scholarly journals SYNTHESIS, CHARACTERIZATION, AND ANTIMICROBIAL EVALUATION OF NEW N-PHENYLCINNAMAMIDE DERIVATIVES LINKED TO ASPIRIN AND IBUPROFEN

Author(s):  
Ameer H Alwash ◽  
Alaa M Mahdi ◽  
Haider J Al-karagully

Objective: The objective of this study was to synthesize phenylcinnamamide (substituted acetanilide chalcone) derivatives linked to aspirin and ibuprofen with potential antibacterial and antifungal activity.Methods: Substituted acetanilide compounds were reacted with different arylaldehydes through Claisen-Schmidt condensation in the presence of KOH. They formed differently substituted acetanilide chalcones (1a-e) which are linked to aspirin and ibuprofen through an ester linkage to form compounds (2a-j) using ethyl chloroformate (ECF) as a catalyst.Results: The synthesized compounds have been characterized by elemental analysis, Fourier transform infrared and1H-nuclear magnetic resonance spectroscopy. An antibacterial evaluation was achieved for Gram-positive bacteria (Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli) and antifungal for Candida albicans.Conclusion: Compounds (2a-j) have shown intermediate antimicrobial activity against different strains of microorganisms.

2014 ◽  
Vol 1 (1) ◽  
pp. 1-3 ◽  
Author(s):  
Deepkumar Joshi ◽  
Rinku Patel ◽  
Nupur Patel ◽  
Devendra Patel ◽  
Chintan Pandya

The leaf and stem of cordia macleodii plant were investigated for evaluating antibacterial and antifungal properties.Different extracts of leaf and stem viz. double distilled water, methanol, ethyl acetate ane n-hexane were collectedand content was optimized for the maximum amount of extraction with varying time of 6 and 12 h. The extracts weretested for their antimicrobial activities against gram-positive bacteria (B. sutilis), gram-negative bacteria (E. coli) andfungi (A. niger). The extracts were found to be more active against bacteria as compared to fungi. It was also observedthat the antibacterial and antifungal potential of the water extracts were found to be excellent as 1A (38 mm) and 1B (22mm) compared to the other extracts. Graphical Abstract:


2020 ◽  
Vol 5 (1) ◽  
pp. 1-5
Author(s):  
K. Kapadiya ◽  
G. Dubal ◽  
Y. Bhola ◽  
P. Dholaria

A new series of 4-((5-(2-chlorophenyl)-1,3,4-oxadiazol-2-yl)methoxy)-N-(benzylidene derivatives)benzenamine (5a-k) have been synthesized and were screened for their in vitro antibacterial activity against Gram-positive bacteria (Pseudomonas aeruginosa, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Staphylococcus aureus) and antifungal activity (Candida albicans, Aspergillus niger, Aspergillus clavatus). Synthesized compounds were characterized by IR, mass (MS), 1H NMR and 13C NMR spectra. The synthesized compounds 5b, 5c, 5g and 5i showed potency in terms of antimicrobial activity against tested microorganisms.


2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Amit Gupta ◽  
Rajendra Singh ◽  
Pankaj K. Sonar ◽  
Shailendra K. Saraf

A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600 µg/mL, respectively. Minimum inhibitory concentrations of all the compounds were also determined and were found to be in the range of 100–400 µg/mL. All the compounds showed moderate-to-good antimicrobial activity. Compounds4a[2-(4-fluoro-phenyl)-3-(4-methyl-5,6,7,8-tetrahydro-quinazolin-2-yl)-thiazolidin-4-one] and4e[3-(4,6-dimethyl-pyrimidin-2-yl)-2-(2-methoxy-phenyl)-thiazolidin-4-one] were the most potent compounds of the series, exhibiting marked antimicrobial activity againstPseudomonas fluorescens,Staphylococcus aureus,and the fungal strains. Thus, on the basis of results obtained, it may be concluded that synthesized compounds exhibit a broad spectrum of antimicrobial activity.


2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Ponnusamy Packialakshmi ◽  
Perumal Gobinath ◽  
Daoud Ali ◽  
Saud Alarifi ◽  
Balasubramani Ravindran ◽  
...  

The goal of this research is to create a novel Schiff base of chitosan polymer derivatives 1a-1j. Nanotechnology is a promising field since it avoids the usage of hazardous chemicals while also saving time. Using the leaf extract of the pharmacologically valuable herb Mentha piperita, we described a green synthesis of ZnO NPs. Zinc oxide ions may be easily reduced into ZnO NPs using a Mentha piperita extract. ZnO NPs were employed as a phytocatalyst in this investigation to make chitosan derivatives. The synthetic procedure is straightforward, with a short reaction time and a high yield. Our newly synthesized compounds have been characterized by FTIR and nuclear magnetic resonance spectroscopy (1H NMR and 13C NMR), and morphology analysis was observed by XRD, SEM, and TEM. In addition, the antibacterial activity was also evaluated against gram-positive bacteria and gram-negative bacteria. Compound 1b is extremely active against gram-negative bacteria (4.0 μg/mL, E. coli), and compound 1h is highly active against gram-positive bacteria (6.0 μg/mL, S. aureus) compared with standard erythromycin and other chitosan derivatives. As a result, compounds 1b and 1h could be a high crucial molecule in the development of antibacterial drugs.


2019 ◽  
Vol 4 (1) ◽  
pp. 32-35
Author(s):  
Priyanka Sharma

8-Substituted-2,5-dihydro-1,5-benzothiazepine derivatives have been synthesized by the reaction of 1-(2-furyl)-3-(3,4-dimethoxyphenyl)-2-propenone with six 5-substiuted-2-minobenzenethiols in dry ethanol saturated with dry HCl gas and also in the presence of aluminium nitrate as catalyst in dry ethanol. All the newly synthesized compounds were characterized by analytical and spectral data comprising IR, 1H NMR, 13C NMR, 19F NMR and mass studies. All these compounds have also been evaluated for their antimicrobial assay against the Gram-positive bacteria, Staphylococcus aureus and the Gram-negative bacteria, Pseudomonas aeruginosa and the fungus, Candida albicans. The antifungal activity was found to be more significant than antibacterial activity.


2021 ◽  
Vol 18 (4) ◽  
pp. 332-338
Author(s):  
Ravindra Sandipan Shinde ◽  
Satish Ashruba Dake ◽  
Rajendra Pundalikrao Pawar

Background: A series of Triazine Chalcone derivatives were synthesized by the condensation of 1-(4-((4,6-dimethoxy-1,3,5-triazin-2-yl)amino)phenyl)ethanone with substituted benzaldehyde in methanol solvent. Methods: All the synthesized derivatives (3a-l) were screened for their anti-bacterial evaluation against Gram negative bacteria Escherichia coli (NCIM 2137) and Pseudomonas aeruginosa (NCIM 2036); Gram positive bacteria Staphylococcus aureus, Bacillus subtilis (NCIM 2250) and four fungal stains. Candida albicans (MTCC 227), Aspergillus niger (NCIM 545), Candida tropicalis (NCIM 3110) and Candida glabrata (NCIM 3236). Results and Conclusion: Several target molecules throughout the series showed good antibacterial and antifungal activity against tested stains.


2019 ◽  
Vol 10 (4) ◽  
pp. 3535-3543
Author(s):  
Mustafa M. AL-Hakiem ◽  
Rita S. Elias ◽  
Munther A. Mohammed-Ali

New series of Schiff base compounds obtained from sulfa drugs have been synthesized by the reaction of sulfonamide compounds (sulfadiazine, sulfapyridine, sulfamethazine, or sulfamerazine) with corresponding aromatic aldehydes (3-pyridinecarboxaldehyde or 4-pyridinecarboxaldehyde). The synthesized compounds were characterized by FT-IR, ESI-Mass, and 1H-NMR spectroscopy to confirm the chemical structures of synthesized compounds. The purity of all synthesized compounds were verified using pre-coated TLC (MERCK) plates using dichloromethane: methanol (9:1) solvent system. The chromatographic plates were viewed under ultraviolet(UV) light at 254 nm The sulfonamide Schiff base compounds were tested for antibacterial evaluation against two pathogenic Gram-positive bacteria (Staphylococcus aureus, Streptococcus spp.) and two pathogenic Gram-negative bacteria (Escherichia coli and Klebsiella pneumonia). The antibacterial activity of synthesized compounds was evaluated by assessing the inhibitory concentration by measuring their inhibition zone versus certain kinds of standard antibiotics with concentrations (500, 750, and 1000) μg /ml. Most synthesized compounds at high concentration were moderately active against all tested bacteria ,compound SH7 showed best antibacterial activity for both (Gram-positive and Gram-negative) bacteria while SH8 compound exhibited moderate antibacterial activity against Gram-positive bacteria and weak activity (<10 mm) against Gram-negative bacteria and all synthesized compounds were less antibacterial activity for all tested bacterial strains than standard drugs.


Author(s):  
Vo Viet Dai Vo

1,5-Disubstituted 1,2,3-triazoles are synthesized viametal-free multi-component reaction from primary amine, ketones and 4-nitrophenyl azide. The structure of three target compounds including:1-(4-methoxybenzyl)-5-(4-methylphenyl)-1H-1,2,3-triazole (1), 1-(4-methoxybenzyl)-5-(4-nitrophenyl)-1H-1,2,3-triazole (2) and 1-(4-methoxybenzyl)-5-phenyl-1H-1,2,3-triazole (3) is elucidated and identified by infrared spectroscopy, nuclear magnetic resonance spectroscopic analysis and high resolution mass spectrum. The formation of heterocyclic aromatic 1,2,3-triazole ring is approved by the appearance of singlet peak at 7.71 ppm in 1H NMR corresponding with triazolyl proton. In addition, antibacterial and antifungal activities of products are also tested with three Gram-positive bacteria (B. subtilis, S. aureus and L. fermentum), three Gram-negative bacteria (P. aeruginosa, E.coli, S. enterica), and Candida albicans fungus.


2011 ◽  
Vol 8 (1) ◽  
pp. 478-483
Author(s):  
Baghdad Science Journal

In this study Oscillatoria limnetica and Chroococus minor were isolated ?purified and identification from water canal around Baghdad University Campus. The water of this canals originally from Tigris River. BG-11 culture media was used for their cultivation in suitable laboratory conditions (25c°, 200µE/m2/sec) for 16:8 hrs. Light: dark. Each culture was harvested at the end of exponential phase .Organic solvents used for extraction were Ethanol? Hexane and Methanol 95% to extract the crude active Intracellular and Extracellular substances, and evaporated down to dryness .Antibacterial and antifungal activity of these different extracts were evaluated against 6 strains of gram positive bacteria and gram negative bacteria in addition to fungi, Agar diffusion method was used in this evaluation. Results showed that the extracellular products which extracted by hexane and the extracellular products which extracted by ethanol from Oscillatoria limnetica were have higher antagonistic activity against bacteria and Fungi comparing with methanol extracts .However higher antibacterial and antifungal were obtained against the studied strains of comparing with methanol and ethanol extracts of the same algae products. The gram positive bacteria studied revealed higher susceptibility to attack by the intracellular and extracellular extracts comparing with the gram negative bacteria. These extracts revealed higher antibacterial activity against Bacillus subtilise and the average of inhibition zone were 26, 22 mm. for intracellular and extracellular products of O.limnetica respectively. However, C. minor intracellular products extract has the antagonistic activity against Staphylococcus aureus with 28 mm inhibition zone


2021 ◽  
Vol 8 (3) ◽  
pp. 94-97
Author(s):  
Maryam Kouhkan ◽  
Fatemeh Ghanbary ◽  
Fatemeh Karimi

Background: Antimicrobial resistance is a major problem in treatment and public health, and it has been increasing over the last few decades. Hence, serious measurements are needed to overcome this challenge. In this study, we evaluated antibacterial and antifungal activity of some nanocomposites including titanium dioxide (5a), polyimide nanocomposites containing cerium oxide (5b), silver-titanium dioxide nanoparticles prepared under desired conditions (5c), polyaniline/wheat husk ash PANI /WHA (5d), Ag-TiO2 prepared by sol–gel route (5e), and cellulose-graphene (5f) against some bacterial and fungal strains, which are the most common agents in many infectious diseases. Methods: The nanoparticles were prepared in desired condition. The agar dilution and well agar diffusion methods were used for determination of inhibition zoon and minimum inhibitory concentration (MIC) during preliminary evaluation of antimicrobial activity against Staphylococcus aureus, Streptococcus pyogenes, Pseudomonas aeruginosa, Escherichia coli and Candida albicans. Results: The results showed that the nanocomposites had good activity against gram-negative bacteria. Conclusions: Our results showed that the inhibitory activity of these nanocomposites on gram-negative bacteria was better than gram-positive bacteria.


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