scholarly journals Synthesis and Spectral Characterisation of (E)-3-(3-(4 (Dimethylamino)Phenyl)Acrylo-yl)-4-Hydroxy-2H-Chromen-2-One and Their Antibacterial Activity and Acetylcholinesterase Inhibition

2021 ◽  
Vol 2021 ◽  
pp. 1-15
Author(s):  
Ichraf Slimani ◽  
Naceur Hamdi ◽  
Sadeq M. Al-Hazmy ◽  
Ibrahim A. Alhagri ◽  
El-Zeiny M. Ebeid ◽  
...  
Keyword(s):  
Antimicrobial Properties ◽  
Emission Spectra ◽  
Coumarin Derivative ◽  
Dielectric Constants ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Enhanced Fluorescence ◽  
Spectral Characterisation ◽  
Molecular Rigidity ◽  
Fluorescent Stain

A new coumarin derivative, (E)-3-(3-(4-(dimethylamino) phenyl) acrylo-yl)-4-hydroxy-2H-chromen-2-one (3), was synthesized by the condensation of 3-acetyl-4-hydroxycoumarin (1) with 4-N,N-dimethylaminobenzaldehyde (2) in the presence of piperidine in ethanol. The structure of the synthesized compound was characterized using spectroscopic data (IR and 1H NMR) and elemental analysis. The antimicrobial properties and acetylcholinesterase inhibition activity (AChEI) of coumarin 3 were investigated, with the highest observed AChEI activity providing 48.25% inhibition. The electronic absorption and emission spectra revealed that 3 exists as two, main keto-enol tautomers. The ratios of these tautomers in both protic and aprotic solvents with different polarities and dielectric constants were calculated. The fluorescence of coumarin 3 was enhanced upon increasing the medium viscosity, which was due to the resultant molecular rigidity. This criterion was further investigated using DNA, whereby 3 showed enhanced fluorescence upon its uptake in DNA grooves and was therefore tested as a novel DNA fluorescent stain.

Fluorescence of the Complexes of 2-Methylnaphthoate and 2-Hydroxypropyl-α-, -β-, and -γ-Cyclodextrins in Aqueous Solution

2002 ◽  
Vol 56 (12) ◽  
pp. 1579-1587 ◽  
Author(s):  
Antonio Di Marino ◽  
Franscisco Mendicuti
Keyword(s):  
Aqueous Solution ◽  
Fluorescence Anisotropy ◽  
Intensity Ratio ◽  
Driving Forces ◽  
Emission Spectra ◽  
Formation Constants ◽  
Dielectric Constants ◽  
Additional Information ◽  
Fluorescence Techniques ◽  
Naturally Occurring

Fluorescence techniques were employed to study the inclusion complexes of 2-methylnaphthoate (MN) with 2-hydroxypropyl-α-cyclodextrin (αHPCD), 2-hydroxypropyl-β-cyclodextrin (βHPCD), and 2-hydroxypropyl-γ-cyclodextrin (γHPCD). Emission spectra of MN show two vibronic bands whose intensity ratio R is very sensitive to the polarity of the medium. The stoichiometry and formation constants of these complexes were investigated by obtaining R as a function of the cyclodextrin (CD) concentration. Results showed identical stoichiometry (1/1) for the three MN/αHPCD, MN/β-HPCD, and MN/γHPCD complexes. Formation constants at 25 °C were 780 ± 15, 2700 ± 130, and 165 ± 10 M−1, respectively. ΔH0 and ΔS0 were obtained from linear van't Hoff plots. Results reveal that the complexation of MN with αHPCD is enthalpy driven. With βHPCD, both the entropy and enthalpy terms favor the process, whereas the formation of the complex with γHPCD is entropically governed. The extrapolation of R at infinite CD concentration allows us to estimate the effective dielectric constants of the inner CD cavities, which are around 50, but which differ from their counterparts, the naturally occurring α-, β-, and γ-CDs. Fluorescence anisotropy, quencher lifetimes, and average lifetimes can also give additional information about the structure and driving forces accompanying the formation of such complexes.

Synthesis and bioactivity of novel C2-glycosyl triazole derivatives as acetylcholinesterase inhibitors

2017 ◽  
Vol 23 (3) ◽  
pp. 231-236 ◽  
Author(s):  
Long Yin ◽  
Lei Wang ◽  
Xiu-Jian Liu ◽  
Feng-Chang Cheng ◽  
Da-Hua Shi ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Sodium Hydroxide ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity ◽  
Triazole Derivatives ◽  
Inhibitory Activities ◽  
Ellman’S Method

AbstractNew C2-glycosyl triazole derivatives 6a–l were synthesized by cyclization of glycosyl acylthiosemicarbazides 5 in refluxing 3 N sodium hydroxide aqueous solution. Substrates 5 were obtained by the reaction of glycosyl isothiocyanate 3 with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of compounds 6 were tested by Ellman’s method. Compounds that exhibited over 85% inhibition were subsequently evaluated for the IC50 values. Compound 6f possesses the best acetylcholinesterase-inhibition activity with IC50 of 1.46±0.25 μg/mL.

Antioxidant, antiproliferative, and acetylcholinesterase inhibition activity of amino alcohol derivatives from 1,4-naphthoquinone

2020 ◽  
Vol 29 (11) ◽  
pp. 1986-1999
Author(s):  
Arturo Estolano-Cobián ◽  
Eduardo Noriega-Iribe ◽  
Laura Díaz-Rubio ◽  
José M. Padrón ◽  
Mirna Brito-Perea ◽  
...  
Keyword(s):  
Amino Alcohol ◽  
Acetylcholinesterase Inhibition ◽  
Inhibition Activity

scholarly journals Purification of Bioactive Peptide with Antimicrobial Properties Produced by Saccharomyces cerevisiae

Foods ◽  
2020 ◽  
Vol 9 (3) ◽  
pp. 324 ◽  
Author(s):  
Shayma Thyab Gddoa Al-sahlany ◽  
Ammar Altemimi ◽  
Alaa Al-Manhel ◽  
Alaa Niamah ◽  
Naoufal Lakhssassi ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Antimicrobial Properties ◽  
Antibacterial Peptide ◽  
Inhibition Activity ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Viable Cells ◽  
Ph Range

A variety of organisms produce bioactive peptides that express inhibition activity against other organisms. Saccharomyces cerevisiae is considered the best example of a unicellular organism that is useful for studying peptide production. In this study, an antibacterial peptide was produced and isolated from Saccharomyces cerevisiae (Baker’s yeast) by an ultrafiltration process (two membranes with cut-offs of 2 and 10 kDa) and purified using the ÄKTA Pure 25 system. Antibacterial peptide activity was characterized and examined against four bacterial strains including Gram-positive and Gram-negative bacteria. The optimum condition for yeast growth and antibacterial peptide production against both Escherichia. coli and Klebsiella aerogenes was 25–30 °C within a 48 h period. The isolated peptide had a molecular weight of 9770 Da, was thermostable at 50–90 °C for 30 min, and tolerated a pH range of 5–7 at 4 °C and 25 °C during the first 24 h, making this isolated antibacterial peptides suitable for use in sterilization and thermal processes, which are very important aspect in food production. The isolated antibacterial peptide caused a rapid and steady decline in the number of viable cells from 2 to 2.3 log units of gram-negative strains and from 1.5 to 1.8 log units of gram-positive strains during 24 h of incubation. The isolated antibacterial peptide from Saccharomyces cerevisiae may present a potential biopreservative compound in the food industry exhibiting inhibition activity against gram-negative and gram-positive bacteria.

scholarly journals Chemical Composition and Acetylcholinesterase Inhibition Activity of Volatile Oil from Leaves of Arbutus unedo L. from Croatia

2019 ◽  
Vol 31 (5) ◽  
pp. 1110-1112
Author(s):  
O. Politeo ◽  
I. Ercegovic
Keyword(s):  
Chemical Composition ◽  
Volatile Oil ◽  
Acetylcholinesterase Inhibition ◽  
Nonanoic Acid ◽  
Inhibition Activity ◽  
Ache Inhibition ◽  
Arbutus Unedo ◽  
Lower Quantity

The volatile oil from leaves of Arbutus unedo L. from Croatia was subjected to chemical composition and acetylcholinesterase inhibition activity. The tested volatile oil was dominated by nonterpene compounds, with (E)-2-decenal, nonanal, nonanoic acid and octanol as main compounds. Terpene compounds were identified in lower quantity, with linalool and α-terpineol as main ones. Results showed low to moderate acetylcholinesterase (AChE) inhibition potential of tested oil, for tested concentration of 1 mg/mL.

Study on a New Coumarin Derivative as Fluorescent Probe for Hg2+ Ions

2014 ◽  
Vol 904 ◽  
pp. 99-102
Author(s):  
Hong Qi Li ◽  
Zhen Chen ◽  
Hao Chen ◽  
Jia Wei Zhang ◽  
Yan Tai Chen ◽  
...  
Keyword(s):  
Metal Ions ◽  
Fluorescent Probe ◽  
Fluorescence Emission ◽  
Emission Spectra ◽  
Coumarin Derivative ◽  
Emission Peak ◽  
Fluorescence Emission Spectra ◽  
Maximum Emission ◽  
H Nmr ◽  
C Nmr

A new coumarin derivative L was synthesized and characterized by1H NMR,13C NMR, IR and mass spectrum. UV-Vis and fluorescence emission spectra of L without or with different anions (NO2, F, Cl, HSO3, HSO4, AcO or NO3) or metal ions were measured, which showed while addition of anions or metal ions Mg2+, Zn2+, Ca2+, Cu2+, Ni2+, Co2+, Fe3+or Al3+led to decrease in intensity of the maximum emission peak at about 480 nm, addition of Hg2+ions caused increase in intensity of the maximum emission peak, suggesting that L may act as a fluorescent probe for detection of Hg2+ions.

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