62918-41-6Relevant academic research and scientific papers
Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies
Alam, Aftab,Ali, Mahboob,Iqbal, Maryam,Khan, Khalid Mohammed,Khan, Momin,Rafique, Rafaila,Rehman, Ashfaq Ur,Shah, Sana,Wadood, Abdul,Yousaf, Muhammad,Zaman, Khair
, p. 903 - 912 (2021/10/21)
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
Synthesis, in vitro and in silico studies of naphthalene pyrazoline prop-2-en-1-one derivatives
Prabha,Raja,Nathiya,Ezhilarasi
, p. 1849 - 1856 (2020/09/02)
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.
Synthesis, Biological Activity and Action Mechanism Study of Novel Chalcone Derivatives Containing Malonate
Guo, Tao,Xia, Rongjiao,Liu, Tingting,Peng, Feng,Tang, Xuemei,Zhou, Qing,Luo, Hui,Xue, Wei
, (2020/03/13)
A series of novel chalcone malonate derivatives were synthesized and their antibacterial and antiviral activities were evaluated. All target compounds were characterized by spectral data. The results of antimicrobial bioassay showed that one compound (die
Facile epoxidation of α, β-unsaturated ketones with urea-2,2-dihydroperoxypropane as a new oxidant
Khosravi, Kaveh,Naserifar, Shirin
, p. 323 - 328 (2017/01/10)
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.]
Metal-Free and Efficient Epoxidation of α,β-Unsaturated Ketones with 1,1,2,2-Tetrahydroperoxy-1,2-Diphenylethane as a Powerful Solid Oxidant
Khosravi, Kaveh,Naserifar, Shirin,Mahmoudi, Boshra
, p. 683 - 689 (2017/06/19)
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.
Silver-catalyzed double-decarboxylative cross-coupling of α-keto acids with cinnamic acids in water: A strategy for the preparation of chalcones
Zhang, Ning,Yang, Daoshan,Wei, Wei,Yuan, Li,Nie, Fafa,Tian, Laijin,Wang, Hua
, p. 3258 - 3263 (2015/03/30)
A silver-catalyzed double-decarboxylative protocol has been proposed for the construction of chalcone derivatives via cascade coupling of substituted α-keto acids with cinnamic acids under the mild aqueous conditions. The developed method for constructing C-C bonds via double-decarboxylative reactions is efficient, practical, and environmentally benign by using the readily available starting materials. It should provide a promising synthesis candidate for the formation of diverse and useful chalcone derivatives in the fields of synthetic and pharmaceutical chemistry.
Effects of structural and electronic characteristics of chalcones on the activation of peroxisome proliferator-activated receptor gamma
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
, p. 229 - 236 (2013/03/14)
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.
Aldol condensations of a variety of different aldehydes and ketones under ultrasonic irradiation using poly(N-vinylimidazole) as a new heterogeneous base catalyst under solvent-free conditions in a liquid-solid system
Khaligh, Nader Ghaffari,Mihankhah, Taraneh
, p. 2167 - 2173 (2014/01/06)
An ultrasound-assisted aldol condensation reaction has been developed for a range of ketones with a variety of aromatic aldehydes using poly(N-vinylimidazole) as a solid base catalyst in a liquid-solid system. The catalyst can be recovered by simple filtration and reused at least 10 times without any significant reduction in its activity. The reaction is also amenable to the large scale, making the procedure potentially useful for industrial applications.
Synthesis and antimicrobial activities of new 4,6-diaryl- 4,5-dihydro-3-hydroxy-2H-indazoles
Amutha, Parasuraman,Nagarajan, Samuthira
experimental part, p. 428 - 432 (2012/06/30)
A series of new 4,6-diaryl-4,5-dihydro-3-hydroxy-2H-indazoles 5a-5k were synthesized by the cyclization of ethyl 2-oxo-4,6-diarylcyclohex-3-ene carboxylates 4a-4k. The compounds were characterized by IR, 1H NMR, 13C NMR, 2D NMR, and elemental analysis. The synthesized compounds were evaluated for in vitro antibacterial and antifungal activities against Staphylococcus aureus, Escherichia coli, Salmonella typhimurium, Pseudomonas aeruginosa, Candida albicans, Aspergillus niger, Aspergillus flavus, and Rhizopus sp. Most of the compounds exhibited good activity against the tested organisms. Copyright
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
Kanagarajan,Thanusu,Gopalakrishnan
scheme or table, p. 56 - 66 (2011/10/19)
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.
