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21.
The base catalyzed intramolecular nucleophilic cyclization of 1‐(2‐haloaroyl)‐3‐aryl thioureas ( 1a‐i ), in the presence of DMF afforded the 1‐aryl‐2‐thioxo‐2,3‐dihydro‐1H‐quinazolin‐4‐ones ( 2a‐i ). The structures were confirmed by spectroscopic data, elemental analyses and in case of the 2c by single crystal X‐ray diffraction data. The mechanistic studies support an intramolecular nucleophilic substitution (SNAr mechanism) rather than intramolecular aromatic substitution (SRN1 mechanism). 相似文献
22.
Synthesis and antimicrobial activity of some novel 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines 总被引:1,自引:0,他引:1
The synthesis of several 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines (2a-t) was carried out by base-catalyzed cyclization of corresponding 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas (1a-t) with 2-bromoacetone in aqueous medium. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. All synthesized compounds were evaluated for in vitro antibacterial activity using Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa). The minimum inhibitory concentration (MIC) was determined for the most active compounds. In vitro antifungal activity was also determined against the five fungal species (Rhizopus oryzae, Fusarium oxysporum, Aspergillus terreus, A. niger and A. fumigatus). 相似文献
23.
Rosa Pereira Tommy Julianto Peh-Kim Ang Sharon Sheue-Nee Ling Carlos Mauricio Barbosa Kah-Hay Yuen Abu Bakar Abdul Majeed 《Chromatographia》2010,71(5-6):373-381
A sensitive and rapid routine LC method was validated for measuring cefotaxime incorporated in three different pH-sensitive nanoparticles. The drug was chromatographed on a C18 reversed-phase column; the mobile phase used was 0.05 M aqueous ammonium acetate, acetonitrile and tetrahydrofuran (87:11:2, v/v) adjusted to pH 5.5 with acetic acid. The flow rate was 1 mL min?1 and cefotaxime was quantified at 254 nm, with a sensitivity range of 0.005 AUFS. The validated method was specific, linear (R 2 ≥ 0.999), precise and accurate in a concentration range of 0.2–50.0 μg mL?1. The method was rapid, selective and suitable for evaluation of cefotaxime in pH-sensitive Eudragit nanoparticles. 相似文献
24.
Asma Rehman Muhammad Irfan Majeed Ayesha Ihsan Syed Zajif Hussain Saif-ur-Rehman Muhammad Afzal Ghauri Zafar M. Khalid Irshad Hussain 《Journal of nanoparticle research》2011,13(12):6747-6754
Abstract
A simple and environmentally benign green method is reported to decorate growing fungal hyphae with high loading of gold nanoparticles, which were initially produced using aqueous tea extract as a sole reducing/stabilizing agent. Inoculation of fungal spores in aqueous suspension of nanoparticles led to the growth of intensely red-coloured fungal hyphae due to the accumulation of gold nanoparticles. Heat treatment of these hybrid materials led to the formation of porous gold microwires. This report is thus an interesting example of using green and sustainable approach to produce nanostructured materials which have potential applications in catalysis, sensing and electronics. 相似文献25.
26.
Shaheen Faizi Humaira Siddiqi Aneela Naz Samina Bano Lubna 《Helvetica chimica acta》2010,93(3):466-481
An H/D exchange process in patuletin ( 1 ) and its derivatives in D‐donor solvents (e.g., CF3COOD), which occurs regioselectively at C(8) was observed for the first time during NMR studies. The effect of substituents and temperature on the deuteration of various flavonoids (see Fig. 1) which include apigenin, chrysin, galangin, kaempferol, luteolin, morin, myricetin, patuletin, patulitrin, and quercetin, as well as derivatives of patuletin was examined extensively under NMR conditions. The rate constant of deuteration at C(8) of patuletin ( 1 ) and two flavones, luteolin ( 3 ) and apigenin ( 12 ), was also determined in CF3COOD. The D‐atom was introduced into the flavonoids via a keto–enol tautomerism (Scheme 1). During these studies, monodeuterated patuletin was also obtained as a new compound. The examined flavonoids have been reported to possess significant pharmacological activities, and their deuterated derivatives would be of importance for the identification and quantification of these compounds in biological matrices. 相似文献
27.
Anwar Sadat M. Alam Ashfaq Ahmad Bina Shaheen Siddiqui 《Natural product research》2015,29(24):2291-2294
Ethanol extract of the aerial parts of Bergenia ligulata was subjected to solvent–solvent separation followed by various chromatographic techniques that lead to isolation of bergenine (1), p-hydroxybenzoyl bergenin (2), 11-O-galloylbergenin (3) and methyl gallate (4) as major constituents. Ethyl acetate fraction showed a dose-dependent urease inhibitory pattern with IC50 value of 54μg/mL. Structures of compounds 1 and 3 were established by XRD and 2, 4 by NMR. All these compounds were subjected to DPPH scavenging activity, reducing power assay and urease inhibitory activity. The EC50 7.45 ± 0.2 μg/mL and 5.39 ± 0.28 μg/mL values in terms of antioxidant and reducing power, respectively, were less for 3. Compounds 1–3 showed moderate to significant urease inhibitory potential with IC50 57.1 ± 0.7, IC50 48.4 ± 0.3 and 38.6 ± 1.5. Antioxidant activities and urease inhibitory potential were investigated and compound 3 was found to be the most active. 相似文献
28.
Separation of isorhamnetin 3‐sulphate and astragalin from Flaveria bidentis (L.) Kuntze using macroporous resin and followed by high‐speed countercurrent chromatography
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Nusrat Shaheen Li Yin Yanxiang Gu Eric Rwigimba Qianqian Xie Yun Wei 《Journal of separation science》2015,38(11):1933-1941
D4020 resin offered the best dynamic adsorption and desorption capacity for total flavonoids based on the research results from ten kinds of macroporous resin. A column packed with D4020 resin was used to optimize the separation of total flavonoids from Flaveria bidentis (L.) Kuntze extracts. The content of flavonoids in the product was increased from 4.3 to 30.1% with a recovery yield of 90%. After the treatment with gradient elution on D4020 resin, the contents of isorhamnetin 3‐sulfate and astragalin were increased from 0.49 to 8.70% with a recovery yield of 74.1% and 1.16 to 30.8%, with a recovery yield of 92.2%, respectively. Further purification was carried out by one‐run high‐speed countercurrent chromatography yielding 4.5 mg of isorhamnetin 3‐sulfate at a high purity of 96.48% and yielding 24.4 mg of astragalin at a high purity of over 98.46%. 相似文献
29.
Chiral N‐sulfonyldiamine was successfully anchored on mesoporous MCM‐41 silica. The MCM‐41‐supported chiral N‐sulfonyldiamine was used as an efficient heterogeneous chiral ligand in the asymmetric transfer hydrogenation of ketones. This heterogeneous system offered satisfactory enantioselectivities up to 94 % with excellent conversions. 相似文献
30.
Polymyxins are cationic lipopeptide antibiotics active against many species of Gram-negative bacteria. We sequenced the gene cluster for polymyxin biosynthesis from Paenibacillus polymyxa PKB1. The 40.8 kb gene cluster comprises three nonribosomal peptide synthetase-encoding genes and two ABC transporter-like genes. Disruption of a peptide synthetase gene abolished all antibiotic production, whereas deletion of one or both transporter genes only reduced antibiotic production. Computational analysis of the peptide synthetase modules suggested that the enzyme system produces variant forms of polymyxin B (1 and 2), with D-2,4-diaminobutyrate instead of L-2,4-diaminobutyrate in amino acid position 3. Two antibacterial metabolites were resolved by HPLC and identified by high-resolution mass spectrometry and MS/MS sequencing as the expected variants 3 and 4 of polymyxin B1 (1) and B2 (2). Stereochemical analysis confirmed the presence of both D-2,4-diaminobutyrate and L-2,4-diaminobutyrate residues. 相似文献