- Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies
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Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biological activities. Objective: In the current study chalcone derivatives (1-16) w
- Alam, Aftab,Ali, Mahboob,Iqbal, Maryam,Khan, Khalid Mohammed,Khan, Momin,Rafique, Rafaila,Rehman, Ashfaq Ur,Shah, Sana,Wadood, Abdul,Yousaf, Muhammad,Zaman, Khair
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p. 903 - 912
(2021/10/21)
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- Synthesis, in vitro and in silico studies of naphthalene pyrazoline prop-2-en-1-one derivatives
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The synthesized new naphthalene pyrazoline prop-2-en-1-one derivatives (NDPP 1-8) were obtained by the Michael addition reaction of ethyl propanoate, hydrazine hydrate with NPD as a multicomponent scaffold. (E)-1-(naphthalen-3-yl)-3-phenylprop-2-en-1-one (NPD) was formed from 2-acetyl naphthalene and substituted aldehyde via Claisen-Schmidt condensation reaction. The NDPP skeleton structures were confirmed by infrared, 1H & 13C NMR spectral data and elemental analysis. The structure of NDPP compounds was subjected to molecular docking and ADME studies. The result of ADME prediction, compound NDPP 2, which contains electron withdrawing -Cl group has high drug-likeness value 4.21 than the compounds NDPP 4 and 7 which had electron donating CH3 and OCH3 group shows the drug-likeness value 2.62. The NDPP 2 also has high drug score 0.63 than NDPP 4 and NDPP 7 have drug score 0.60 and 0.69, respectively. Docking studies shows that compound NDPP 5 which also contain electron withdrawing NO2 group has good binding affinity value -8.8 Kcal/mol were docked with 1UAG protein. These compounds showed good drug-likeness value 2.25 and drug score 0.65. in vitro Studies have a high inhibition value for the same NO2 substituted derivative. All the compounds have higher binding affinity value than standards binding affinity value.
- Prabha,Raja,Nathiya,Ezhilarasi
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p. 1849 - 1856
(2020/09/02)
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- Facile epoxidation of α, β-unsaturated ketones with urea-2,2-dihydroperoxypropane as a new oxidant
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Abstract: Various aromatic α, β-unsaturated ketones were successfully transformed into their corresponding epoxides using urea-2,2-dihydroperoxypropane as the oxygen source for the first time. The reactions were carried out under mild alkaline conditions at room temperature in high yields and short reaction times. Graphical Abstract: [Figure not available: see fulltext.]
- Khosravi, Kaveh,Naserifar, Shirin
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p. 323 - 328
(2017/01/10)
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- Metal-Free and Efficient Epoxidation of α,β-Unsaturated Ketones with 1,1,2,2-Tetrahydroperoxy-1,2-Diphenylethane as a Powerful Solid Oxidant
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1,1,2,2-Tetrahydroperoxy-1,2-diphenylethane was used for the efficient and metal-free epoxidation of various α,β-unsaturated ketones, carried out under mild alkaline conditions at room temperature.
- Khosravi, Kaveh,Naserifar, Shirin,Mahmoudi, Boshra
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p. 683 - 689
(2017/06/19)
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- Effects of structural and electronic characteristics of chalcones on the activation of peroxisome proliferator-activated receptor gamma
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Chalcones share some structural similarities with GW-1929, a highly-selective and potent agonist for peroxisome proliferator-activated receptor-gamma (PPARγ). In this study, we tested 53 structurally diverse chalcones to identify characteristics essential for PPARγ activation in a GAL4-based transactivation assay. This screen identified several novel chalcone agonists of PPARγ. Our results indicate that chalcones with an electron rich group or sterically large groups such as naphthyl on the carbonyl side tend to activate PPARγ. The absence of any strict structural or electronic requirements suggests that the flexibility of the PPARγ ligand binding pocket may allow binding of diverse chalcones with some preference for a slightly larger electron-rich group on the carbonyl side. We predict that further structure-activity relationship studies on chalcones with naphthalene or electron-rich groups near the carbonyl moiety will lead to the development of more potent PPARγ agonists.
- Schott, Jason Taylor,Mordaunt, Charles Edward,Vargas, Anthony Joseph,Leon, Martin Antonio,Chen, Kevin Hsinwen,Singh, Mandeep,Satoh, Mikiko,Cardenas, Emilio Leal,Maitra, Santanu,Patel, Nilay Vinod,De Lijser, Hubrecht Johan Peter
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p. 229 - 236
(2013/03/14)
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- Synthesis, spectral analysis and in vitro microbiological evaluation of novel ethyl 4-(naphthalen-2-yl)-2-oxo-6-arylcyclohex-3-enecarboxylates and 4,5-dihydro-6-(napthalen-2-yl)-4-aryl-2H-indazol-3-ols
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A series of ethyl 4-(naphthalen-2-yl)-2-oxo-6-arylcyclohex-3- enecarboxylates 8-14 and 4,5-dihydro-6-(naphthalen-2-yl)-4-aryl-2H-indazol-3-ols 15-21 were synthesised and characterised by their spectroscopic data. In vitro microbiological evaluations were carried out for all the newly synthesised compounds 8-21 against clinically isolated bacterial and fungal strains. Compounds 9, 12 and 20 against Staphylococcus aureus, 10, 12, 20 against β-haemolytic streptococcus, 11, 17 against Bacillus subtilis, 12, 16 and 20 against Vibreo cholerae, 13, 16 against Escherichia coli, 13, 16, 18, 19 against Salmonella typhii, 12, 18 against Shigella flexneri, 10 against Salmonella typhii, 10, 13, 17, 18 against Aspergillus flavus, 12, 17, 21 against Aspergillus niger, 12, 15, 17, 18, 20 against Mucor, Rhizopus and Microsporeum gypsuem exhibit potent antimicrobial activity.
- Kanagarajan,Thanusu,Gopalakrishnan
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scheme or table
p. 56 - 66
(2011/10/19)
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- Naphthylchalcones induce apoptosis and caspase activation in a leukemia cell line: The relationship between mitochondrial damage, oxidative stress, and cell death
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In this study, we investigated the effects of 24 chalcone derivatives from 2-naphthylacetophenone toward a lymphoblastic leukemia cell line (L1210). Three compounds, called R7, R13, and R15, presented concentration- and time-dependent cytotoxicity and induced cellular death by apoptosis via mitochondrial injury and oxidative stress. The effects of these compounds appear to occur through different mechanisms because R13 and R7 induced a greater disturbance of mitochondrial potential, and all compounds induced disturbances of cellular ATP content and increased caspase-3 activity before cellular death. These compounds also interfered with antioxidant enzymes activities and GSH content through different mechanisms.
- Winter, Evelyn,Chiaradia, Louise Domeneghini,De Cordova, Clarissa A.S.,Nunes, Ricardo José,Yunes, Rosendo Augusto,Creczynski-Pasa, Tania Beatriz
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experimental part
p. 8026 - 8034
(2011/02/22)
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- Antihyperglycemic activity of naphthylchalcones
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The purpose of the present work was to investigate, following previous works, naphthylchalcones as antihyperglycemic agent in glucose loaded animal model, insulin secretion as well as the action of these compounds on glucose uptake in a target tissue of insulin. The naphthylchalcones were found to have an acute serum glucose-lowering effect in hyperglycemic normal rats. In addition, chalcones 2 and 4 stimulated significantly the insulin secretion induced by glucose. These results suggest that the presence of nitro group and their position in the phenyl rings are responsible for the antihyperglycemic activity of chalcones. Additionally, the effect of chalcones on serum glucose-lowering seems to be a consequence of insulin secretion and these chalcones represent potential compounds with strong antihyperglycemic properties.
- Damazio, Rosangela Guollo,Zanatta, Ana Paula,Cazarolli, Luisa Helena,Chiaradia, Louise Domeneghini,Mascarello, Alessandra,Nunes, Ricardo José,Yunes, Rosendo Augusto,Barreto Silva, Fátima Regina Mena
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experimental part
p. 1332 - 1337
(2010/06/16)
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- Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: Inhibitors of leukotriene B4
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A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene B4 inhibitory activity using human whole blood assay (HWBL) afforded a lead compound, 1
- Deshpande, Anil M.,Argade, Narshinha P.,Natu, Arvind A.,Eckman, Joseph
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p. 1237 - 1240
(2007/10/03)
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- Substituent Effects on Carbonyl Stretching Frequency of β-Naphthyl Styryl Ketones
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The s-cis carbonyl stretching frequencies of two series of substituted β-naphthyl styryl ketones have been measured in chloroform and carbon tetrachloride.One series contains substituents in benzene ring (Series-A) and the other contains substituents in naphthalene ring (Series-B).Substituent effects have been analysed in terms of Hammett equation.Good correlations have been obtained with ?p(+) constants in both the solvents.The low ρ-value for Series-A as compared to that of chalcones is explained on the basis of non-coplanarity of the styryl group and the carbonyl group in the ketones of Series-A.
- Rajasekaran, K.,Gnanasekaran, C.
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