Regioselective synthesis, antimicrobial evaluation and theoretical studies of 2-styryl quinolines

2015 ◽  
Vol 13 (5) ◽  
pp. 1347-1357 ◽  
Author(s):  
Ahmed Kamal ◽  
Abdul Rahim ◽  
Sd Riyaz ◽  
Y. Poornachandra ◽  
Moku Balakrishna ◽  
...  

2-Styryl quinolines have been synthesized regioselectively from 2-methyl-quinoline using NaOAc in water acetic acid binary solvents and evaluated for their antibacterial activity against both Gram-positive and Gram-negative strains.

Author(s):  
Sushma Vashisht ◽  
Manish Pal Singh ◽  
Viney Chawla

The methanolic extract of the resin of Shorea robusta was subjected to investigate its antioxidant and antibacterial properties its utility in free radical mediated diseases including diabetic, cardiovascular, cancer etc. The methanol extract of the resin was tested for antioxidant activity using scavenging activity of DPPH (1,1-diphenyl-2-picrylhydrazil) radical method, reducing power by FeCl3 and antibacterial activity against gram positive and gram negative bacteria using disc diffusion method. The phytochemical screening considered the presence of triterpenoids, tannins and flavoniods. Overall, the plant extract is a source of natural antioxidants which might be helpful in preventing the progress of various oxidative stress mediated diseases including aging. The half inhibition concentration (IC50) of resin extract of Shorea robusta and ascorbic acid were 35.60 µg/ml and 31.91 µg/ml respectively. The resin extract exhibit a significant dose dependent inhibition of DPPH activity. Antibacterial activity was observed against gram positive and gram negative bacteria in dose dependent manner.Key Words: Shorea robusta, antioxidant, antibacterial, Disc-diffusion, DPPH.


Author(s):  
Elaf Ayad Kadhem ◽  
Miaad Hamzah Zghair ◽  
Sarah , Hussam H. Tizkam, Shoeb Alahmad Salih Mahdi ◽  
Hussam H. Tizkam ◽  
Shoeb Alahmad

magnesium oxide nanoparticles (MgO NPs) were prepared by simple wet chemical method using different calcination temperatures. The prepared NPs were characterized by Electrostatic Discharge (ESD), Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD). It demonstrates sharp intensive peak with the increase of crystallinty and increase of the size with varying morphologies with respect to increase of calcination temperature. Antibacterial studies were done on gram negative bacteria (E.coli) and gram positive bacteria (S.aureus) by agar disc diffusion method. The zones of inhibitions were found larger for gram positive bacteria than gram negative bacteria, this mean, antibacterial MgO NPs activity more active on gram positive bacteria than gram negative bacteria because of the structural differences. It was found that antibacterial activity of MgO NPs was found it has directly proportional with their concentration.


2020 ◽  
Vol 16 (4) ◽  
pp. 481-488
Author(s):  
Heli Sanghvi ◽  
Satyendra Mishra

Background: Curcumin, one of the most important pharmacologically significant natural products, has gained significant consideration among scientists for decades since its multipharmacological activities. 1, 3-Dicarbonyl moiety of curcumin was found to be accountable for the rapid degradation of curcumin molecule. The aim of present work is to replace 1, 3-dicarbonyl moiety of curcumin by pyrazole and phenylpyrazole derivatives with a view to improving its stability and to investigate the role of substitution in N-phenylpyrazole curcumin on its antibacterial activity against both Gram-positive as well as Gram-negative bacteria. Methods: Pyrazole derivatives of curcumin were prepared by heating curcumin with phenyhydrazine/ substituted phenyhydrazine derivatives in AcOH. The residue was purified by silica gel column chromatography. Structures of purified compounds were confirmed by 1H NMR and Mass spectroscopy. The synthesized compounds were evaluated for their antibacterial activity by the microdilution broth susceptibility test method against gram positive (S. aureus) and gram negative (E. coli). Results: Effects of substitution in N-phenylpyrazole curcumin derivatives against S. aureus and E. coli were studied. The most active N-(3-Nitrophenylpyrazole) curcumin (12) exhibits twenty-fold more potency against S. aureus (MIC: 10μg/mL)) and N-(2-Fluoroophenylpyrazole) curcumin (5) fivefold more potency against E. coli (MIC; 50 μg/mL) than N-phenylpyrazole curcumin (4). Whereas, a remarkable decline in anti-bacterial activity against S. aureus and E. coli was observed when electron donating groups were incorporated in N-phenylpyrazole curcumin (4). Comparative studies of synthesized compounds suggest the effects of electron withdrawing and electron donating groups on unsubstituted phenylpyrazole curcumin (4). Conclusion: The structure-activity relationship (SAR) results indicated that the electron withdrawing and electron donating at N-phenylpyrazole curcumin played key roles for their bacterial inhibitory effects. The results of the antibacterial evaluation showed that the synthesized pyrazole derivatives of curcumin displayed moderate to very high activity in S. aureus. In conclusion, the series of novel curcumin derivatives were designed, synthesized and tested for their antibacterial activities against S. aureus and E. coli. Among them, N-(3-Nitrophenylpyrazole curcumin; 12) was most active against S. aureus (Gram-positive) and N-(2-Fluoroophenylpyrazole) curcumin (5) against E. coli (Gram-negative) bacteria.


Materials ◽  
2020 ◽  
Vol 13 (21) ◽  
pp. 4715
Author(s):  
Adam Kubiak ◽  
Marta Kubacka ◽  
Elżbieta Gabała ◽  
Anna Dobrowolska ◽  
Karol Synoradzki ◽  
...  

The TiO2-Fe3O4 composite materials were fabricated via the hydrothermal-assisted technique. It was determined how the molar ratio of TiO2 to Fe3O4 influences the crystalline structure and morphology of the synthesized composite materials. The effect of the molar ratio of components on the antibacterial activity was also analyzed. On the basis of XRD patterns for the obtained titanium(IV) oxide-iron(II, III) oxide composites, the two separate crystalline forms—anatase and magnetite —were observed. Transmission electron microscopy revealed particles of cubic and tetragonal shape for TiO2 and spherical for Fe3O4. The results of low-temperature nitrogen sorption analysis indicated that an increase in the iron(II, III) oxide content leads to a decrease in the BET surface area. Moreover, the superparamagnetic properties of titanium(IV) oxide-iron(II, III) oxide composites should be noted. An important aim of the work was to determine the antibacterial activity of selected TiO2-Fe3O4 materials. For this purpose, two representative strains of bacteria, the Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus, were used. The titanium(IV) oxide-iron(II, III) oxide composites demonstrated a large zone of growth inhibition for both Gram-positive and Gram-negative bacteria. Moreover, it was found that the analyzed materials can be reused as antibacterial agents in three consecutive cycles with good results.


2020 ◽  
Author(s):  
Rekhachandran Prasanna Ramachandran ◽  
Archana Valliyamma ◽  
Nitha Nellithanathu Thomas ◽  
Mangalaraja Ramalinga Viswanathan ◽  
Boby Theophilofe Edwin ◽  
...  

CrystEngComm ◽  
2018 ◽  
Vol 20 (24) ◽  
pp. 3353-3362 ◽  
Author(s):  
Ian R. Colinas ◽  
Mauricio D. Rojas-Andrade ◽  
Indranil Chakraborty ◽  
Scott R. J. Oliver

Two novel Zn-based coordination polymers with unique structural properties display an exceptional antibacterial activity against Gram-positive and Gram-negative bacteria.


2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.


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