- 2,4-Dinitrophenyl hydrazone derivatives as potent alpha amylase inhibitors
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In our current study thirteen new 2,4-dinitrophenyl hydrazone derivatives 1-13 have been evaluated for alpha amylase activity. The molecular docking results indicate that compounds potentially bind in the catalytic site of the enzyme with excellent result. Molecular Operating Environment (MOE) software was used for docking study. 2,4-Dinitrophenyl hydrazone 1-13 have been obtained under reflux conditions by reacting dinitrophenyl hydrazine in methanol with different aromatic as well as aliphatic aldehydes in the presence of acetic acid act as a catalyst. The current results have shown that compounds 5 (IC50 =12.16μg/mL), 6 (IC50 =15.03μg/mL), and 12 (IC50 =16.42 μg/mL) have been found to be the more potent alpha amylase inhibitors as compared to the standard acarbose (IC50 = 42.47μg/mL). These compounds may provide better leads for alpha amylase inhibitor and further assessment of these compounds can be of great help in the discovery of new antidiabetic drugs.
- Adil, M.,Ahmad, Shakeel,Faisal, Shah,Haq, Mirajul,Hassan, Amir,Idrees, M.,Kainat,Yousaf, Muhammad,Zia, Huma
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p. 277 - 282
(2021/09/28)
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- Correlation analysis of reactivity in the oxidation of substituted benzyl alcohols by benzimidazolium dichromate - A kinetic and mechanistic aspects
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The oxidation of a number of para- and meta-substituted benzyl alcohols by benzimidazolium dichromate (BIDC), in dimethyl sulphoxide, leads to the formation of the corresponding benzaldehydes. The reaction is first order with respect to each BIDC and alcohol. The reaction is catalyzed by hydrogen ions and the dependence has the form kobs = a + b[H+]. The oxidation of [1,1-2H2]benzyl alcohol exhibited the presence of a substantial kinetic isotope effect. The rates of the oxidation of meta-substituted benzyl alcohols correlated best with Taft's σ1 and σR0 constants. The para-substituted compounds exhibited excellent correlation with σ1 and σRBA values. The polar reaction constants are negative. The rate of oxidation of benzyl alcohol was determined in nineteen organic solvents. An analysis of the solvent effect by multiparametric equations indicated the greater importance of the cation-solvating power of the solvents. Suitable mechanisms have been discussed.
- Kumar, Pravesh,Panday, Dinesh,Kothari, Seema
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p. 1207 - 1215
(2020/06/27)
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- Synthesis, structural characterization, and antioxidant activities of 2,4-dinitrophenyl-hydrazone derivatives
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Thirty-two derivatives of 2,4-dinitro phenylhydrazone 1-32 were synthesized by one step reaction and characterized by spectroscopic techniques such as EI-MS and 1H-NMR. Compounds 1-32 were screened for their in vitro antioxidant activities. DPPH radical s
- Ahad, Ghulam,Khan, Momin,Khan, Asif,Ibrahim, Mohammad,Salar, Uzma,Kanwal,Khan, Khalid Mohammed,Perveen, Shahnaz
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p. 961 - 973
(2018/10/02)
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- Preparation, X-ray structure, and reactivity of 2-iodylpyridines: Recyclable hypervalent iodine(V) reagents
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2-Iodylpyridine and four examples of 3-alkoxy-2-iodylpyridines were prepared by oxidation of the respective 2-iodopyridines with 3,3-dimethyldioxirane. Structures of 2-iodylpyridine, 2-iodyl-3- isopropoxypyridine, and 2-iodyl-3-propoxypyridine were established by single-crystal X-ray diffraction analysis. 2-Iodyl-3-propoxypyridine has moderate solubility in organic solvents (e.g., 1.1 mg/mL in acetonitrile) and can be used as a recyclable reagent for oxidation of sulfides and alcohols. The reduced form of this reagent, 2-iodo-3-propoxypyridine, can be effectively separated from the reaction mixture by treatment with diluted sulfuric acid and recovered from the acidic aqueous solution by adding aqueous sodium hydroxide.
- Yoshimura, Akira,Banek, Christopher T.,Yusubov, Mekhman S.,Nemykin, Victor N.,Zhdankin, Viktor V.
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p. 3812 - 3819
(2011/07/08)
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- Structure-Reactivity correlation in the oxidation of substituted benzaldehydes by tetraethylammonium chlorochromate
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Oxidation of 36 monosubstituted benzaldehydes by tetraethylammonium chlorochromate in dimethyl sulphoxide, leads to the formation of corresponding benzoic acids. The reaction is of first order with respect to chlorochromate and aldehydes. The reaction is promoted by H+; the H+ dependence has the form kobs = a + b[H+]. The oxidation of duteriated benzaldehyde exhibits substantial primary kinetic isotope effect. The reaction was studied in 19 different organic solvents and the effect of solvent was analyzed using Taft's and Swain's multiparametric equations. The rates of the oxidation of para- and meta-substituted benzaldehydes showed excellent correlation in terms of Charton's triparametric LDR equation, whereas the oxidation of ortho-substituted benzaldehydes were correlated well with tetraperametric LDRS equation. The oxidation of para-substituted benzaldehydes is more susceptible to the delocalized effect than is the oxidation of ortho- and meta- substituted compounds, which display a greater dependence on the field effect. The positive value of h suggests the presence of an electron-deficient reaction centre in the rate-determining step. The reaction is subjected to steric acceleration by the orthosubstituents. A suitable mechanism has been proposed.
- Gehlot,Prasadrao,Sharma
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experimental part
p. 1173 - 1178
(2012/01/05)
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- Characterization and thermal analysis of mercury complexes containing intermolecular N→Hg interactions
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The new mercury (II) compounds with (L1), (L2) of the general formula [Hg(L)2], have been synthesized and characterized by elementalanalysis, electronic and IR, Raman spectra and thermogravimetry and differential thermogravimetry tec
- Sahebalzamani, Hajar,Salimi, Farshid,Ghammamy, Shahriare
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experimental part
p. S502-S508
(2012/06/15)
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- Effect of the micellar surfactant nanoreactors on the reactions of 2,4-dinitrophenylhydrazine with some aldehydes
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By thermogravimetry, the IR and electronic spectroscopy physicochemical characteristics of systems including aromatic aldehydes, 2,4- dinitrophenylhydrazine, and a surfactant were investigated. Selective solubilization effect of the cationic surfactant (c
- Doronin,Chernova,Burmistrova
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p. 903 - 907
(2008/12/20)
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- Highly efficient RuCl3-catalyzed disproportionation of (diacetoxyiodo)benzene to iodylbenzene and iodobenzene; leading to the efficient oxidation of alcohols to carbonyl compounds
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(Diacetoxyiodo)benzene (DIB) selectively oxidizes primary and secondary alcohols to the respective carbonyl compounds in the presence of RuCl3 (0.8-1.0 mol %) at room temperature in aqueous acetonitrile. This reaction proceeds via an initial instantaneous Ru-catalyzed disproportionation of DIB to iodobenzene and iodylbenzene with the latter acting as the actual stoichiometric oxidant toward alcohols.
- Yusubov, Mekhman S.,Chi, Ki-Whan,Park, Joo Yeon,Karimov, Rashad,Zhdankin, Viktor V.
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p. 6305 - 6308
(2007/10/03)
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- In situ alcohol oxidation-protection reactions
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The one-pot conversion of primary and secondary alcohols into phenylhydrazones and 2,4-dintrophenylhydrazones is reported using chromium trioxide supported on silica gel and phenylhydrazines or 2,4- dintrophenylhydrazines under solvent-free conditions. This oxidation arylhydrazone formation reaction has been applied to a range of aliphatic and benzylic alcohols. Copyright Taylor & Francis, Inc.
- Kiasat,Kazemi,Nourbakhsh
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p. 1555 - 1558
(2007/10/03)
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- Dowex polymer-mediated protection of carbonyl groups
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Dowex (strongly acidic cationic exchange resin) polymer is employed as solid acid catalyst for the clean and less hazardous protection of carbonyl compounds as phenylhydrazones and 2,4-dintrophenylhydrazones in ethanol under reflux conditions. The reactions proceed very smoothly and the yields of the derivatives are excellent. Copyright Taylor & Francis, Inc.
- Niknam, Khodabakhsh,Kiasat, Ali Reza,Karimi, Sadegh
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p. 2231 - 2236
(2007/10/03)
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- H2SO4/SiO2 as an efficient catalyst for the preparation of phenylhydrazones and 2,4-dinitrophenylhydrazones under solvent-free conditions
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H2SO4 mixed with silica gel (1:1) by weight produces a white powder which is an effective catalyst for the conversion of carbonyl compounds to their corresponding phenylhydrazones and 2,4-dintrophenylhydrazones under solvent-free conditions.
- Kiasat, Ali Reza,Kazemi, Foad,Nourbakhsh, Kazem
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p. 569 - 573
(2007/10/03)
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- Kinetics and Mechanism of the Oxidation of Substituted Benzylamines by N-Chlorosuccinimide
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The oxidation of ortho-, meta-, and para-substituted benzylamines by N-chlorosuccinimide (NCS), to the corresponding benzaldehydes, is first-order with respect to NCS and the amine.The pH dependence of the reaction rate suggests that the unprotonated benzylamine is the reductant.There is no effect of added succinimide.NCS itself has been postulated as the reactive oxidising species.The oxidation of benzylamine exhibited a substantial primary kinetic isotope effect (kH/kD=6.20).The rates of oxidation of the meta- and para-substituted benzylamines were separately correlated in Taft and Swain's dual substituent parameter equations.For the para-substituted compounds, the best correlation is obtained with ?I and ?R+ values; meta-substituted compounds correlate with ?I and ?R0 values.The reaction constants have negative values.The oxidation rates of the ortho-substituted compounds yield an excellent correlation in a triparametric equation involving Taft's ?I and ?R+ values and Charton's steric parameter, V.A mechanism involving transfer of a hydride ion from the amine to the oxidant in the rate-determining step is proposed.
- Banerji, Kalyan K.
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p. 1015 - 1020
(2007/10/02)
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- Kinetics and Mechanism of the Oxidation of Substituted Benzyl Alcohols by Lead Tetraacetate
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The kinetics of the oxidation of benzyl alcohol to benzaldehyde by lead tetraacetate have been studied in benzene solution both in the absence and presence of pyridine.The values of the reaction constant ρ for the reactions in the absence and presence of pyridine at 303 K are -1.13 and -1.92 respectively.The activation enthalpies and entropies of the nine compounds are linearly related.The oxidation of α,α-dideuteriobenzyl alcohol indicated presence of a primary kinetic isotope effect.The reaction does not induce polymerisation of acrylonitrile.Probable mechanisms have been suggested.
- Bhatia, Indu,Banerji, Kalyan K.
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p. 1076 - 1092
(2007/10/02)
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