Synthesis, Characterization and Biological Evaluation of Some 2-[1-(1,3-Diphenyl-1HPyrazol-4-yl)-meth-(E)-ylidene]indan-1-one Derivatives as Antibacterial Agents

2020 ◽  
Vol 5 (2) ◽  
pp. 127-132
Author(s):  
Uttam B. Chougule ◽  
Hemant V. Chavan ◽  
Savita R. Dhongade
Keyword(s):  
Reaction Time ◽  
Antibacterial Agents ◽  
Spectroscopic Analysis ◽  
Knoevenagel Condensation ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Short Reaction Time ◽  
E Coli ◽  
Time Structures ◽  
Substituted 1

A new series of 2-[1-(1,3-diphenyl-1H-pyrazol-4-yl)-meth-(E)-ylidene]-indan-1-one derivatives (5a-l) have been synthesized through through the Knoevenagel condensation of pyrazole carbaldehydes with differently substituted 1-indanone derivatives in the presence of base. A high yielding and solvent-free method was developed for the synthesis of hydrazones from acetophenones under microwave irradiation in a very short reaction time. Structures of the newly synthesized compounds were affirmed by IR, 1H & 13C NMR and mass spectroscopic analysis. The confirmed structures were screened for their antibacterial potency against S. aureus and E. coli bacterial strains. Among the series, compounds 5b, 5c and 5f were evoked as potent antibacterial agents

scholarly journals Spectroscopic and Biophysical Studies on Chalcones and Schiff Bases Derived from Chromen-2-one and Quinoline-2(1H)-one Derivatives as Antibacterial Agents

2020 ◽  
Vol 32 (7) ◽  
pp. 1719-1727
Author(s):  
Saad H. Alotaibi
Keyword(s):  
13C Nmr ◽  
Dna Cleavage ◽  
Antibacterial Agents ◽  
Spectroscopic Analysis ◽  
Docking Studies ◽  
The Other ◽  
Moderate Activity ◽  
Bacterial Strains ◽  
E Coli ◽  
Biophysical Studies

A series of chalcone derivatives and arylidene analogues derived from 3-acetyl coumarin were synthesized. The synthesized compounds were elucidated by spectroscopic analysis such as elemental analysis, infrared, 1H & 13C NMR and mass spectroscopies, and then the synthesized compounds were purified and tested against three bacterial strains. Compound 9c showed high activity against E. coli and P. aeruginosa. Compounds 4 and 6a showed moderate activity against E. coli while compounds 6a, 6b and 9c showed moderate activity against S. aureus. The reference antibiotics were tested against the same bacteria strains in the same conditions and showed that ciprofloxacin have positive activity against P. aeruginosa and S. aureus but it shows negative activity against E. coli while amoxicillin have positive activity against S. aureus and negative activity against E. coli and P. aeruginosa. On the other hand, vancomycin has positive activity against P. aeruginosa but not tested against E. coli and S. aureus. Staph strains were treated with compounds 4 and 7 on DNA fragmentation and DNA cleavage. Docking studies of synthesized compound 9c was determined and the results were compared with ampicillin. Finally, UV and fluorescence analyses of the synthesized compounds (3, 4, 6b, 6c, 6e, 7, 9c and 9e) were also conducted.

scholarly journals Synthesis, Antibacterial, and Antioxidant Evaluation of Novel Series of Condensed Thiazoloquinazoline with Pyrido, Pyrano, and Benzol Moieties as Five- and Six-Membered Heterocycle Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 357
Author(s):  
Ebraheem Abdu Musad Saleh ◽  
Abdullah Mohammed AL Dawsari ◽  
Kakul Husain ◽  
Ismail Hassan Kutty ◽  
K.M.Lokanatha Rai
Keyword(s):  
Antibacterial Activity ◽  
Heterocyclic Compounds ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
E Coli ◽  
Antioxidant Evaluation ◽  
Synthetic Approaches ◽  
Membered Heterocycle ◽  
Molecular Framework

A novel synthesis of thiazolo[2,3-b]quinazolines 4(a–e), pyrido[2′,3′:4,5]thiazolo[2,3-b]quinazolines {5(a–e), 6(a–e), and 7(a–e)}, pyrano[2′,3′:4,5]thiazolo[2,3-b]quinazolines 8(a–e), and benzo[4,5]thiazolo[2,3-b]quinazoloine9(a–e) derivatives starting from 2-(Bis-methylsulfanyl-methylene)-5,5-dimethyl-cyclohexane-1,3-dione 2 as efficient α,α dioxoketen dithioacetal is reported and the synthetic approaches of these types of compounds will provide an innovative molecular framework to the designing of new active heterocyclic compounds. In our study, we also present optimization of the synthetic method along with a biological evaluation of these newly synthesized compounds as antioxidants and antibacterial agents against the bacterial strains, like S. aureus, E. coli, and P. aeruginosa. Among all the evaluated compounds, it was found that some showed significant antioxidant activity at 10 μg/mL while the others exhibited better antibacterial activity at 100 μg/mL. The results of this study showed that compound 6(c) possessed remarkable antibacterial activity, whereas compound 9(c) exhibited the highest efficacy as an antioxidant. The structures of the new synthetic compounds were elucidated by elemental analysis, IR, 1H-NMR, and 13C-NMR.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

scholarly journals Syntheses and biological evaluation of 2-amino-3-acyl-tetrahydrobenzothiophene derivatives; antibacterial agents with antivirulence activity

2014 ◽  
Vol 12 (12) ◽  
pp. 1942-1956 ◽  
Author(s):  
Hung The Dang ◽  
Erik Chorell ◽  
Hanna Uvell ◽  
Jerome S. Pinkner ◽  
Scott J. Hultgren ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Biological Evaluation ◽  
E Coli ◽  
Pilus Assembly

The synthesis, SAR and effects of 2-amino-3-acyl-tetrahydrobenzothiophene derivatives on pilus assembly inE. colihave been described.

scholarly journals 1,4-Naphthoquinone Analogues: Potent Antibacterial Agents and Mode of Action Evaluation

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1437 ◽  
Author(s):  
Palanisamy Ravichandiran ◽  
Sunirmal Sheet ◽  
Dhanraj Premnath ◽  
Ae Rhan Kim ◽  
Dong Jin Yoo
Keyword(s):  
Antibacterial Activity ◽  
Mode Of Action ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Annexin V ◽  
Ros Generation ◽  
Redox Potentials ◽  
Bacterial Strains ◽  
E Coli ◽  
New Class

1,4-Naphthoquinones have antibacterial activity and are a promising new class of compound that can be used to treat bacterial infections. The goal was to improve effective antibacterial agents; therefore, we synthesized a new class of naphthoquinone hybrids, which contain phenylamino-phenylthio moieties as significant counterparts. Compound 4 was modified as a substituted aryl amide moiety, which enhanced the antibacterial activity of earlier compounds 3 and 4. In this study, five bacterial strains Staphylococcus aureus (S. aureus), Listeria monocytogenes (L. monocytogenes), Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa) and Klebsiella pneumoniae (K. pneumoniae) were used to evaluate the antibacterial potency of synthesized naphthoquinones using the minimal inhibitory concentration (MIC) method. Most of the studied naphthoquinones demonstrated major antibacterial activity with a MIC of 15.6 µg/mL–500 µg/mL. Selected compounds (5a, 5f and 5x) were studied for the mode of action, using intracellular ROS generation, determination of apoptosis by the Annexin V-FITC/PI assay, a bactericidal kinetic study and in silico molecular modelling. Additionally, the redox potentials of the specified compounds were confirmed by cyclic voltammetry (CV).

scholarly journals Synthesis, reactions and biological evaluation of some novel thienothiophene derivatives

2019 ◽  
Vol 10 (3) ◽  
pp. 209-217
Author(s):  
Mounir Abbas Ali Mohamed ◽  
Hanan Salah ◽  
Ahmed Mohamed Mohamed El-Saghier
Keyword(s):  
Antibacterial Agents ◽  
Building Blocks ◽  
Biological Evaluation ◽  
E Coli ◽  
Synthesis Reactions

Synthesis of some new bis(chalcones)-based thienothiophene derivatives and study of their synthetic utilities as building blocks for new bis(thiazole), bis(dihydropyran), bis(dihydro pyridine), bis(isoxazoles), bis(pyrazoles), bis(hydropyrimidinethiones), bis(tetrahydro diazepines, oxazepines) and bis(dihydrobenzodiazepnies, benzoxazepines) each linked to a thienothiophene core, is reported. Biological evaluation of the obtained compounds as antibacterial agents was achieved. Compounds 4b, 4c, 7a, 6a, 9a and 11b were found to be very potent against P. aeruginosa, E. coli and K. pneumonia.

Design, Molecular Docking, Synthesis and Biological Evaluation of 4, 5-Substituted 1, 2, 3-Triazoles as Anti-bacterial Agents

2021 ◽  
Vol 14 (2) ◽  
pp. 5372-5383
Author(s):  
Vijayabhargavi M ◽  
Kusuma M. P. ◽  
Akhila Sai ◽  
Sumakanth M ◽  
Zaber Unnisa
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Infections ◽  
Thiophene Ring ◽  
Docking Studies ◽  
Biological Evaluation ◽  
In Silico Docking ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Therapeutic Activities ◽  
Substituted 1

Newer antibacterial agents are needed to combat the growing bacterial infections. Triazoles are one of the leading and most sought out nucleus amongst the heterocyclic rings in the drug world. 1, 2, 3-Triazoles are synthesized by Click Chemistry of alkynes with azides. A synergistic effect is observed when the triazoles are combined with other heterocycles. They also exhibit diversified therapeutic activities like anti-viral, anti-bacterial, anti-diabetic, anti-tubercular, anti-inflam-matory, antihypertensive etc which makes Triazoles an interesting molecule for the researchers to work on. In the current study, we combined 1,2, 3-triazoles with thiophene ring system to get synergistic antibacterial activity. Here, 12 derivatives of 4, 5-substituted-1, 2, 3-Triazoles were subjected to in silico docking studies on Biotin ligase protein (PDB ID: 3V7R). The compounds that showed the best results were synthesized. The newly synthesized derivatives were characterized by using IR, H1 NMR and Mass spectrum. All the synthesized derivatives were evaluated for antibacterial activity against Gram-negative bacteria (E. coli and P. aerugenosa) and gram-positive bacteria (B. subtilis and S. aureus). The compounds showed moderate to good activity, which was comparable to that of the standard Streptomycin drug.

scholarly journals Synthesis and biological evaluation of new hydrazide-Schiff bases

2015 ◽  
Vol 10 (3) ◽  
pp. 555 ◽  
Author(s):  
Asif Husain ◽  
Munendra M. Varshney ◽  
Versha Parcha ◽  
Aftab Ahmad ◽  
Shah Alam Khan
Keyword(s):  
Schiff Bases ◽  
Anthelmintic Activity ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
E Coli ◽  
New Class ◽  
Antibacterial Screening ◽  
Synthesis And Biological Evaluation

<div><p>A new series of N-({5-(substituted aryl)-furan-2-yl}-methylidene)-hydrazides were synthesized with a new class of Schiff bases derived from the reaction of substituted phenyl-1-ketohydrazide <strong>2</strong> or 2-(4-chloro-3-methylaryloxy) acetohydrazide <strong>3</strong> with different 5-(substituted aryl)-2-furfuraldehyde (<strong>1a-k</strong>) to yield substituted N-({5-(substituted aryl)-furan-2-yl}-methylidene)-hydrazides-Schiff bases <strong>(4a-f, 4g-k)</strong>. The title compounds were subjected to <em>in vitro</em> antibacterial screening against Gram positive bacterial strains-<em> S. aureus</em>, <em>B. cereus</em>, <em>E. faecalis</em> and <em>S. epidermidis</em>, and Gram negative bacteria strains- <em>E. coli</em>, <em>S. typhi</em>, <em>S. dysenteriae</em>  and <em>K. pneumoniae</em>. The synthesized Schiff bases were also evaluated for their anthelmintic activity against two species of earthworms (<em>Pheritima posthuma</em> and <em>Perionyx excavates</em>). Some compounds have shown promising antibacterial and anthelmintic activities.</p></div>

Ferrocene-Based Antibacterial Agents: Synthesis, Characterization, and Biological Evaluation of Metal (II) Complexes with Glycine-Derived Compounds

2011 ◽  
Vol 339 ◽  
pp. 317-320 ◽  
Author(s):  
Yu Ting Liu ◽  
Xiao Ming Sun ◽  
Da Wei Yin
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Salmonella Typhi ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Gram Negative ◽  
And Staphylococcus Aureus

A series of Ferrocene Schiff bases derived from glycine and their cobalt (II), copper (II), nickel (II), and zinc (II) metal complexes have been synthesized and characterized by IR, 1H NMR, MS and elemental analysis, the results conformed well with expected structures. The synthesized ligands, along with their metal (II) complexes, were screened in vitro for their antibacterial activity against three Gram-negative (Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains. The results showed that the metal (II) complexes are more potent in antibacterial activity against one or more species in comparison with those of uncomplexed ligands.

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