scholarly journals Synthesis and Biologically Important of 2-Mercaptobenthiazole (MBT)-Clubbed Chalcone Derivatives

Author(s):  
Falguni Bhabhor ◽  
K. Satish ◽  
Hiren Variya ◽  
Vikram Panchal

In this present work base catalyzed method used for formation of Chalcone of (E)-4-(3-(4-hydroxyphenyl) acryloyl)-5-methyl-2(p-tolyl)-1H-pyrazol-3(2H)-one (II) reacted with derivatives of S-benzo [d] thiol-2yl-2-chloroethanethioate (Ia-f) resulted in formation of corresponding derivatives of (E)-S-benzo [d] thiazol-2-yl 2-(4-(3-(5-methyl-3oxo-2(p-tolyl)-2,3-dihydro-1H-pyrazol-4-yl)-3-oxoprop-1-en-1-yl) phenoxy) etanethioate (IIIa-f) was confirmed by spectral characterization such as IR,1H NMR, LC-MS and elemental analysis. The compounds were screened for their antimicrobial properties against a broad panel Gram-positive and Gram-negative bacteria as well as fungi.

2015 ◽  
Vol 70 (1-2) ◽  
pp. 45-50
Author(s):  
Asu Usta ◽  
Hacer Taşkıran

Abstract N-alkyl substituted 2′,3″-thiazachalcones {3-[(1E)-3-(4-methylthiophene-2-yl)-3-oxoprop-1-en-1-yl]-1-alkyl (C5–12,14) pyridinium bromides} were synthesized by a two-step reaction. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, elemental analysis and mass spectral studies. The synthesized compounds were tested for antibacterial activities and found to be more active against Gram-positive as compared to Gram-negative bacteria.


2005 ◽  
Vol 2 (2) ◽  
pp. 109-112
Author(s):  
A. K. Parekh ◽  
K. K. Desai

Some new chalcones have been prepared by Claisen-schmidt condensation of ketone and different aromatic aldehydes. These chalcones on condensation with urea in presence of acid gave Pyrimidine-2-ones. The synthesized compounds have been characterized by elemental analysis, IR and1H NMR spectral data. They have been screened for their antibacterial activity against Gram positive bacteria B. subtillis & S. aureus and Gram negative bacteria E. coli & S. typhi.


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.


1999 ◽  
Vol 43 (5) ◽  
pp. 1274-1276 ◽  
Author(s):  
Manhong Wu ◽  
Robert E. W. Hancock

ABSTRACT Both linear and cyclic derivatives of the cyclic 12-amino-acid antimicrobial peptide bactenecin were designed based on optimization of amphipathicity and charge location. In general, increasing the number of positive charges at the N and C termini and adding an extra tryptophan residue in the loop not only increased the activities against both gram-positive and gram-negative bacteria but also broadened the antimicrobial spectrum.


Chemistry ◽  
2021 ◽  
Vol 3 (4) ◽  
pp. 1271-1285
Author(s):  
Patricia Zimet ◽  
Ruby Valadez ◽  
Sofía Raffaelli ◽  
María Belén Estevez ◽  
Helena Pardo ◽  
...  

Microbial technology offers a green alternative for the synthesis of value-added nanomaterials. In particular, fungal compounds can improve silver nanoparticle production, stabilizing colloidal nanoparticles. Based on a previous study by our group, silver nanoparticles obtained using the extracellular cell-free extracts of Phanerochaete chrysosporium (PchNPs) have shown antimicrobial and antibiofilm activity against Gram-negative bacteria. Moreover, nisin—a bacteriocin widely used as a natural food preservative—has recently gained much attention due its antimicrobial action against Gram-positive bacteria in biomedical applications. Therefore, the aim of this work was to conjugate biogenic silver nanoparticles (PchNPs) with nisin to obtain nanoconjugates (PchNPs@nis) with enhanced antimicrobial properties. Characterization assays were conducted to determine physicochemical properties of PchNPs@nis, and also their antibacterial and antibiofilm activities were studied. The formation of PchNPs@nis was confirmed by UV-Vis, TEM, and Raman spectroscopy analysis. Different PchNPs@nis nanobioconjugates showed diameter values in the range of 60–130 nm by DLS and surface charge values between −20 and −13 mV. Nisin showed an excellent affinity to PchNPs, with binding efficiencies higher than 75%. Stable synthesized PchNPs@nis nanobioconjugates were not only able to inhibit biofilm formation by S. aureus, but also showed inhibition of the planktonic cell growth of Staphyloccocus aureus and Escherichia coli, broadening the spectrum of action of the unconjugated antimicrobials against Gram-positive and Gram-negative bacteria. In conclusion, these results show the promising application of PchNPs@nis, prepared via green technology, as potential antimicrobial nanomaterials.


2012 ◽  
Vol 9 (1) ◽  
pp. 481-486
Author(s):  
K. Anuradha ◽  
R. Rajavel

Novel Cu(II),Ni(II) and VO(II) complexes are synthesized with N1,N4-bis(2-aminobenzylidene)benzene-1,4-diamine (L). Complexes were characterized by elemental analysis, molar conductance, IR, UV and EPR. Spectral studies reveals a square planner geomentry for Cu(II), Ni(II) complexes and square pyramidal for VO(II) complex. The ligand and its complexes were also evaluated against the growth of gram positive bacteria and gram negative bacteria.


2014 ◽  
Vol 31 ◽  
pp. S66-S67 ◽  
Author(s):  
Mayri Alejandra Diaz De Rienzo ◽  
Ben Dolman ◽  
Fernando Guzman ◽  
Candice Kaisermann ◽  
James Winterburn ◽  
...  

2021 ◽  
Vol 4 (4) ◽  
pp. 348-354
Author(s):  
Aliyu Shehu ◽  
Ahmed Salisu ◽  
Nura S. Gwaram

In this study, the antimicrobial and physicochemical properties of translucent antimicrobial soap prepared using two medicinal plants, Aloe vera gel and Ziziphus jujube leaf extract   was evaluated. The results of the physicochemical analysis showed the pH (7.52±0.02), hardness(1.3 cm±0.02), solubility (0.82 g±0.02) and foamability (6.80 cm±0.03) of the prepared soap and these values were within the acceptable limit  set by WHO/SON which make the prepared soap skin-friendly. Similarly, the antimicrobial screening was carried out on selected Gram-positive and gram-negative bacteria as well as on fungi species using disc diffusion methods and the results showed varying antimicrobial activity at different concentrations ranging from 62.5-500 mg/ml. However, the susceptibility of test bacteria in terms of the zone of inhibition at 500mg/ml of the soap was observed on Staphylococcus lentus (22 mm), Staphylococcus aureus (20mm), Escherichia coli (15 mm), Raoltella ornithinolytica (12mm). The result of antifungal properties was as follows,  Candida albicans (12 mm), Trichophyton rubrum (12 mm), and Aspergillus nigar (10 mm)  at 500 mg/ml concentration. The results when compared to other antimicrobial soap in the market indicate good quality by inhibiting the growth of both Gram-positive, gram-negative bacteria and fungi. The antimicrobial activities exhibited by the soap in this study could be attributed to the presence of phytochemical constituents in the plant extracts, which signify the potential of the soap as an antimicrobial agent. Therefore, these findings confirmed the efficacy of Aloe vera gel and Zizipus jujube extract in traditional medicine.


Author(s):  
Shipra Baluja ◽  
Nilesh Godvani ◽  
Sumitra Chanda

In this work, some novel derivatives of Cyanopyridines and Isoxazoles were synthesized using Vilsmeier-Haack reagent and their structures were confirmed by FTIR, 1H NMR and mass spectroscopic methods. The antibacterial activities of these synthesized compounds were studied in DMSO and DMF by agar well diffusion method against some Gram positive and Gram negative bacteria. It is observed that activity depends upon three S: solvent, strain and structure.


Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1389 ◽  
Author(s):  
Søren Wedel Svenningsen ◽  
Rikki Franklin Frederiksen ◽  
Claire Counil ◽  
Mario Ficker ◽  
Jørgen J. Leisner ◽  
...  

Infections caused by bacteria resistant to antibiotics are an increasing problem. Multivalent antibiotics could be a solution. In the present study, a covalent conjugate between Ciprofloxacin and a G0-PAMAM dendrimer has been synthesized and tested against clinically relevant Gram-positive and Gram-negative bacteria. The conjugate has antimicrobial activity and there is a positive dendritic effect compared to Ciprofloxacin itself.


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