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Mohammad Mahdi Ahari-Mostafavi Ali Sharifi Mojtaba Mirzaei Massoud Amanlou 《Journal of the Iranian Chemical Society》2014,11(4):1113-1119
The objective was to obtain new scaffold of compounds possessing anti-urease activity. For this new and simple method for the synthesis of β-aryl-β-mercapto ketone derivatives based on Michael addition of thiophenol to chalcones in an ionic liquid as a solvent was improved. The products were obtained in good to moderate yields with high purity and characterized by spectral and elemental analyses. The activities of synthesized compounds were investigated as new inhibitors of jack bean urease. Among 22 synthesized compounds, all of them have shown inhibitory effect in micromolar range, and the most potent one has IC50 = 6 μM compared to hydroxyurea IC50 = 100 μM as a reference inhibitor. A docking study was performed using Autodock 4.2 in parallel to in vitro experiments to illustrate the corresponded binding affinities as well as binding site, and involved residues in interaction. These computational results complimented the experimental inhibition activity and enabled us to report a potent urease inhibitors based on β-aryl-β-mercapto ketone scaffold. 相似文献
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Souri E Jalalizadeh H Farsam H Ghadiri R Amanlou M 《Chemical & pharmaceutical bulletin》2005,53(8):949-951
Derivative spectrophotometry offers a useful approach for the analysis of drugs in multi-component mixtures. In this study a third-derivative spectrophotometric method was used for simultaneous determination of cyproterone acetate and ethinylestradiol using the zero-crossing technique. The measurements were carried out at wavelengths of 316 and 226 nm for cyproterone acetate and ethinylestradiol respectively. The method was found to be linear (r2>0.999) in the range of 0.5-6 mg/100 ml for cyproterone acetate in the presence of 35 microg/100 ml ethinylestsradiol at 316 nm. The same linear correlation (r2>0.999) was obtained in the range of 10-80 microg/100 ml of ethinylestradiol in the presence of 2 mg/100 ml of cyproterone acetate at 226 nm. The limit of determination was 0.5 mg/100 ml and 10 microg/100 ml for cyproterone acetate and ethinylestradiol respectively. The method was successfully applied for simultaneous determination of cyproterone acetate and ethinylestradiol in pharmaceutical preparations without any interferences from excipients. 相似文献
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Saboury AA Bagheri S Ataie G Amanlou M Moosavi-Movahedi AA Hakimelahi GH Cristalli G Namaki S 《Chemical & pharmaceutical bulletin》2004,52(10):1179-1182
Thermodynamic studies were carried out to evaluate the binding of theophylline on adenosine deaminase (ADA) in 50 mM sodium phosphate buffer pH 7.5, at 300 K, using isothermal titration calorimetry (ITC). A simple method for determination of binding isotherm in the drug--ADA interaction was applied using ITC data. ADA has two binding sites for theophylline, which show positive cooperativity in its sites. The intrinsic association equilibrium constants are 6 and 52 mM(-1) in the first and second binding sites, respectively. Hence, occupation of the first site has produced an appreciable enhancement by 8.7 of the binding affinity of the second site. The molar enthalpies of binding are -12.2 and -14.9 kJ/mol in the first and second binding sites, respectively. 相似文献
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Mehdi Adib Ehsan Sheikhi Morteza Karimzadeh Hamid Reza Bijanzadeh Massoud Amanlou 《Helvetica chimica acta》2012,95(5):788-794
A simple synthesis of N2‐alkyl‐N3‐[2‐(1,3,4‐oxadiazol‐2‐yl)aryl]benzofuran‐2,3‐diamines 5 via a one‐pot four‐component reaction is described (Scheme 1). A mixture of N‐(isocyanoimino)triphenylphosphorane ( 1 ), a 2‐aminobenzoic acid 2 , a 2‐hydroxybenzaldehyde 3 , and an isocyanide 4 in absolute EtOH at room temperature undergoes a smooth reaction to afford 5 in excellent yields (Table). 相似文献
6.
Ramezani Fatemeh Amanlou Massoud Rafii-Tabar Hashem 《Journal of nanoparticle research》2014,16(7):1-9
Three-dimensional (3D) hierarchical rutile TiO2 microspheres composed of nanorods with diameter of several-tens of nanometers, with different morphologies and with average size ranging from 1.3 to 1.8 μm, were successfully synthesized through a surfactant-free solvothermal route. The effects of the solvents n-hexane, chloroform, and cyclohexane on the microstructures of 3D hierarchical TiO2 nanostructures were investigated. Results of scanning electron microscopy showed that 3D sea-urchin like hierarchical TiO2 composed of nanorods with a diameter of ~10 nm can only be prepared in the cyclohexane-water system. The growth mechanism of 3D sea-urchin like hierarchical TiO2 composed of numerous nanorods was further examined and found to differ from the well-known “growth → assembly” mode. The effects of surface tension and polarity of solvents on the morphology and crystal strength of 3D hierarchical TiO2 nanostructure were also investigated. In addition, the prepared 3D sea-urchin like hierarchical TiO2 showed highest photocatalytic activity compared with other 3D hierarchical TiO2 nanostructures in this study and Degussa P25 for the degradation of Rhodamine B solution under UV light irradiation, which could be attributed to its special hierarchical superstructure, the increase of surface catalytic sites and its special composition units. 相似文献
7.
Torabizadeh H Habibi-Rezaei M Safari M Moosavi-Movahedi AA Sharifizadeh A Azizian H Amanlou M 《Applied biochemistry and biotechnology》2011,165(7-8):1661-1673
The structural and storage and functional thermostabilization of endo-inulinase (EC 3.2.1.7) through semi-rational modification of surface accessible lysine residues by pyridoxal-5'-phosphate (PLP) and ascorbate reduction have been explored. Improved stability was observed on modifications in the absence or presence of inulin, which indicates storage or functional thermostabilization, respectively. Comparisons have been made between non-modified and modified enzyme by the determination of Tm as an indicator of structural stability, temperature-dependent half-lives (t1/2), energy barrier of the inactivation process, and thermodynamic parameters (ΔH, ΔG, and ΔS) in a storage thermostability approach. These parameters coincided well with the observed stabilization of the engineered enzyme. Moreover, relative activities with sucrose and inulin were determined for non-modified and modified endo-inulinases at different temperatures. A comparison of the sucrose-to-inulin ratios of the initial rate of hydrolysis as an indicator of substrate specificity revealed about twofold improvement in inulinase versus sucrose activity by enzyme modification. Molecular dynamics simulations and molecular docking approaches were employed to explain the observed structural and functional thermostabilization of endo-inulinase upon modification. We hypothesize the establishment of intramolecular interactions between the covalently attached PLP-Lys381 and Arg526 and Ser376 residues as a representative of modification-originated intramolecular contacts in the modified enzyme. 相似文献
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Mohtavinejad Naser Bitarafan-Rajabi Ahmad Shafiee Ardestani Mehdi Darbandi-Azar Amir Khalaj Ali Ghodrati Atefe Asadi Mehdi Amanlou Massoud 《Journal of Radioanalytical and Nuclear Chemistry》2020,324(2):635-646
Journal of Radioanalytical and Nuclear Chemistry - Myocardial ischemia and infarction represent a major health burden worldwide, but their immediate diagnosis can reduce mortality and healthcare... 相似文献
9.
Sedaghati Saeb Azizian Homa Montazer Mohammad Nazari Mohammadi-Khanaposhtani Maryam Asadi Mehdi Moradkhani Fatemeh Ardestani Mehdi Shafiee Asgari Mohammad Sadegh Yahya-Meymandi Azadeh Biglar Mahmood Larijani Bagher Sadat-Ebrahimi Seyed Esmaeil Foroumadi Alireza Amanlou Massoud Mahdavi Mohammad 《Structural chemistry》2021,32(1):37-48
Structural Chemistry - A novel series of (thio)barbituric-phenoxy-N-phenylacetamide derivatives 7a-l was synthesized and evaluated against Helicobacter pylori urease. The latter assay revealed that... 相似文献
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