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1.
A series of 2,4-dichloro-5-fluorophenyl substituted arylidenetriazolothiazolidinones were obtained by one-pot reaction of
3-(2,4-dichloro-5-fluorophenyl)-4H-1,2,4-triazole-5-thiol with substituted benzaldehydes and monochloroacetic acid in the presence of acetic anhydride, acetic
acid, and sodium acetate. The structures of the newly synthesized compounds were characterized and confirmed by IR, 1H NMR, mass spectra, and elemental analysis. Compounds bearing the 4-methylthiophenyl, 3,4-methylenedioxyphenyl, and 2,3,5-trichlorophenyl
moiety showed excellent antiinflammatory activity. The antimicrobial screening studies revealed that compounds with 4-anisyl,
4-methylthiophenyl, 3,4-methylenedioxyphenyl, and 2,3,5-trichlorophenyl at position 5 of the arylidenetriazolothiazolidinone
moiety showed excellent activity against all tested strains at 6.25 μg cm−3 concentrations. 相似文献
2.
A series of 2,4-dichloro-5-fluorophenyl substituted arylidenetriazolothiazolidinones were obtained by one-pot reaction of
3-(2,4-dichloro-5-fluorophenyl)-4H-1,2,4-triazole-5-thiol with substituted benzaldehydes and monochloroacetic acid in the presence of acetic anhydride, acetic
acid, and sodium acetate. The structures of the newly synthesized compounds were characterized and confirmed by IR, 1H NMR, mass spectra, and elemental analysis. Compounds bearing the 4-methylthiophenyl, 3,4-methylenedioxyphenyl, and 2,3,5-trichlorophenyl
moiety showed excellent antiinflammatory activity. The antimicrobial screening studies revealed that compounds with 4-anisyl,
4-methylthiophenyl, 3,4-methylenedioxyphenyl, and 2,3,5-trichlorophenyl at position 5 of the arylidenetriazolothiazolidinone
moiety showed excellent activity against all tested strains at 6.25 μg cm−3 concentrations.
Correspondence: Mari Sithambaram Karthikeyan, Department of Chemistry, Mangalore University, Mangalagangothri 574199, Karnataka,
India. 相似文献
3.
Mari S. Karthikeyan Bantwal S. Holla Shalini Shenoy 《Monatshefte für Chemie / Chemical Monthly》2008,139(6):707-716
2,4-Dichloro-5-fluorophenyl containing 7-arylidenetriazolothiadiazines were obtained by the reaction of 4-amino-3-(2,4-dichloro-5-fluorophenyl)-5-mercapto-1,2,4-triazole
with 2,3-dibromo-1,3-diarylpropan-1-ones, and also by the reaction of 4-amino-3-(2,4-dichloro-5-fluorophenyl)-5-mercapto-1,2,4-triazole
with α-bromopropenones in the presence of a base. The structure of the 7-arylidenetriazolothiadiazines was confirmed by an
alternative synthesis. A plausible mechanism for the formation of 7-arylidenetriazolothiadiazines is proposed. All newly synthesized
compounds were screened for their analgesic and antimicrobial activities. Compounds bearing 4-chlorophenyl or 3,4-methylenedioxyphenyl
moieties at position 7 of the arylidenetriazolothiadiazines showed excellent analgesic activity. Arylidenetriazolothiadiazines
carrying a phenyl, 4-chlorophenyl, 4-methylphenyl, 3,4-dimethoxyphenyl, and 2,4-dichlorophenyl moieties at position 7 showed
excellent antibacterial and antifungal activities.
Correspondence: Mari Sithambaram Karthikeyan, Department of Chemistry, Mangalore University, Mangalagangothri 574199, Karnataka,
India. 相似文献
4.
Nuray Ulusoy Öznur Ateş Ömer Küçükbasmacı Muammer Kiraz Yıldız Yeğenoğlu 《Monatshefte für Chemie / Chemical Monthly》2003,134(3):465-474
Summary. Some novel 4-[[2-[[5-(2-furanyl)-4-alkyl/aryl-4H-1,2,4-triazol-3-yl]thio]-acetyl/propionyl]-amino]-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazoles were synthesized and evaluated for in vitro antibacterial activity against Staphylococcus aureus ATCC 29213, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, and Enterococcus faecalis ATCC 29212 and antifungal activity against Candida albicans ATCC 10231, Candida parapsilosis ATCC 22019, Candida krusei ATCC 6258, Candida parapsilosis, Trichophyton mentagrophytes var. erinacei NCPF 375, Microsporum gypseum NCPF 580, and Trichophyton rubrum using the microbroth dilution method. All of the compounds were found to be ineffective against the above bacteria within
the applied MIC ranges. On the other hand, they were effective against fungi to different degrees. Three compounds showed
high activity against C. parapsilosis and T. mentagrophytes var. erinacei NCPF 375 (MIC = 8 μg cm−3). The in vitro antimycobacterial activity of the new compounds was also investigated against Mycobacterium tuberculosis H37RV (ATCC 27294) in BACTEC 12B medium using a broth microdilution assay, the Microplate Alamar Blue Assay (MABA). Compounds
exhibiting fluorescence were tested in the BACTEC 460 radiometric system. The most active compound was found with 66% inhibition
at >6.25 μg cm−3.
Corresponding author. E-mail: nurayulusoy@yahoo.com
Received July 24, 2002; accepted August 26, 2002 相似文献
5.
Summary. A new simple, rapid, sensitive, and selective method is proposed for the microdetermination of mercury. Mercury(II) forms
insoluble complexes with 2,3-dichloro-6-(2-hydroxy-3,5-dinitrophenylazo)-quinoxaline (1), 2,3-dichloro-6-(5-amino-3-carboxy-2-hydroxy-phenylazo)-quinoxaline (2), 2,3-dichloro-6-(2,7-dihydroxynaphth-1-ylazo)-quinoxaline (3), and 2,3-dichloro-6-(3-carboxy-2-hydroxy-naphth-1-ylazo)-quinoxaline (4) in aqueous acidic medium; the complexes can be made soluble by the action of an anionic surfactant. The solution of the
pink coloured compounds is stable for at least 24 h. Beer’s law is obeyed over the concentration range from 0.1 to 2.8 μg · cm−3 of mercury. For a more accurate analysis, Ringbom optimum concentration ranges were found to be 0.25–2.5 μg · cm−3. The molar absorpitivity, Sandell sensitivity, and relative standard deviations were also calculated. A slight interference from Pd2+ and Cd2+ is exhibited by the first three ligands, whereas the last one is only negligibly affected by these metal ions. Strong interference
from Ag(I) is evident for all ligands, whereas alkali, alkaline earth, and other transition metals tested posed negligible
interference. 15 μg · cm−3 of Cd2+ and Pd2+ or 10 μg · cm−3 of Ag+ can be tolerated if 1.0 mg of potassium bromide and 2.0 mg of citrate as masking agents are added for the determination of
1.5 μg · cm−3 of mercury(II). The method was applied to the determination of methyl- and ethylmercury chloride and the analysis of environmental
water samples.
Received August 7, 2000. Accepted (revised) October 18, 2000 相似文献
6.
The development and characterization of one rat monoclonal antibody (mAb) for 2,4-dinitroaniline and of two rat mAbs for 2,6-dinitroaniline
are described. With the immunization of rats with 2,4,6-trinitrophenyl-glycylglycine–keyhole limpet hemocyanine (KLH) conjugate
one mAb (PK 5H6) has been developed and formatted into a competitive enzyme-linked immunosorbent assay (ELISA). This assay
no. 1 is very sensitive for 2,4-dinitroaniline with a test midpoint of 0.24 ± 0.06 μg L−1 (n = 19) in 40 mM phosphate-buffered saline (PBS). A second hapten, 3-(4-amino-2,6-dinitrophenyl)propionic acid, which was also
conjugated to KLH and used for the immunization of rats, led to two sensitive ELISAs for 2,6-dinitroaniline in 40 mM PBS with
test midpoints of 0.61 ± 0.08 μg L−1 (n = 15; mAb DNT4 3C6; assay no. 2) and 0.94 ± 0.29 μg L−1 (n = 17; mAb DNT4 1A7, assay no. 3). Selectivities of all mAbs were checked with more than 20 compounds, including nitroaromatic
compounds, 2,6-dinitroaniline pesticides, and other substituted derivatives of aniline. As very noticeable cross-reactivities,
all mAbs recognize 2-chloro-4,6-dinitroaniline, 4-chloro-2,6-dinitroaniline and 2-bromo-4,6-dinitroaniline, the last of these
being a major metabolite of the azo dye Disperse Blue 79. As first demonstrations of applications, two ELISAs (assays no.
1 and 2) were used for the analysis of 2,4- or 2,6-dinitroaniline in spiked water and soil samples. Recovery data were determined
and the majority of these data were in the range of 90–120%. These assays can contribute to a very cost-effective and environmentally
friendly immunochemical surveillance monitoring of environmental samples for contaminations with these compounds. To the best
of the authors’ knowledge, these are the first antibodies described for 2,4-dinitroaniline and for 2,6-dinitroaniline. 相似文献
7.
Summary. 2-Hydroxy-2,2-diphenylacetohydrazide (2), cyclic ketones, and mercaptoalkanoic acids were converted into 2-hydroxy-N-(3-oxo-1-thia-4-azaspiro[4.4]non/[4.5]dec-4-yl)-2,2-diphenylacetamide derivatives (3, 4) in a one pot procedure. Compounds 3 and 4 were tested for in vitro antimycobacterial activity against M. tuberculosis H37Rv. The compounds were found to provide 0–86% inhibition of mycobacterial growth in the primary screen conducted at 6.25 μg/cm3. 相似文献
8.
The Fe3O4-Prussian blue (PB) nanoparticles with core-shell structure have been in situ prepared directly on a nano-Fe3O4-modified glassy carbon electrode by cyclic voltammetry (CV). First, the magnetic nano-Fe3O4 particles were synthesized and characterized by X-ray diffraction. Then, the properties of the Fe3O4-PB nanoparticles were characterized by CV, electrochemical impedance spectroscopy, and superconducting quantum interference
device. The resulting core-shell Fe3O4-PB-modified electrode displays a dramatic electrocatalytic ability toward H2O2 reduction, and the catalytic current was a linear function with the concentration of H2O2 in the range of 1 × 10−7~5 × 10−4 mol/l. A detection limit of 2 × 10−8 (s/n = 3) was determined. Moreover, it showed good reproducibility, enhanced long-term stability, and potential applications in
fields of magnetite biosensors. 相似文献
9.
Yunchun Wang Zhongyuan Bai Zengjun Wei Shengzhen Xu Xuegang Li Jianhong Li Xiufang Cao Changshui Chen 《Research on Chemical Intermediates》2011,37(8):1029-1039
Twenty-two novel N-nitro-N′-substituted phenyl-N-(2,6-dibromo-4-fluorophenyl)urea derivatives were designed and synthesized via a simple and convenient BTC ‘one-pot’ procedure
using DMAP as the catalyst. The structures of all newly synthesized compounds were confirmed by IR, 1H NMR, and elemental analysis, and a part has been identified by 13C NMR. The preliminary bioassay indicates that the target compounds possesses moderate herbicidal activity against Sorghum sudanense. However, some of the title compounds presented high plant growth regulating activity against rape. 相似文献
10.
Nuray Ulusoy Muammer Kiraz Ömer Küçükbasmacı 《Monatshefte für Chemie / Chemical Monthly》2002,133(10):1305-1315
Summary. New 4-alkyl/aryl-1-((6-(4-bromophenyl)-imidazo[2,1-b]thiazol-3-yl)-acetyl)-3-thiosemicarbazides and 3-alkyl/aryl-2-(((6-(4-bromophenyl)-imidazo[2,1-b]thiazol-3-yl)-acetyl)-hydrazono)-4-thiazolidinones were synthesized from 6-(4-bromophenyl)-imidazo[2,1-b]thiazole-3-acetic acid hydrazide. Their structures were elucidated by elemental analyses and spectroscopic data. All compounds
were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by the
microbroth dilution technique. The compounds were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294); they exhibited varying degrees of inhibition in the in vitro primary screening at 6.25 μg · cm−3. The most active compound was 3-(4-nitrophenyl)-2-(((6-(4-bromophenyl)-imidazo[2,1-b]thiazol-3-yl)-acetyl)-hydrazono)-4-thiazolidinone.
Corresponding author. E-mail: nurayulusoy@yahoo.com
Received December 10, 2001. Accepted (revised) March 1, 2002 相似文献
11.
Livio Racanè Vesna Tralić-Kulenović Richard P. Kitson Grace Karminski-Zamola 《Monatshefte für Chemie / Chemical Monthly》2006,137(12):1571-1577
Summary. Series of cyano, dicyano, amidino, and diamidino substituted 2-phenylbenzothiazoles were prepared. Mono- and dicyano substituted
benzothiazoles were obtained by condensation of appropriate substituted benzaldehydes with 2-aminothiophenol or 4-amino-3-mercaptobenzonitrile.
The appropriate amidines or diamidines were prepared by Pinner reaction. The compounds were tested against breast, prostate, and lung cancer cell lines in a 72 h cytotoxicity assay. Many
of the compounds had at 10 μM activity equivalent to 2-(4-aminophenyl)benzothiazole, while four compounds had significantly better activity, particularly
in the breast cancer model. 相似文献
12.
Mario Wurglics Astrid Michelitsch Gotthard Wurm 《Monatshefte für Chemie / Chemical Monthly》2002,133(9):1225-1230
Summary. Comparative studies of redox behaviour and antioxidative activity (AOA) were carried out with two series of arylnaphthoquinone
derivatives. For the electrochemical investigations, a voltammetric procedure combined with a glassy carbon electrode was
applied. The AOA was examined using the photo-chemiluminometric method with the Photochem? measuring device according to Popov et al. and the chemical procedure with the radical quencher DPPH (diphenylpicrylhydrazyl). Both the redox potential and the antioxidative activity of the investigated compounds are influenced
by their substituents. Compounds with the OH-group at position 3 are easiest to oxidize (E
p = 0.18 V; pH 7.4). The lag phases (AOA) of these compounds are five to ten times greater than those of the strong antioxidants ascorbic
acid and Trolox?. As suggested for other natural compounds, we also found a good correlation between the oxidation potential and the AOA.
Therefore, it seems that a good antioxidative activity requires a low redox potential.
Corresponding authors. E-mail: wurglics@pharmchem.uni-frankfurt.de
Received March 1, 2002; accepted March 28, 2002 相似文献
13.
Summary. The two new compounds Mn(dien)2[MoS4] (1) and Mn(dien)2[Mo2O2S6] (2) (dien = diethylenetriamine) were prepared under solvothermal conditions. Both compounds were obtained as phase-pure products. The
structures consist of new [Mn(dien)2]2+ cations and isolated tetrahedral [MoS4]2− (1) or [Mo2O2S6]2− (2) anions. Between the anions and the cations, hydrogen bonding is observed. Compound 1 crystallizes in the tetragonal space group I (a = 10.219(2), c = 9.259(2) ?, Z = 2), whereas 2 crystallizes in the monoclinic space group P21/c (a = 8.703(2), b = 18.390(4), c = 14.603(3) ?, β = 103.18(3)°, Z = 4). The thermal behaviour of the thiomolybdates was investigated using difference thermoanalysis (DTA) and thermogravimetry
(TG). Both compounds decompose under argon with a single endothermic signal in the DTA curve (peak maximum: 252 (1) and 242°C (2)).
Received November 5, 2001. Accepted December 27, 2001 相似文献
14.
Summary. Rhodococcus AJ270 is adsorbed by Dowex 1 at 15.4 mg dry weight per g resin with maximum amidase specific activity observed at lower
loadings. Bacteria form a monolayer on the resin surface, and adsorption is complete within 2 min. AJ270 can be entrapped
in agar and agarose gels (optimum loading: 20 mg dry weight bacteria per cm3 gel). Adsorption and entrapment improve amidase thermal stability 3–4 fold, and entrapment shifts the pH optimum from 8 to 7. Adsorbed and free bacteria show similar values for K
m and V
max, but entrapped bacteria have higher K
m values. Compared with bacteria adsorbed to Dowex, the activity per cm3 of matrix of agar-entrapped AJ270 is eight-fold higher. In stirred-tank reactors, exposure to acrylic acid reduces the amidase
activity of the biocatalyst in the hydrolysis of acrylamide. In column reactors, entrapped AJ270 suffers little reduction
in amidase activity against 0.25 M acrylamide over 22 h continuous operation.
Received November 18, 1999. Accepted December 14, 1999 相似文献
15.
Juozas Kulys Heinz-Josef Deussen Kastis Krikstopaitis Palle Schneider Arturas Ziemys 《Monatshefte für Chemie / Chemical Monthly》2001,132(2):295-304
Summary. N-Aryl-N-hydroxy urethanes (AHUs), which are promising N*OH mediators for oxidoreductase catalysis, are electrochemically active redox compounds with a redox
potential of 0.35–0.40 V vs. SCE (0.59–0.64 V vs. NHE). Alkyl substituents in the carbamic acid residue have, as expected, only little influence on the redox potential. The
highest potential was noticed for N-hydroxy-N-(4-cyanophenyl)-carbamic acid methyl ester. Recombinant Coprinus cinereus peroxidase (rCiP) catalyzes oxidation of the AHUs with apparent bimolecular constants k
ox of 2.5ċ104–7.5ċ104 M
−1s−1 at pH = 8.5 and 25°C.
Structure-function connectivities of the substrates were analysed within the framework of the Marcus cross relationship and by using ab initio quantum chemical calculations. An excellent correlation of the redox potentials and the HOMO energies could be found. However,
no correlation of log(k
ox) with redox potential and HOMO energy was indicated as predicted by theory. This was explained by specific docking of the
substrates in the active center of rCiP.
Received June 26, 2000. Accepted (revised) August 9, 2000 相似文献
16.
Nuray Ulusoy Muammer Kiraz ?mer Kü?ükbasmac? 《Monatshefte für Chemie / Chemical Monthly》2002,20(3):1305-1315
New 4-alkyl/aryl-1-((6-(4-bromophenyl)-imidazo[2,1-b]thiazol-3-yl)-acetyl)-3-thiosemicarbazides and 3-alkyl/aryl-2-(((6-(4-bromophenyl)-imidazo[2,1-b]thiazol-3-yl)-acetyl)-hydrazono)-4-thiazolidinones were synthesized from 6-(4-bromophenyl)-imidazo[2,1-b]thiazole-3-acetic acid hydrazide. Their structures were elucidated by elemental analyses and spectroscopic data. All compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by the microbroth dilution technique. The compounds were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294); they exhibited varying degrees of inhibition in the in vitro primary screening at 6.25 μg · cm−3. The most active compound was 3-(4-nitrophenyl)-2-(((6-(4-bromophenyl)-imidazo[2,1-b]thiazol-3-yl)-acetyl)-hydrazono)-4-thiazolidinone. 相似文献
17.
CeO2 nanoparticles approximately 12 nm in size were synthesized and subsequently characterized by XRD, TEM and UV-vis spectroscopy.
Then, a gold electrode modified with CeO2 nanoparticles was constructed and characterized by electrochemical impedance spectroscopy (EIS) and cyclic voltammetry (CV).
The modified electrode demonstrated strong catalytic effects with high stability towards electrochemical oxidation of rutin.
The anodic peak currents (measured by differential pulse voltammetry) increased linearly with the concentration of rutin in
the range of 5.0 × 10−7–5.0 × 10−4 mol · L−1. The detection limit (S/N = 3) was 2.0 × 10−7 mol · L−1. The relative standard deviation (RSD) of 8 successive scans was 3.7% for 5.0 × 10−6 mol · L−1 rutin. The method showed excellent sensitivity and stability, and the determination of rutin in tablets was satisfactory. 相似文献
18.
Süleyman Gürsoy Ali Cihan Makbule B. Koçak Oüzer Bekaroğlu 《Monatshefte für Chemie / Chemical Monthly》2001,132(7):813-819
Summary. A novel phthalodinitrile derivative carrying dimethylaminoethylsulfanyl groups at positions 4 and 5 was synthesized from
2-dimethylaminoethanethiol hydrochloride and 1,2-dichloro-4,5-dicyanobenzene. Its cyclotetramerization in the presence of
2-dimethylamino-ethanol or metal salts (CoCl2, Zn(OAc)2) gave metal-free or metal-containing phthalocyanines (M = Co or Zn). These phthalocyanines were converted into water soluble quaternized products by reaction with methyl iodide.
The new compounds were characterized by elemental analysis, IR, NMR, and electronic spectra. 相似文献
19.
Gangyue Li Xuhong Qian Shenggang Yan Jingnan Cui Rong Zhang Yi Xiao 《Monatshefte für Chemie / Chemical Monthly》2008,139(2):169-178
Summary. A series of novel 2-phenyliminothiazolidine derivatives were designed and synthesized. All title compounds were characterized
by 1H NMR and, in some cases, by 13C NMR, IR, and HRMS. Their agricultural bioactivities were evaluated and some of these compounds exhibited efficient herbicidal
activities against Echinochloa crusgalli, Sorghum vulgare, Digitaria sanguinalis, Eclipta prostrasta, Cucumis sativus, and Brassica campestris at 50 μg/cm3. Analysis of the quantitative structure-activity relationship (QSAR) showed that the electronic parameter was the main factor
to affect herbicidal activities. 相似文献
20.
Aisha Y. Hassan Marwa T. Sarg Ebtehal M. Hussein 《Journal of heterocyclic chemistry》2019,56(4):1437-1457
On the pharmaceutical account of the reported anticancer activity of benzothiazole derivatives, differently substituted benzothiazole derivatives 2a – c to 34a , b , attached at 2‐position to different heterocyclic moieties, were synthesized via different chemical reactions. Thirteen of the newly synthesized compounds were selected by the National Cancer Institute, Bethesda, Maryland, USA, and evaluated for their in vitro antitumor activity against 60 human tumor cell lines in a one‐dose screening panel among which two compounds 4 and 17 showed high activity and were selected for further evaluation in the five‐dose full panel assay, in which compound 4 exerted powerful growth inhibitory activity against all cell lines with GI50 ranging from 0.683 to 4.66 μM/L in addition to excellent lethal activity against most of the cell lines. 相似文献