Article Synthesis, Characterization and Antimicrobial Activity of New (original) (raw)
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Synthesis, Characterization and Antimicrobial Activity of New 1,2,3-Selenadiazoles
Molecules, 2008
The commercially available aromatic polyketones 1a-d were utilized for the synthesis of the multi-arm1,2,3-selenadiazole derivatives 3a-d. The preparation starts with the reaction between compounds 1a-d and p-toluenesulfonyl hydrazide to give the corresponding tosylhydrazones 2a-d. Subsequent reaction with selenium dioxide leads to regiospecific ring closure of the tosylhydrazones to give the target multi-arm 1,2,3selenadiazole derivatives in high yield. A 1,2,3-selenadiazole derivative 3e containing an epoxide ring was also prepared. The structures of all the synthesized compounds were confirmed on the basis of spectral and analytical data. The compounds were screened in vitro for their antimicrobial activity against various pathogenic bacterial and Candida strains obtained from King Abdullah Hospital in Irbid-Jordan. Compounds 3a, 3c and 3e were found to be highly active against all the selected pathogens. Compound 3e showed an inhibition zone of 13 mm against the highly resistant P. aruginosa.
European Journal of Medicinal Chemistry, 2011
A series of mono and bis-1,2,3-selenadiazole derivatives have been synthesized by the oxidative cyclization of mono and bis semicarbazones of 2-(3-oxo-1,3-diarylpropyl)-1-cyclohexanones using selenium(IV) oxide. The newly synthesized compounds were evaluated for their in vitro antimicrobial activity against Escherichia coli (ATCC 25922), Staphylococcus aureus (ATCC 11632) and Candida albicans (ATCC 90028) and in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB). Among these compounds, 1,3di(4-chlorophenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2h) and 3-(4-chlorophenyl)-1-(4-methylphenyl)-3-(4,5,6,7-tetrahydro-1,2,3-benzoselenadiazol-4-yl)-1-propanone (2g) were found to be the most active compounds with MIC of 3.3 and 3.5 mM respectively against MTB.
Synthesis of novel 2,5-disubstituted-1,3,4-selenadiazoles from fatty acid hydrazides
Arabian Journal of Chemistry, 2018
A series of novel unsaturated hydroxy and non-hydroxy fatty acid residue substituted 1,3,4-selenadiazoles were described here. These derivatives were synthesized from the reaction of fatty acid hydrazide 1(a-d) with acetyl chloride in the presence of anhydrous sodium carbonate in tetrahydrofuran and water at 0°C, to form N 0-acetyl undec-10-enoic hydrazide 2a, N 0-acetyl-(9Z)-octadec-9-enoic hydrazide 2b, N 0-acetyl-(9Z, 12R)-12-hydroxy-9-enoic hydrazide 2c, and N 0acetyl-(9R, 12Z)-9-hydroxy-12-enoic hydrazide 2d. Then these hydrazines (dicarbonyl compound) on reaction with Woollin's reagent (WR) in toluene led to the corresponding 2-(dec-9 0-enyl)-5methyl-1,3,4-selenadiazole 3a, 2-[(8 0 Z)-heptadec-8 0-enyl]-5-methyl-1,3,4-selenadiazole 3b, 2-[(8 0 Z, 11 0 R)-11 0-hydroxy-octadec-8 0-enyl)]-5-methyl-1,3,4-selenadiazole 3c, and 2-[(8 0 R, 11 0 Z)-8 0-hydroxyoctadec-11 0-enyl)]-5-methyl-1,3,4-selenadiazole 3d, respectively. These synthesized compounds were characterized on the basis of IR, 1 H NMR, 13 C NMR, mass spectra and elemental analysis results.
Synthesis and in vitro anti-bacterial evaluation of tetracyclic-ortho-fused 4H-naphtho[1′,2′–5,6]pyrano3,4-dselenadiazole and its derivatives
European journal of medicinal chemistry, 2008
Pyrazolo[3,4-d]pyrimidines are one of the most important classes of fused heterocyclic compounds which exhibit a broad range of biological and medicinal properties. They are known as anticancer, antifungal, antibacterial, antiviral and anti-inflammatory agents. In this study, some new 6-substituted 4-amino-pyrazolo[3,4-d]pyrimidine derivatives were prepared via reaction of 5-amino-3methyl-1-phenyl-1H-pyrazole-4-carbonitrile with various nitriles in the presence of sodium ethoxide as catalyst. The inhibitory properties of synthesized compounds were studied according to CLSI guidelines against some pathogenic bacteria including four gram-positive strains (Streptococcus pyogenes, Staphylococcus aureus, Bacillus cereus and Bacillus subtilis subsp. spizizenii) and three gramnegative strains (Pseudomonas aeruginosa, Shigella flexneri and Salmonella enterica subsp. enterica). The antibacterial effects of all derivatives were compared with those of antibiotics belonging to different classes. The values were reported as inhibition zone diameter (IZD), minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The effect of substituents on the biological activity of derivatives was discussed as well. The inhibitory effect of compound 6a, was shown to be the most, with MIC values in the range of 32-4096 lg/mL. Since most of the synthesized compounds were effective against Streptococcus pyogenes and Pseudomonas aeruginosa, they can be considered as inhibitors of these two bacteria.
Asian Journal of Chemistry
The commercially available aromatic polyketones 1a-d were utilized for the synthesis of the multi-arm1,2,3-selenadiazole derivatives 3a-d. The preparation starts with the reaction between compounds 1a-d and p-toluenesulfonyl hydrazide to give the corresponding tosylhydrazones 2a-d. Subsequent reaction with selenium dioxide leads to regiospecific ring closure of the tosylhydrazones to give the target multi-arm 1,2,3selenadiazole derivatives in high yield. A 1,2,3-selenadiazole derivative 3e containing an epoxide ring was also prepared. The structures of all the synthesized compounds were confirmed on the basis of spectral and analytical data. The compounds were screened in vitro for their antimicrobial activity against various pathogenic bacterial and Candida strains obtained from King Abdullah Hospital in Irbid-Jordan. Compounds 3a, 3c and 3e were found to be highly active against all the selected pathogens. Compound 3e showed an inhibition zone of 13 mm against the highly resistant P. aruginosa.
ChemistrySelect, 2020
A number of diversely functionalized derivatives of a novel [1,3] selenazolo[4,5-d]pyrimidine have been synthesized through heterocyclization of some 2,4,5-trisubstituted-1,3-selenazoles with orthoesters in refluxing acetic acid. The synthetic compounds were evaluated for their antimicrobial activity against a panel of microorganisms including Gram-negative bacteria, Gram-positive bacteria, and pathogenic fungi. The antifungal results revealed that the new selenium-containing heterocycles were as good as or sometimes better than terbinafine and fluconazole. The in vitro anticancer activities of aforementioned heterocyclic compounds were screened against human breast carcinoma MCF-7 and HeLa cervical cancer cells as well as HDF (human dermal fibroblast) normal cells. Antiproliferative results indicated that compounds with piperidine moiety on MCF-7 cells and with morpholine moiety on HeLa cells exhibited well broad-spectrum of anticancer activities with 397, 298 and 235 μM and 533, 390 and 204 μM of IC 50 values after 24, 48 and 72 h of treatments, respectively, while they had no significant toxic effects on normal cells.
Synthesis, Reaction and Antiviral Activity of 2,4-Diaryl-1,3-selenazoles
Journal of the Korean Chemical Society
요 약. α-Bromoketones을 가진 1차 arylselenocarboxylic amide의 고리화는 여러가지 새로운 2,4-diaryl-1,3-selenazoles에 사용되었다. 염소, 브롬, 요오드를 사용한 2,4-diaryl-1,3-selenazoles의 할로겐화는 좋은 수율의 새로운 1,1-dihalo-2,4-diaryl-1,3-selenazoles를 준다. AIDS virus(HIV-1 and HIV-2)에 대하여 몇몇의 1,1-dihalo-2,4-diaryl-
2021
Ethyl 2-(1H-pyrazol-1-yl)acetate (1) was synthesized by the reaction of ethylchloroacetate with 1H-pyrazole, Then compound (1) refluxed with hydrazine hydrate to get 2-(1H-pyrazol-1-yl) acetohydrazide (2). Compound (2) was reaction with appropriate aryl aldehyde to get schiff bases N'-arylidine-2-(1H-pyrazol-1-yl)acetohydrazide derivatives (3a-3f). schiff’s base (3a-3e) were cyclized by reflux with acetic anhydride to get new 1-(5-((1H-pyrazol-1-yl)methyl)-2-aryl-1,3,4-oxadiazol-3(2H)-yl)ethanone derivatives (4a-4e). The structures of the synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, mass spectra, and elemental analysis data. Synthesized compounds (4a-4e) were evaluated as antibacterial agents against some common pathogenic bacteria Gram-positive (Staphylococcus aureus, Streptococcus pyogenes) and Gram-negative bacteria (Escherichia coli, Psuedomonas aeruginosa). The result of antibacterial activity was compared with standard drugs (Ciprofloxacin and Tetracycl...
Journal of the Serbian Chemical Society, 2015
A new series of hydrazinecarbothioamides 6-9 bearing a 5H-dibenzo[a,d][7]annulene moiety were synthesized. Cyclization of 6-9 in NaOH solution produced the corresponding 4H-1,2,4-triazole-3-thiols 10-13, which proved to be axial isomers. The thioethers 14-17 were prepared by alkylation of 10-13 with methyl iodide. All new compounds were characterized by elemental analysis, and IR, UV, 1 H-NMR and 13 C-NMR spectroscopy. An evaluation for antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Bacillus subtilis, Salmonella enterica subsp. enterica serovar Typhimurium, Shigella flexneri and Candida albicans was performed.