New chalcone derivatives as potential antimicrobial and antioxidant agent (original) (raw)
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Synthesis, In-vitro antibacterial and antioxidant activity of chalcone derivatives
GSC Biological and Pharmaceutical Sciences
In the face of the emergence of bacteria resistant to common antibacterials and excessive accumulation of free radicals that can cause several diseases, it is important to look for new antibacterials and antioxidants. The goal of this work was to synthesize three chalcones derivatives by the Claisen-Schmidt condensation and then evaluate their antibacterial and antioxidant activities. The structure of these 3 compounds has been determined by NMR (1H and 13C) spectroscopy. The in vitro antibacterial activity assessed by Microdilution methods, was tested against Gram positive bacteria (Staphylococcus aureus and Bacillus subtilis) and gram negative bacteria (Escherichia coli and Pseudomonas aeruginosa) at different concentrations ranging from 7.82 to 1000 µg/mL. All three synthesized chalcones showed good antibacterial activity against gram positive and negative bacteria used with a range of MIC ranging from 62.50 to 1000 µg/mL. However, the (E)-3-(3, 4-dimethoxyphenyl)-1-(2-hydroxyphe...
STUDY ON SYNTHESIS OF NOVEL CHALCONE THEIR ANTIMICROBIAL ACTIVITY
1-chloro-4-(p-tolyolxy)benzene react with 1-(4-hydrogy phenyl)-ethanone in presence of copper metal as a catalyst gives 1-(4-(4(p-tolyolxy) phenoxy)phenyl )ethanone,this derivatives react with various substituted aldehyde to give corresponding substituted chalcone derivatives (Step-1).Now these derivatives(Step-1).on condensation with Thiourea gives 6-phenyl-4(4-(4-(ptolyolxy)phenoxy)phenyl)-5,6-dinydropyridinmin-2(H)-Thione .(Step-2) Structure elucidation of synthesized. Compound has been made on the basis of element analysis, 1H NMR Spectra studies.
Synthesis and biological activities of some chalcone derivatives
2014
A series of chalcone derivatives were synthesized in order to obtain multipotent antioxidant and antimicrobial agents. These compounds were characterized by IR, and 1H-NMR. All the compounds were screened for in vitro antioxidant activity using DPPH, total reducing power activity (FRAP) based on the ability of compounds to reduce the Fe 3+-TPTZ complex to the Fe 2+ /ferrous, NO scavenging activity, and H2O2 scavenging activity methods. The present results showed that chalcone containing a hydroxyl group attached to one of the aromatic rings showed relatively high ability to reduce the danger of free radicals either directly (DPPH, NO scavenging activity, and FRAP) or indirectly (H2O2 scavenging activity). However, the highest activity was obtained when two hydroxyl groups attached to the two aromatic rings in chalcones. In addition, these compounds have been screened for their antibacterial and antifungal activities against strains of St. aureus, B. subtillis, E. coli, P. auriginose...
Synthesis, characterization, docking studies and bio-efficacy evaluation of novel chalcones
2013
TwoNovel Chalcones(2E)-3-[3-(4-Methylphenyl)-1-phenyl-1H-pyrazol-4-yl]-1-(naphthalen-2-yl)prop-2-en-1-one (1a) and (2E)-3-(1H-Indol-3-yl)-1-(naphthalen-2-yl) prop-2-en-1-one (1b)were synthesized and characterized by using spectral techniques like IR, 1 H NMR, 13 C NMR and GC-MS.In general, these compoundsshowed better antibacterial activity. The newly synthesized compounds were docked with inflammatory protein (Pdb id: 2X6L)from the result it has been clearthat compound (1a)has highgold score.
Asian Journal of Chemistry, 2021
Several chalcones viz. 1,3-diaryl-2-propane-1-one (1a), 3-(4-hydroxy phenyl)-1-phenyl-2-propane-1- one (1b), 3-(4-amino-phenyl)-1-phenyl-2-propane-1-one (1c) and their derivatives 2-ethoxy-4,6- diphenyl-4H-pyran-3-carboxylic acid ethyl ester (2a), 4-(4-hydroxy-phenyl)-7,7-dimethyl-2-phenyl- 4,6,7,8-tetrahydro-chromen-5-one (2b) and 7-(4-amino-phenyl)-5-phenyl-1,5-dihydropyrano[2,3- d]pyrimidine-2,4-dione (2c ) have been synthesized following both conventional and microwave irradiation methods. The structures of the isolated compounds were elucidated on the basis of UV-visible, FTIR, 1H NMR spectral data. The antimicrobial results showed some remarkable facts about the structure–activity relationship, which states that the electronic atmosphere around the chalcone derivative moieties and substituents considerably affect the antimicrobial potential of the synthesized compounds. Theoretical calculation as well as antimicrobial activity of the compounds were also studied.
Spectral Studies and Antimicrobial Screening for Some Novel Chalcones Analogues
International Journal of Current Pharmaceutical Research, 2016
Objective: The present work aim to study the spectral and antimicrobial activity for synthesized chalcones Methods: The synthesized Chalcones were characterized by Physical and spectral methods such as melting point, IR, 1 H-NMR and Mass analysis. The synthesized compounds have been screened for their antimicrobial activity. Results: The biological data showed that compounds III, VII had strong activities against the Staphylococcus aureus, Bacillus subtilis, and Pseudomonas aeruginosa, but not activity against fungus. Conclusion: The main purpose to use an easy and useful method to synthesize biologically active chalcone. Keywords: Chalcones, Synthesis, Spectral studies, Antimicrobial Activity
Synthesis and screening for biological potential of some substituted chalcones
IP Innovative Publication Pvt. Ltd., 2018
The present paper describes the synthesis and antibacterial as well as antioxidant activity of new chalcone derivatives derived from p-chloroacetopheneone. In the present work the reaction of p-chloroacetophenone with different substituted aromatic aldehyde. The newly synthesized chalcones (A-D) were analysed by their spectral data TLC, IR, UV and melting point. These newly synthesized compounds were evaluated for in-vitro antioxidant activity by Diphenyl Picryl Hydrazine (DPPH) model using ascorbic acid as standard and for antimicrobial activity by Cup Plate method on gram positive and gram negative bacterial strain using amoxicillin as standard. Keywords: Chalcone, Antimicrobial, Antioxidant, P-chloroacetophenone, Aromatic aldehyde.
Synthesis, antioxidant activity, and quantitative structure-activity relationship (QSAR) of 25 of chalcone derivatives is reported here. They were synthesized by Claisen-Schmidt reaction and were characterized by FTIR, NMR, and mass spectroscopy. Antioxidant activity is evaluated through four different methods namely, superoxide radical-scavenging, hydrogen peroxide scavenging, reducing power, and DPPH radical-scavenging assays. Generally, compounds with -SCH 3 and -OCH 3 in the para position of the A-ring and -OH in the B-ring were more active than others. In few cases some of the compounds were more active than ascorbic acid or butylated hydroxytoluene. QSAR was developed correlating the antioxidant activity with the structural features of the compounds and the predictive capability of the models was estimated using internal and external validation methods. All the predictions were within the 99% confidence level. Spatial, structural, and lipophilic properties of the compounds determine their antioxidant properties.
Synthesis and antimicrobial activity of some chalcone derivatives
International Journal of ChemTech Research, 2010
In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR, 1 H-NMR spectral data. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.
Synthesis and antimicrobial evaluation of some chalcones
2013
Chalcones are ubiquitous in nature and they are precursors to the flavonoids family. Natural occurring chalcones as well as synthetic chalcone analogues have demonstrated many pharmaceutical effects, including antiinflammatory, anti-oxidant, anti-parasite, and anti-tumor activities. The synthesis of some substituted chalcones was carried out in alcoholic potassium hydroxide at room temperature by Claisen-Schmidt condensation reaction. The compounds were obtained in good yield and were characterized using the combination of IR and NMR spectroscopy. The antibacterial activity of the synthesized compounds was carried out and they were found to be inactive against the tested strains of microorganisms. Contrary to the popular belief that most chalcones do exhibit antimicrobial activity, these substituted chalcones lack such activity.