scholarly journals An Efficient Synthesis of Novel 3-[(Heteroaryl-2-ylimino)-methyl]-4-hydroxy-chromen-2-ones and Analogue of Tetrazole Derivatives and Their Antibacterial Activity

Molbank ◽  
10.3390/m1303 ◽  
2021 ◽  
Vol 2021 (4) ◽  
pp. M1303
Author(s):  
Ramiz Hoti ◽  
Hamit Ismaili ◽  
Veprim Thaçi ◽  
Gjyle Mulliqi-Osmani ◽  
Malësore Pllana-Zeqiri ◽  
...  

Synthesis of a series of the substituted [(pyridinyl and pyrimidin-2-ylimino)-ethyl]-4-hydroxy-chromen-2-ones and their tetrazole derivates is presented in this study. By catalytic condensation of 4-hydroxy-3-acetylcoumarine 2 and 2-aminopyridines 3(a-d), 3-[(pyridin-2-ylimino)-ethyl]-4-hydroxy-chromen-2-ones 4(a-d) are synthesized in high yield. During the condensation reaction of 2 and 4-amino-2,6-dihydroxypyrimidine 3e, 3-[1-(2,6-Dihydroxy-pyrimidin-4-ylimino)-ethyl]-4-hydroxy-chromen-2-one 4e as condensation products is synthesized. In following series, by cyclization reactions of compounds 4 (a-e) with sodium azide, analogue 3-substituted pyridin-2-yl and pyrimidin-2-yl-5-methyl-2,5-dihydro-1H-tetrazol-5-yl]-4-hydroxy-chromen-2-one 5(a-e) are synthesized the products. Structural characterization of the synthesized products is done on the basis of spectrometric data. Antibacterial activity of the compounds 4(a-e) and 5(a-e) against S. aureus, E. coli and Klebsiella was examined by measuring the inhibition zones around the disks marked with the corresponding products solution. The impact of substitutions in antimicrobial is also explored. Compounds with polar groups have shown significant antibacterial activity against these microorganisms.

2021 ◽  
pp. 0887302X2110094
Author(s):  
V. Mamtha ◽  
H. N. Narasimha Murthy ◽  
V. Pujith Raj ◽  
Prashantha Tejas ◽  
C. S. Puneet ◽  
...  

Antibacterial activity and fire retardation are equally desired for protective clothing. For achieving this, AgNP and MgO are independently researched as nanofillers in Polyurethane based electrospun nanofibers and their synergistic effect is scarcely addressed. This article reports synthesis and characterization of MgO of 70.01 nm and AgNP of 51 to 76 nm by solution combustion and hydrothermal routes respectively and their incorporation in electrospinning of Polyurethane. Flow rate 1 ml/hr, applied voltage 13 kV, tip to collector distance 15 cm were adopted for the electrospinning. Nanofibers of 65 nm were obtained for PU/MgO (3 wt. %) and 106 nm for PU/MgO (3 wt. %)/Ag (1 wt. %). Addition of MgO increased the melting point, after flame time and afterglow time. Incorporation of AgNP improved antibacterial activity. PU/MgO/Ag (2 wt. %) exhibited zone of inhibition of 2.1 cm and 3 cm against E. Coli and S. Aureus, respectively.


2017 ◽  
Vol 13 (1) ◽  
pp. 95
Author(s):  
Susy Yunita Prabawati ◽  
Arifah Khusnuryani ◽  
Khamidinal Khamidinal

<p>The aims of this study was to synthesize a compound of 3-methoxy-4-hydroxychalcone through Claisen-Schmidt condensation with grinding technique (solvent-free). Vanillin, acetophenone and 60 % NaOH catalyst used in this synthesis. Characterization of products was done with a spectrophotometer FTIR and <sup>1</sup>H-NMR spectrometer. The  product was obtained as a orange solid which has a melting point at    58 - 59 ˚C. Identification of the product by IR spectrophotometer showed the absorption of  C=C in the wavenumber of 1496.76 cm<sup>-1</sup> which confirmed that the hydration reaction of chalcone had occurred. Analysis using <sup>1</sup>H-NMR spectrometer also showed the proton of the CH=CH appearing on chemical shift (δ) 7.99 ppm. The antibacterial activity test showed that the compounds of 3-methoxy-4- hydroxychalcone has a potential as an antibacterial against bacteria <em>E. coli</em> and <em>B. subtilis</em>.</p>


2020 ◽  
Vol 4 (2) ◽  

Metal nanoparticles possess an extensive scientific and technological significance due to their unique physiochemical properties and their potential applications in different fields like medicine. Silver and gold nanoparticles have shown to have antibacterial and cytotoxic activities. Conventional methods used in the synthesis of the metal nanoparticles involve use of toxic chemicals making them unsuitable for use in medical field. In our continued effort to explore for simple and eco-friendly methods to synthesize the metal nanoparticles, we here describe synthesis and characterization of gold and silver nanoparticles using Gonaderma lucidum, wild non-edible medicinal mushroom. G. lucidum mushroom contain bioactive compounds which can be involved in the reduction, capping and stabilization of the nanoparticles. Antibacterial activity analysis was done on E. coli and S. aureus. The synthesis was done on ultrasonic bath. Characterization of the metal nanoparticles was done by UV-VIS., High Resolution Transmission Electron Microscope (HRTEM) and FTIR. HRTEM analysis showed that both silver and gold nanoparticles were spherical in shape with an average size of 15.82±3.69 nm for silver and 24.73±5.124nm for gold nanoparticles (AuNPs). FTIR analysis showed OH and -C=C- stretching vibrations, an indication of presence of functional groups of biomolecules capping both gold and silver nanoparticles. AgNPs showed inhibition zones of 15.5±0.09mm and 13.3±0.14mm while AuNPs had inhibition zones of 14.510±0.35 and 13.3±0.50mm on E. coli and S. aureus respectively. The findings indicate the potential use of AgNPs and AuNPs in development of drugs in management of pathogenic bacteria.


2020 ◽  
Vol 840 ◽  
pp. 265-269
Author(s):  
Nurjanah Nurjanah ◽  
Endang Saepudin

Curcumin, a diarylheptanoids compound which isolated primary from Curcuma longa, exhibits a variety of exciting biological activities, including as an antibacterial agent. In the present study, a sulfanilamide-contained curcumin compound was synthesized and characterized to investigate the antibacterial activity against gram-positive bacteria S. aureus, B. subtilis and gram-negative bacteria E. coli. The characterization of the synthesized compound was determined by analysing peak absorbance, functional group, and molecular weight using mass spectroscopy, UV/Vis and FTIR spectrophotometry. Curcumin-sulfanilamide compound exhibited the best antibacterial activity against gram-negative bacteria compared to curcumin and the curcumin-derived compound containing isoxazole with inhibitory zone of 11 mm.


2014 ◽  
Vol 14 (6) ◽  
pp. 1087-1094 ◽  
Author(s):  
Luis Sanchez ◽  
Lucas Guz ◽  
Pilar García ◽  
Silvia Ponce ◽  
Silvia Goyanes ◽  
...  

ZnO nanorods (ZnO NRs) were grown on ZnO seeded fluorine doped tin oxide (FTO) substrates at low temperatures (90 °C) from Zn2+ precursors in alkaline aqueous solution. The ZnO seeds were deposited on the FTO substrate heated at 350 °C by spray pyrolysis of a zinc acetate solution in a water ethanol mixture. The structure of seeds was tuned by the ethanol water ratio, Γ, which controls the solvent evaporation rate of drops impinging the substrate. The relationship between the microstructure and optical properties of the ZnO NR films and the photocatalytic antibacterial activity for Escherichia coli abatement, was determined through a detailed characterization of the material. The higher photocatalytic antibacterial activity was performed by ZnO NR films grown on seeds deposited from solutions with Γ in the 0.0–0.03 range. With these films, the population of viable E. coli dropped more than six orders, from 8 × 108 to 4 × 102 CFU. These results show the potential of these materials in water disinfection.


2016 ◽  
Vol 71 (11) ◽  
pp. 1135-1140 ◽  
Author(s):  
Javad Safaei-Ghomi ◽  
Mehrnoosh Asgari-Kheirabadi ◽  
Hossein Shahbazi-Alavi

AbstractIn this work, we report the synthesis and characterization of CeO2 nanoparticles as an efficient catalyst for the preparation of methyl 6-amino-5-cyano-4-aryl-2,4-dihydropyrano[2,3-c]pyrazole-3-carboxylates via one-pot four-component condensation reaction of dimethyl acetylenedicarboxylate, hydrazine hydrate, malononitrile, and aldehydes in aqueous medium. The use of a non-hazardous organic solvent, easy recovery of the catalyst, compatibility with various functional groups, and high yield of the products make the protocol attractive, greener, and economic.


2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
María A. León-Calvijo ◽  
Aura L. Leal-Castro ◽  
Giovanni A. Almanzar-Reina ◽  
Jaiver E. Rosas-Pérez ◽  
Javier E. García-Castañeda ◽  
...  

Peptides derived from human and bovine lactoferricin were designed, synthesized, purified, and characterized using RP-HPLC and MALDI-TOF-MS. Specific changes in the sequences were designed as (i) the incorporation of unnatural amino acids in the sequence, the (ii) reduction or (iii) elongation of the peptide chain length, and (iv) synthesis of molecules with different number of branches containing the same sequence. For each peptide, the antibacterial activity againstEscherichia coliATCC 25922 andEnterococcus faecalisATCC 29212 was evaluated. Our results showed that Peptides I.2 (RWQWRWQWR) and I.4 ((RRWQWR)4K2Ahx2C2) exhibit bigger or similar activity againstE. coli(MIC 4–33 μM) andE. faecalis(MIC 10–33 μM) when they were compared with lactoferricin protein (LF) and some of its derivate peptides as II.1 (FKCRRWQWRMKKLGA) and IV.1 (FKCRRWQWRMKKLGAPSITCVRRAE). It should be pointed out that Peptides I.2 and I.4, containing the RWQWR motif, are short and easy to synthesize; our results demonstrate that it is possible to design and obtain synthetic peptides that exhibit enhanced antibacterial activity using a methodology that is fast and low-cost and that allows obtaining products with a high degree of purity and high yield.


2021 ◽  
Vol 2 (2) ◽  
pp. 16-24
Author(s):  
Sara Hajib ◽  
Mohamed Hssaini ◽  
Anouar Alami ◽  
Hicham Bekkari ◽  
Najoua Benchemsi ◽  
...  

Bacterial resistance to antibiotics and disinfectants has become a real concern. The hospital presents a favorable environment for the colonization and development of bacteria resistant to antibiotics and disinfectants. The search for new antimicrobial compounds is essential to combat this phenomenon. Tetrazole derivatives may represent a solution due to their interesting antibacterial activity. In this work, two tetrazole derivatives; thiophene-2-carbaldehyde (T2C) and 5-(thiophen-2-yl)-1H-tetrazole (5TPh-1HT), were evaluated for their antibacterial activities against a set of reference strains and strains isolated from the hospital environment. The antibacterial effect was studied by the disc diffusion method and by determination of MIC and MBC. The 5-(thiophen-2-yl)-1H-tetrazole (5TPh-1HT) has a broader spectrum of activity than its oxime derivative (T2C). The latter has bactericidal activity only on gram-negative Escherichia coli, Pseudomonas aeruginosa with MICs ranging from 0.62 mg/ml to 2.5 mg/ml, while 5TPh-1HT has a bactericidal effect on all strains with MICs ranging from 0.62 mg/ml to 1.25 mg/ml. Both products have a significant inhibitory activity on the strains tested in particular E. coli H, S. aureus H, P. aeruginosa and Streptococcus spp A. It was found that these activities vary depending on the microbial strain tested and the product applied.


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