Synthesis, Characterizations, and Biological Effects Study of Some Quinoline Family

Author(s):  
Messai Amel

The objective of this work is the synthesis of new quinoline molecules which could have some biological activities. This chapter reported a new approach to the synthesis of some quinoline derivatives. The Baylis-Hillman reaction on 2-methoxy-3-formyl quinoléines derivatives have applied in order to obtain Baylis-Hillman adducts. The products are characterized by FTIR, NMR and X-ray single crystal diffraction .Also, a study of the antibacterial activity of the 3-(2-chloro quinoline)-3-hydroxy-2 methylene propanonitrile products synthesized have been explored. This assessment is made by using the disk diffusion method. The results showed that the 3-(2'-chloroquinoline)-3-hydroxy-2-methylenepropanonitril derivatives present a good antibacterial effectiveness against the strains tested Gram-positive and no antibacterial potency was observed against the stains Gram-negative used in the test.

2021 ◽  
Vol 13 (1) ◽  
pp. 106-112
Author(s):  
Sri Kasmiyati ◽  
Elizabeth Betty Elok Kristiani ◽  
Maria Marina Herawati ◽  
Andreas Binar Aji Sukmana

The medicinal plant-derived bioactive compounds have a potential for many biological activities, including antimicrobial activity. Artemisia cina is a medicinal plant from the Compositae family with the potential of having antitumor, antifungal, and antibacterial activity. This study aimed to determine the antibacterial activity and the flavonoid content of A. Cina’s ethyl acetate extract. Plants samples were extracted by ethyl acetate maceration method. Antibacterial activity was tested against Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) by a disk diffusion method using 25, 50, and 100 mg/l extract concentrations. The flavonoid contents (quercetin and kaempferol) were measured using High-Performance Liquid Chromatography. The extracts of diploid and polyploid A. cina displayed some antibacterial activity, with the Gram-negative bacteria being more resistant than the Gram-positive counterpart. However, no significant difference was observed between the diploid and polyploid extracts. As for the flavonoid content, the highest quercetin content (0.5501 mg/ml) was found in the polyploid A. cina (J), while the highest kaempferol content (0.5818 mg/ml) was observed in the diploid A. cina (KJT). Although A. cina is widely grown in Indonesia, compared to other Artemisia species, A. cina has not been widely studied, especially its antibacterial  potential and in related to its flavonoid content and the use of ethyl acetate as the extraction solvent.  This study reveals the potential of A. cina as a natural antibacterial agent. 


2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).


Chemotherapy ◽  
2017 ◽  
Vol 62 (3) ◽  
pp. 194-198 ◽  
Author(s):  
Socorro Leyva-Ramos ◽  
Denisse de Loera ◽  
Jaime Cardoso-Ortiz

Background: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. Methods: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL. Results: MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones. Conclusion: Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity - some even better than the original compound.


2018 ◽  
Vol 2018 ◽  
pp. 1-5 ◽  
Author(s):  
Ali Yetgin ◽  
Kerem Canlı ◽  
Ergin Murat Altuner

In this study, antimicrobial activities of two different samples ofAllium sativumL. from Turkey (TR) (Taşköprü, Kastamonu, Turkey) and China (CN) were determined. A broad spectrum of Gram-negative and Gram-positive bacteria (17 bacteria) including species ofBacillus,Enterobacter,Enterococcus,Escherichia,Klebsiella,Listeria,Pseudomonas,Salmonella, andStaphylococcuswere used for testing antibacterial activity. In addition, antifungal activity againstCandida albicanswas also investigated. Antimicrobial activity was tested by using 3 different processes (chopping, freezing, and slicing by the disk diffusion method). The results showed that TR garlic presented more antimicrobial activity than CN garlic. Mechanism of activity of CN garlic could be proposed to be different from that of TR garlic.


2020 ◽  
Vol 23 (2) ◽  
pp. 51-60
Author(s):  
Ihsan Ikhtiarudin ◽  
Nesa Agistia ◽  
Neni Frimayanti ◽  
Tria Harlianti ◽  
Jasril Jasril

Chalcone analogs have been reported to have a variety of exciting biological activities, such as anticancer, anti-inflammatory, antioxidant, photoprotective, antibacterial, and antidiabetic activities. Therefore, analogs of these compounds have been widely synthesized as intermediate compounds or target molecules in the discovery of bioactive compounds to be applied in the pharmaceutical field. The purpose of this study is to synthesize chalcone analog compounds (E)-1-(4-hydroxyphenyl)-3-(4-methoxyphenyl) prop-2-en-1-on with the microwave irradiation method and explore some of the biological activities of these compounds, including testing the antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method, in vitro sunscreen activity by microplate method, and antibacterial activity by disk diffusion method. DPPH test results indicate that the compound has weak antioxidant activity, with an IC50 value of 300.43 µg/mL. However, the compound showed excellent potential as a UV B and UV A filter at a concentration of 150 µg/mL with a value of %Te of 0.73±0.10% (sunblock), %Tp of 0.07±0.00% (sunblock), SPF value of 21.10±1.46 (ultra-protection) and potentially better than benzophenone-3 as a standard sunscreen. Then, disk diffusion testing showed that the compound had weak antibacterial activity against Staphylococcus aureus and did not show antibacterial activity against Escherichia coli bacteria at test concentrations of 30, 60, and 120 µg/disk.


2021 ◽  
pp. 254-262
Author(s):  
N.S. Lyakhovchenko ◽  
V.Yu. Senchenkov ◽  
A.Yu. Moldavanova ◽  
D.A. Myagkov ◽  
A.A. Sirotin ◽  
...  

The article provides a study of the antibacterial activity of nanostructured copper sulfate in Nacarboxymethyl cellulose on the example of an indigenous strain of the gram-negative bacterium Esherichia coli by the disk-diffusion method. The study revealed that the modification of the active material increases its biocidal properties by 321.34; 121.5; 369.5; 562.6 and 351.7% with an increase in the weight ratio “core : shell” to 1:2 and concentration from 0.5 to 1% in aqueous suspensions.


2020 ◽  
Vol 20 (2) ◽  
pp. 72-77
Author(s):  
Kholhring Lalchhandama ◽  
J. H. Zomuanpuia ◽  
Lai thangliani ◽  
R. L. Malsawmdawngkimi ◽  
Hulianthanga ◽  
...  

Callicarpa arborea and Hemigraphis alternata are two medicinal plants claimed to have antimicrobial property in Indian traditional medicine. The methanol extracts of the stem bark of C. arborea and the leaves of H. alternata were prepared and tested for antibacterial activity using disk diffusion method. Four Gram-negative bacteria such as Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Salmonella typhimurium; and two Gram-positive bacteria such as Micrococcus luteus and Bacillus subtilis were used. C. arborea extract was effective against all the bacteria tested, while H. alternata did not show any inhibitory activity. These findings suggest that C. arborea is a good source of antibacterial compound.


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.


2021 ◽  
Author(s):  
Filippo Fratini ◽  
Margherita Giusti ◽  
Simone Mancini ◽  
Francesca Pisseri ◽  
Basma Najar ◽  
...  

AbstractStaphylococcus aureus and coagulase-negative staphylococci are among the major causes of mastitis in sheep. The main goal of this research was to determine the in vitro antibacterial activity of several essential oils (EOs, n 30), then five of them were chosen and tested alone and in blends against staphylococci isolates. Five bacteria were isolated from episodes of ovine mastitis (two S. aureus and three S. xylosus). Biochemical and molecular methods were employed to identify the isolates and disk diffusion method was performed to determine their antimicrobial-resistance profile. The relative percentage of the main constituents in the tested essential oils and their blends was detected by GC-EIMS analysis. Antibacterial and bactericidal effectiveness of essential oils and blends were evaluated through minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). All of them showed sensitivity to the used antimicrobials. The EOs with the highest antibacterial activity were those belonging to the Lamiaceae family characterized by high concentrations of thymol, carvacrol and its precursor p-cymene, together with cinnamon EO, rich in cinnamaldehyde. In terms of both MIC and MBC values, the blend composed by Thymus capitatus EO 40%, Cinnamomum zeylanicum EO 20%, Thymus serpyllum EO 20% and Satureja montana EO 20% was found to be the most effective against all the isolates. Some essential oils appear to represent, at least in vitro, a valid tool against ovine mastitis pathogens. Some blends showed a remarkable effectiveness than the single oils, highlighting a synergistic effect in relation to the phytocomplex.


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