scholarly journals Synthesis, characterization and antibacterial studies of Schiff bases of acyclovir

2020 ◽  
Vol 11 (1) ◽  
pp. 411-415
Author(s):  
Abood S Huda ◽  
Abdullah S. Asia ◽  
Wrewish S Zainab
Keyword(s):  
Antibacterial Activity ◽  
Schiff Base ◽  
Schiff Bases ◽  
Retardation Factor ◽  
Anticancer Activities ◽  
Spectral Techniques ◽  
Gram Positive Bacteria ◽  
Medical Need ◽  
Wide Range ◽  
Base Moiety

There is a crucial medical need for the progress of new antibacterial agents with new and more efficient mechanisms. Schiff bases are stated to have a wide range of pharmacological activities, including antimicrobial, antibacterial, antifungal, antioxidant, and anticancer activities, which are largely due to the distinguishing C=N group. Furthermore, heterocyclic compounds containing acyclic hydroxylated side chains, for example, acyclovir (ACV), are an essential class of antiviral acyclonucleosides. Therefore, this work was to synthesize and evaluate a new series of acyclovir analogues bearing a Schiff base moiety. Some of Schiff's bases synthesis in an ethanolic solution of drug, aldehydes, and glacial acetic acid as a catalyst followed in the synthesis of substituted acyclovir drug compounds. In this work, two new series of acyclovir analogues bearing a Schiff base moiety were Synthesised, characterized, and confirmed by various spectral techniques like FTIR, CHN, and 1HNMR spectra, in addition to melting point and retardation factor (Rf.). The biological activity of synthesized Schiff base compounds measured against a panel of various bacteria. The results revealed that these compounds showed antibacterial activity against Gram-positive bacteria such as bacillus and Gram-negative bacteria such as proteus, E-coli, pseudomonas, and klebsiella. It concluded that synthesized Schiff base compounds showed higher antibacterial activity than acyclovir that they derived from it.

Green Synthesis of Some Novel Imidazole Schiff base Derivatives Under Microwave Irradiation / Reflux Conditions and Evaluations of the Antibacterial Activity

2020 ◽  
Vol 7 (3) ◽  
pp. 207-215
Author(s):  
Samaneh Eftekhari ◽  
Naser Foroughifar ◽  
Sara Hallajian ◽  
Alireza Khajeh-Amiri
Keyword(s):  
Antibacterial Activity ◽  
Schiff Base ◽  
Microwave Irradiation ◽  
Schiff Bases ◽  
Synthetic Method ◽  
Antibacterial Effects ◽  
Gram Positive ◽  
Imidazole Derivatives ◽  
Schiff Base Derivatives ◽  
Wide Range

Background: Schiff bases are excellent compounds. They were synthesized by condensation of active carbonyl and amines. They were widely used as a substrate in the preparation of industrial compounds as well as pharmaceutical purposes. They exhibit a wide range of biological activities. In this study, based on the importance of Schiff bases, a sustainable synthetic method was developed employing reflux and microwave irradiation. Objective: Develop a new synthetic method for imidazole Schiff base derivatives synthesis employing reflux, microwave irradiation, and ethanol as a green solvent. Methods: Synthesis of imidazole Schiff base derivatives was carried out under reflux and microwave irradiation conditions. Antibacterial activity of imidazole derivatives and standard drugs was examined against two Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and two Gramnegative bacteria (Proteus mirabilis, Escherichia coli). Results: Schiff bases were synthesized in the presence of microwave irradiation and ethanol in high yields 90-98% for 2-4 min. The antibacterial effects of Schiff bases were evaluated against both strains of Gram-positive and Gram-negative. Conclusion: In this paper, a novel series of imidazole Schiff base derivatives were synthesized using reflux, microwave irradiation, and ethanol. Antibacterial effects were investigated. The excellent advantages of microwave irradiation in the synthesis of imidazole derivatives include reduction of reaction time from an hour to a minute, high product yield. In this study, the measurement of antibacterial activity was also important. Imidazole derivatives with Cl, OH, and CH3 groups showed antibacterial effects.

scholarly journals Synthesis and Evaluation of Schiff Bases of 4-Amino-5-(chlorine substituted phenyl)-4H-1,2,4-triazole-3-thione as Antimicrobial Agents

2020 ◽  
Vol 41 (1) ◽  
pp. 26-35
Author(s):  
Kishor Devkota ◽  
Govinda Pathak ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Triazole Ring ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Spectral Techniques ◽  
Schiff Base Derivatives ◽  
Bacteria And Fungi ◽  
Different Strains

Triazole ring system has attracted a continuously growing interest of synthetic organic chemists and those dealing with the medicinal compounds due to its versatile potential to interact with biological systems. Schiff bases are also considered as one of the most biologically active compounds.  The aim of the present study was to synthesize new Schiff bases bearing triazole nucleus and to assess their antimicrobial activities. Four new Schiff base derivatives of 1,2,4-triazole-3-thione were synthesized by combining two different pharmacophores viz. triazole nucleus and Schiff base moiety and were characterized by spectral techniques (UV, FT-IR, and NMR). The Schiff bases were evaluated for antibacterial (Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae) and antifungal (Candida albicans) activities. The synthesized compounds exhibited good to moderate activities against different strains of bacteria and fungi tested.

scholarly journals SYNTHESIS, CHARACTERIZATION, QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP, DOCKING, ANTIBACTERIAL ACTIVITY, AND BRINE SHRIMP LETHAL STUDIES ON L-PHENYLALANINE SCHIFF BASES

2016 ◽  
Vol 9 (9) ◽  
pp. 203
Author(s):  
Easwaramoorthi Deivanayagam ◽  
Jayaprakash R ◽  
Aroj Kumar Sha ◽  
Hemalatha S
Keyword(s):  
Antibacterial Activity ◽  
Schiff Base ◽  
Schiff Bases ◽  
Brine Shrimp ◽  
Quantitative Structure Activity Relationship ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Group ◽  
Quantitative Structure ◽  
Structure Activity

ABSTRACTObjective: Aim of this work is to synthesize and characterization of the hydroxyl group the hydroxyl group substituted L-phenylalanine Schiff basesto compare their predicted quantitative structure-activity relationship (QSAR) and molecular docking against Escherichia coli protein ZipA (1s1j)outcomes with the antibacterial activity and brine shrimp lethal assay (BSLA) results.Methods: The Schiff bases of L-Phenylalanine were synthesized by the simple condensation reaction using methanol, water in 2:1 ratio at reflux andwere characterized by spectral techniques. QSAR parameters of the Schiff bases were predicted using java-based online and offline tools. Moleculardocking carried through online mcule server and CLC Drug Discovery Workbench 3. Antibacterial activity and toxicity studies were conducted usingbroth dilution and brine shrimp lethal assay methods, respectively.Results: The Schiff bases fulfilled the QSAR drug-likeness parameters and showed the docking score between −6.8 and −6.0 Kcal/mol which arehigher than amoxilicillin and gentamicin like standard drugs. They also possess good inhibition for urinary tract infection causing E. coli bacteria,and minimum inhibitory concentrations (MIC) exists between 3.25 and 5.25 μg/ml. The brine shrimp lethal concentration for 50% mortality [LC50])between 58.73 and 135.6 μg/ml.Conclusion: Para, meta and 2,4 hydroxyl substituted Schiff bases exhibited good inhibition against Gram-negative E. coli bacteria at low concentrationand the MIC exists below the LC50 value. The Schiff base showed high drug score, high docking score, and low toxicity than other Schiff base. Dockingscore, high inhibition, low clogP, low MICKeywords: L-phenylalanine, Schiff base, Quantitative structure-activity relationship, Docking, Antibacterial, Lethal concentration for 50% mortality.

scholarly journals Synthesis of Phthalyl Substituted Imidazolones and Schiff Bases as Antimicrobial Agents

2011 ◽  
Vol 8 (1) ◽  
pp. 427-434
Author(s):  
Pramilla Sah ◽  
Neha Saraswat ◽  
Manu Manu
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Schiff Bases ◽  
Phthalic Anhydride ◽  
Thionyl Chloride ◽  
Antimicrobial Agents ◽  
Spectral Techniques ◽  
E Coli ◽  
H Nmr ◽  
Ethanoic Acid

A new series of phthalyl substituted imidazolones (4a–g) and Schiff bases (5a–d) were synthesized from 2-methyl-(m-nitro-1,3-dioxo-1,3-dihydro-(2H)-isoindole-2-yl)-5-amino-1,3,4-thiadiazole (3a–b). Compounds (3a–b) were prepared by cyclisation of 2-(m-nitro-1,3-dioxo-1,3-dihydro-(2H)-isoindole-2-yl)methyl ethanoate (2) with thiosemicarbazide. 2-(m-nitro-1,3-dioxo-1,3-dihydro-(2H)-isoindole-2-yl)ethanoic acid (1) in presence of thionyl chloride and methanol gave the ester (2) while compound (1) was synthesized by aminolysis of phthalic anhydride with glycine. The compounds were characterized by spectral techniques of IR,1H NMR, Mass and elemental analysis. All the synthesized compounds (4a–g) and (5a–d) were screened for their antibacterial activity against the pathogenic strainsE. coli, P. aureus, C. freundiiwhile antifungal activity was evaluated againstA. niger, A. flavus, Penicillium sp. and C. albicans.

scholarly journals Synthesis and antibacterial activity of some Schiff base complexes

2006 ◽  
Vol 71 (7) ◽  
pp. 733-744 ◽  
Author(s):  
R. Nair ◽  
A. Shah ◽  
S. Baluja ◽  
S. Chanda
Keyword(s):  
Antibacterial Activity ◽  
Schiff Base ◽  
Metal Complexes ◽  
Schiff Bases ◽  
Schiff Base Complexes ◽  
Ethyl Benzene ◽  
Resistant Bacteria ◽  
Bacterial Strains ◽  
Iron And Zinc

Two Schiff bases were synthesized from raceacetophenone: 1) ADS1 4-ethyl-6-{(E)-1-[(3-nitrophenyl)imino]ethyl}benzene-1,3-diol and 2) ADS3 4-ethyl-6-[(E)-1-{(2-nitrophenyl)imino]ethyl}benzene-1,3-diol. Then their metal complexes were formed. The metals selected for the preparation of complexes were copper, nickel, iron and zinc. Hence, in total 8 metal complexes were synthesized and screened for antibacterial activity against some clinically important bacteria, such as Pseudomonas aeruginosa, Proteus vulgaris, Proteus mirabilis, Klebsiella pneumoniae and Staphylococcus aureus. The in vitro antibacterial activity was determined by the Agar Ditch technique using DMF (polar) and 1,4-dioxane (non polar) as solvents. The Schiff bases showed greater activity than theirmetal complexes; themetal complexes showed differential effects on the bacterial strains investigated and the solvent used, suggesting that the antibacterial activity is dependent on the molecular structure of the compound, the solvent used and the bacterial strain under consideration. The Schiff base ADS3 in the polar solvent DMF showed better antibacterial activity towards the investigated bacterial strains. Amongst the four metals, Zn showed the best antibacterial activity followed by Fe in 1,4-dioxane while Ni followed by Zn and Fe showed the best antibacterial activity in DMF. P. vulgaris was the most resistant bacteria.

scholarly journals A review on biological activities of Schiff base ligand and their metal complexes

2020 ◽  
Vol 13 (1) ◽  
pp. 217-221
Author(s):  
P.M. Jadhav
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Schiff Bases ◽  
Carbonyl Compounds ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Cytotoxic Activities ◽  
Wide Range ◽  
Enzymatic Agents ◽  
Dye Industry

Schiff bases and their metal complexes are wide range of biological applications and are synthesized from the condensation reaction of amino compounds with carbonyl compounds. Schiff base and their metal complexes have a wide variety of applications in food and dye industry, agrochemical, polymer, catalysis, analytical chemistry, antifertility, antiinflammatory activity, antiradical activity, and biological system as enzymatic agents. Several have reviewed them of their antimicrobial, antibacterial, antifungal, antitumor, and cytotoxic activities. This review summarized the most promising biological activities of Schiff bases and their metal complexes

scholarly journals Characterization, Molecular Docking, Antimicrobial and Anticancer Studies on 5-Bromo salicylaldehyde-furan-2-yl-methanamine Condensed Schiff Base Rare Earth Metal Complexes

2021 ◽  
Vol 33 (9) ◽  
pp. 2127-2134
Author(s):  
B. Preethi ◽  
R. Jayaprakash ◽  
S. Kutti Rani ◽  
N. Vijayakumar
Keyword(s):  
Schiff Base ◽  
Rare Earth ◽  
Metal Complexes ◽  
Rare Earth Metal ◽  
Earth Metal ◽  
Anticancer Activities ◽  
Spectral Techniques ◽  
Biological Efficacy ◽  
Rare Earth Metal Complexes

This work described the synthesis and characterization of 1-(furan-2-yl) methanamine condensed with 5-bromo-2-hydroxybenzaldehyde Schiff base rare earth metal (Ln3+, Pr3+, Nd3+, Sm3+ and Eu3+) complexes.. They were characterized using relevant spectral techniques and docked against microbial target proteins (1H9Z, 3ZBO) theoretically. The experimental antibacterial and anticancer activities (HeLa, MCF7) of these metal complexes were investigated for biological efficacy. Out of five metal complexes, Pr3+ complex exposed good biological efficacy result in both assays.

scholarly journals Synthesis and Pharmacological Evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

2020 ◽  
Vol 10 (5) ◽  
pp. 274-292
Author(s):  
Rohit Kumar ◽  
Sushil Kumar ◽  
Mohammad Asif Khan
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Biological Activities ◽  
Diffusion Method ◽  
Gram Positive ◽  
Standard Drug ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Pharmacological Evaluation

Recently a series of Schiff bases of diphenylamine derivatives have been synthesized and evaluated in vitro for their antibacterial activity against pathogenic both Gram-positive bacteria B. subtitles and Gram-negative bacteria E. coli using ciprofloxacin as standard drug at conc. of 50 μg/ml and 100 μg/ml. Literature review revels that chalcones possesses various biological activities like antimicrobial, antiviral, anti-inflammatory, anticancer and sedative etc. Therefore the present study was designed on synthesis and pharmacological evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides. Target compound was synthesized by reaction of chloroacetylchloride with diphenylamine to afford 2-chloro-N, N-diphenylacetamide which further by reaction with substituted Chalcones and characterized following recrystallization and evaluated for anti-microbial potential through cup-diffusion method. In results, the target compounds were tested for activity against B. Subtilis, E.Coli and C. albicans. The chalcones having the lipophilic 4-chloro group (RKCT2) showed the greatest antimicrobial activity (zone of inhibition 20 & 22 mm against. B. subtilis, E. Coli, C. Albicans respectively. It suggests further researchers to go through anti-microbial evaluations against a more varieties of bacteria and fungi. Keywords: Schiff bases of diphenylamine derivatives, antibacterial activity, Gram-positive bacteria, 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

scholarly journals Design and Development of Complexation of Ce+3 Metal Ions with Synthesized INZ Incorporated Bio-active Schiff Bases

2021 ◽  
Vol 11 (4) ◽  
pp. 3989-4006
Keyword(s):  
Schiff Base ◽  
Metal Ions ◽  
Schiff Bases ◽  
Elemental Analysis ◽  
Metal Ion ◽  
Organic Ligands ◽  
Schiff Base Complexes ◽  
Spectral Techniques ◽  
The Stability ◽  
Antibacterial And Antifungal

In the present research, a series of Ce+3 metal ions complexation with INZ incorporating Schiff bases have been reported. INZ incorporated Schiff Bases (3a-e) were developed by condensing INZ with substituted aromatic aldehyde and confirmed with various spectral Techniques such as Elemental analysis, UV, IR, 1H-NMR, 13H NMR. All the synthesized organic ligands were evaluated against antibacterial and antifungal stains and found moderate to significant results. The Ce+3 metal ion solution mixed with newly prepared bio-active INZ Schiff bases (3a-e) to afford the [Ce-INZ Schiff Base] complexes (4a-e). The stability constants of prepared complexes were evaluated and found in order as a (3e) > (3d) > (3a) > (3b) > (3c).

scholarly journals Cytogenotoxic effects of two potential anticancer Ruthenium(III) Schiff Bases complexes

2016 ◽  
Vol 6 (2) ◽  
pp. 112-120 ◽  
Author(s):  
Izet Eminovic ◽  
Emira Kahrovic ◽  
Aner Mesic ◽  
Emir Turkusic ◽  
Dzenana Kargic ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Chromosome Segregation ◽  
Toxic Effects ◽  
Control Group ◽  
Anticancer Activities ◽  
Antiproliferative Effects ◽  
Clinical Level ◽  
Ruthenium Compounds ◽  
Wide Range ◽  
Chromosome Bridges

Introduction: Treatment of cancer has been subject of great interest. Researchers are continuously searching for new medicines. In this sense, ruthenium complexes have big potential. Some evidences suggest that ruthenium compounds possess anticancer activities. We synthesized two recently published ruthenium(III) complexes with bidentate O,N and tridentate O,O,N Schiff bases derived from 5-substituted salicylaldehyde and aminophenol or anilineare. These compounds showed affinity for binding to the DNA molecule, however, insufficient data are available regarding their possible toxic effects on biological systems.Methods: In the present study we evaluated genotoxic, cytotoxic, and cytostatic effects of Na[RuCl2(L1)2] and Na[Ru(L2)2], using the Allium cepa assay.Results: Different toxic effects were observed depending on the substance, tested concentration, and endpoint measured. In general, the tested compounds significantly lowered the root growth and mitotic index values as compared to the control group. Additionally, a wide range of abnormal mitotic stages, both clastogenic and non-clastogenic were observed in the treated cells. Na[RuCl2(L1)2] significantly increased the frequency of sticky metaphases, chromosome bridges, micronuclei, impaired chromosome segregation, as well as number of apoptotic and necrotic cells over the controls. In contrast, Na[Ru(L2)2] did not show significant evidence of genotoxicity with regard to chromosome aberrations and micronuclei, however, significant differences were detected in the number of apoptotic and necrotic cells when the highest concentration was applied.Conclusions: In this study we demonstrated antiproliferative effects of Na[RuCl2(L1)2] and Na[Ru(L2)2]. At clinical level, these results could be interesting for further studies on anticancer potential of the ruthenium(III) complexes using animal models.

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