo[3,4-b]benzothiazoles as ma-jor and minor product, respectively.

Synthesis of New Xanthenone Derivatives of Expected Antibilharzial Activity

  • Omar, Mahmoud-T.
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.602-609
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    • 1997
  • A new series of 1, 3, 4-oxadiazoles, 1, 3, 4-thiadiazoles and 1, 2, 4-triazoles incorporated directly and/or indirectly into a xanthenone moiety at position-2-were synthesized. Some of the newly prepared compounds were biologically tested as schistosomicides in experimental animals.

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Synthesis and Characterization of 1-Benzofuran-2-yl thiadiazoles, Triazoles and Oxadiazoles by Conventional and Non-conventional Methods (반응방법에 따른 1-Benzofuran-2-yl thiadiazoles, Triazoles과 Oxadiazoles의 합성)

  • Shinde, Ananta D.;Kale, Bhima Y.;Shingate, Bapurao B.;Shingare, Murlidhar S.
    • Journal of the Korean Chemical Society
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    • v.54 no.5
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    • pp.582-588
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    • 2010
  • The synthesis of benzofuran based 1,3,4-thiadiazoles, 1,3,4-triazoles and 1,3,4-oxadiazole via cyclocondensation of thiosemicarbazides have been carried out by conventional and non-conventional methods in excellent yields of product.

Synthesis of New Salicylamide Derivatives with Evaluation of Their Antiinflammatory, Analgesic and Antipyretic Activities

  • Fahmy, H.H.;Soliman, G.A.
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.180-189
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    • 2001
  • A new series of pyridazine, pyrazoles, pyrazolidine-3,5-dione, Semicarbazide, thiosemicarbazides, hydantoin, thiohydantoins, 1,2,4-triazoles, S-triazolo[3,4-b]-1,3,4-thiadiazoles incorporated indirectly into salicylamide moiety at position 2 were synthesized. Also the synthesis of novel series of 3-salicylamido-2-hydroxypropyl-amino derivatives were prepared. Several of these compounds were screened for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.

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Antibacterial, Antifungal and Anticonvulsant Evaluation of Novel Newly Synthesized 1-[2-(1H-Tetrazol-5-yl)ethyl]-1H-benzo[d][1,2,3]triazoles

  • Rajasekaran, Aiyalu;Murugesan, Sankaranarayanan;AnandaRajagopal, Kalasalingam
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.535-540
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    • 2006
  • Several novel 1-[2-(1H-tetrazol-5-yl) ethyl]-1H-benzo[d][1,2,3]triazoles (3a-h) have been synthesized by the condensation of 1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-benzotriazole (2) and appropriate acid chlorides. 1-[2-(1H-tetrazol-5-yl)-ethyl]-1H-benzotriazole (2) was synthesized by reacting 3-(1H-benzo[d][1,2,3]triazol-1-yl)propanenitrile with sodium azide and ammonium chloride in the presence of dimethylformamide. The synthesized compounds were characterized by IR and PMR analysis. The titled compounds were evaluated for their in vitro antibacterial and antifungal activity by the cup plate method and anticonvulsant activity evaluated by the maximal electroshock induced convulsion method in mice. All synthesized compounds exhibited moderate antibacterial activity against Bacillus subtilis and moderate antifungal activity against Candida albicans. Compounds 5-(2-(1 H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(4-aminophenyl)methanone 3d and 5-(2-(1 H-benzo[d][1,2,3]triazo-1-yl)ethyl)-1H-tetrazol-1-yl)(2-aminophenyl)methanone 3e elicited excellent anticonvulsant activity.

Synthesis, Fastness and Spectral Properties of Some New Azo Pyrazole and Pyrazolotriazole Derivatives (Pyrazole과 Pyrazolotriazole 유도체의 합성 및 특성 연구)

  • Rizk, Hala F.;El-Badawi, Mahmoud A.;Ibrahim, Seham A.;El-Borai, Mohamed A.
    • Journal of the Korean Chemical Society
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    • v.54 no.6
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    • pp.737-743
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    • 2010
  • Coupling of 5-amino-1,3-diaryl-pyrazoles 1a-c with diazonium salts of different aryl amines gave a series of novel 1,3-diaryl-5-amino-4-arylazopyrazoles 3a-l. Such compounds could be also obtained by reaction of 5-amino-1,3-diaryl-4-nitroso- 1H-pyrazoles 2a-c with different aryl amines in alkaline medium. Oxidation of azo derivatives 3a-l with cupric acetate, in dimethyl formamide and stream of air, gave 2,4,6-triaryl-2,4-dihydropyrazolo [4,3-d]-1,2,3-triazoles 4a-l. and the fluorescence properties of the cyclic triazoles were studied. Diazotization of 5-amino-1,3-diaryl-1H-pyrazoles 1a-c by sodium nitrite in ortho-phosphoric acid followed by coupling with some aryl amines gave o-aminoazo compounds 5a-f. Cyclisation of compounds 5a-f in pyridine and cupric acetate gave the corresponding triazoles 6a-f. The coupling of compounds 6a-f with different aryl diazonium salts gave compounds 7a-j. The synthesized dyes were applied to polyesters as disperse dyes and the fastness properties were evaluated.

Chemical Modification of Poly(vinylacetylene) and Synthesis of Poly(1,2,3-triazole)s

  • Wang, Lian-Jun;Liao, Shan;Wang, Le-Yong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.5
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    • pp.1471-1474
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    • 2011
  • A series of new polymers containing 1,2,3-triazoles were synthesized and their structures and properties were characterized by FT-IR, $^1H$ NMR, TGA, DSC and GPC. The results showed that the polymers modified by alkyl groups had good solubility, thermal stability and reasonable molecular weights. It was also demonstrated that the properties of fluorine-containing polymers were seriously affected by fluorine atoms with hydrophobic and chemical proof properties.

Synthesis of Novel Halobenzyloxy and Alkoxy 1,2,4-Triazoles and Evaluation for Their Antifungal and Antibacterial Activities

  • Wan, Kun;Zhou, Cheng-He
    • Bulletin of the Korean Chemical Society
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    • v.31 no.7
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    • pp.2003-2010
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    • 2010
  • A new class of halobenzyloxy or alkoxy 1,2,4-triazoles and their hydrochlorides were synthesized through cyclization starting from commercially available phenylhydrazine. The structures were characterized by MS, IR and $^1H$ NMR spectra as well as elemental analyses. All the synthesized compounds were screened for their antibacterial activities in vitro against Staphylococcus aureus (ATCC29213), methicillin-resistant Staphylococcus aureus (N315), Bacillus subtilis, Escherichia coli (ATCC25922), Pseudomonas aeruginosa, Shigella dysenteriae, Eberthella typhosa, and antifungal activities against Candida albicans (ATCC76615), Aspergillus fumigatus by broth microdilution assay method. The results of preliminary bioassay indicated that 3-(2,4-difluorobenzyloxy)-1-phenyl-1H-1,2,4-triazole hydrochloride exhibited the best inhibitory activity with an MIC value of 56.25 ${\mu}M$ against P. aeruginosa superior to Chloramphenicol, and showed comparable activity with Chloramphenicol against E. coli (ATCC25922).

Ecofriendly Synthesis of Antifungal Azoles

  • Kidwai, M.;Mohan, R.
    • Journal of the Korean Chemical Society
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    • v.48 no.2
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    • pp.177-181
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    • 2004
  • 1,2,4-Triazoles, pyrazolones and 1,3,4-oxadiazoles have been synthesized from substituted hydrazide using various solid supports under microwave irradiation (MWI). The results obtained highlight the versatility of the solid supports. All synthesized compounds were screened for their antifungal activity against A. niger and A. flavus and were found to possess good activity.