scholarly journals The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

2021 ◽  
Vol 90 (1) ◽  
pp. 2
Author(s):  
Halyna Hryhoriv ◽  
Illia Mariutsa ◽  
Sergiy M. Kovalenko ◽  
Victoriya Georgiyants ◽  
Lina Perekhoda ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Antibacterial Agents ◽  
Docking Studies ◽  
Synthetic Method ◽  
Bacillus Subtilis Atcc ◽  
Resistant Strains ◽  
Derivatives Of

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.

scholarly journals Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1339 ◽  
Author(s):  
Islam H. El Azab ◽  
Nadia A.A. Elkanzi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Positive Control ◽  
Design Synthesis ◽  
Aspergillus Brasiliensis ◽  
In Vitro Investigation ◽  
Bacillus Subtilis Atcc ◽  
Antimicrobial Evaluation

A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

scholarly journals Antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata

2020 ◽  
Vol 4 (1) ◽  
pp. 49
Author(s):  
Gracielle Oliveira Sabbag Cunha ◽  
Ana Paula Terezan ◽  
Andreia Pereira Matos ◽  
Marcela Carmen De Melo Burger ◽  
Paulo Cezar Vieira ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Methyl Esters ◽  
Carboxyl Group ◽  
Isomeric Mixture ◽  
E Coli ◽  
Bacillus Subtilis Atcc ◽  
Derivatives Of

This study evaluated the antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata (Melastomataceae) against five microorganisms: Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6623), Pseudomonas aeruginosa (ATCC 15442), and Candida albicans (ATCC 10231). The isomeric mixture of ursolic and oleanolic acids was active against S. aureus (MIC = 250 μg mL-1) and against E. coli, B. subtilis, and P. aeruginosa (MIC = 500 μg mL-1). The flavone 5,6,7-trihydroxy-4’-methoxyflavone and the methyl esters, semisynthetic derivatives of a mixture of ursolic and oleanolic acids, showed no activity against the tested microorganisms. These results suggest that the carboxyl group present in the triterpenes may contribute to antimicrobial activity.

scholarly journals Suzuki Reaction for the Synthesis of New Derivatives of 4-Chloro-3,5-Dimethyl Phenol and their in vitro Antibacterial Screening

2019 ◽  
Vol 31 (12) ◽  
pp. 2955-2958
Author(s):  
R.H. Zaooli ◽  
F.A. Hussein ◽  
N.N.A. Jafar ◽  
S.N.K. Al-Thamir
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Elemental Analysis ◽  
Proteus Mirabilis ◽  
Suzuki Reaction ◽  
Antibacterial Properties ◽  
Antibacterial Screening ◽  
Derivatives Of ◽  
Dimethyl Phenol

Many derivatives of 4-chloro-3,5-dimethylphenol have been synthesized using Suzuki reaction and characterized by IR, 1H NMR and micro elemental analysis. These compounds also tested in terms of their antibacterial properties against Staphylococcus aureus, Escherichia coli and Proteus mirabilis.

scholarly journals Actividad antibacteriana de extractos hexánico y etanólico de macroalgas marinas de la Bahía de Ancón, Lima – Perú

2020 ◽  
Vol 31 (2) ◽  
pp. e17829
Author(s):  
Ramón Muñoz A. ◽  
Selma Santome ◽  
Jorge León Q.
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Bacillus Subtilis ◽  
Salmonella Typhimurium ◽  
San Francisco ◽  
Subtilis Atcc ◽  
Bacillus Subtilis Atcc ◽  
Para Determinar

En el presente trabajo se evaluaron las actividades antimicrobianas de extractos etanólicos y hexánicos de nueve especies de macroalgas marinas recolectadas en la zona intermareal de la playa San Francisco, Ancón, de Lima, Perú. La evaluación se realizó in vitro frente a un panel de bacterias estándar Gram positivas (Staphylococcus aureus ATCC 6538, Bacillus subtilis ATCC 6633 y Enterococcus faecalis ATCC 51922) y Gram negativas (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 9027 y Salmonella Typhimurium ATCC 14028). Los extractos etanólicos fueron de mayor rendimiento (67%) en comparación a los hexánicos (33%), en especial frente a los Gram positivos, siendo el extracto obtenido de Ulva enteromorpha var. intestinalis y U. nematoidea los más activos frente a S. aureus ATCC 6538 (74.1 y 78.2 % de inhibición, respectivamente). Los extractos etanólicos de Cladophora sp y U. nematoidea frente a B. subtilis ATCC 6633 presentaron inhibiciones entre moderada y baja (52.5 y 33%, respectivamente). Los extractos etanólicos de U. enteromorpha y Cladophora sp frente a S. Typhimurium presentaron solo 40% de inhibición. El extracto etanólico de Cladophora sp fue el único que presentó actividad antimicrobiana frente a las cinco cepas bacterianas y fue elegida para determinar la Concentración Mínima Inhibitoria (CMI), que resultó en 12.5 y 25 mg/ml frente a B. subtilis ATCC 6633 y S. aureus ATCC 6538, respectivamente. Se concluye que, la mayoría de las macroalgas estudiadas contienen compuestos inhibitorios, cuyos extractos etanólico y hexánico son capaces de inhibir el crecimiento de bacterias patógenas.

scholarly journals Synthesis and Antibacterial Activities of Coumarins with an Acyl Amino Side Chain

2021 ◽  
Vol 68 (1) ◽  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Antibacterial Activities ◽  
Ring Structure ◽  
Coumarin Derivatives ◽  
Anti Cancer ◽  
Synthetic Reactions ◽  
Derivatives Of

Coumarin is a heterocyclic moiety containing benzo pyran ring structure. It is widely distributed in the plant kingdom as a glycoside. Many compounds of medicinal and pharmaceutical importance possess coumarin ring structure. Drugs with coumarin structure can be synthesized by many well-known synthetic reactions. Coumarin derivatives were found to be antibacterial, anticoagulant, antiinflammatory, anti-HIV, anti-cancer and antioxidant. As part of the search for new and effective antibacterial agents, eight novel derivatives of coumarins were synthesized by Mannich reaction. All the compounds were evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli using ciprofloxacin as standard and DMSO as solvent. Three of the synthesized derivatives exhibited good antibacterial activity against Staphylococcus aureus and Escherichia coli. The work must be extended so as to develop coumarin derivatives into highly effective antibacterial agents.

scholarly journals Synthesis of new derivatives of hydrazinecarbothioamides and 1,2,4-triazoles and evaluation of their antimicrobial activities

2015 ◽  
Vol 80 (12) ◽  
pp. 1461-1470 ◽  
Author(s):  
Laura Socea ◽  
Gabriel Saramet ◽  
Constantin Draghici ◽  
Bogdan Socea ◽  
Vlad Constantin ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Shigella Flexneri ◽  
13C Nmr Spectroscopy ◽  
Antimicrobial Activities ◽  
Bacillus Subtilis Atcc ◽  
Naoh Solution ◽  
New Compounds ◽  
Derivatives Of

A new series of hydrazinecarbothioamides 6-9 bearing 5H-dibenzo[a,d][7]annulene moiety were synthesized. Cyclization of 6-9 in NaOH solution produced the corresponding 1,2,4-triazoles-3(4H)-thiol 10-13, which proved to be axial isomers. The thioethers 14-17 were prepared by alkylation of 10-13 with methyl iodide. All new compounds were characterized by elemental analysis, IR-, UV-, 1H-NMR and 13C-NMR spectroscopy. The evaluation for antimicrobial activity against Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6663, Salmonella tiphimurium ATCC 14028, Shigella flexneri ATCC 12022, Candida albicans ATCC 90028 was performed.

Synthesis of New Piperazine Substituted Chalcone Sulphonamides as Antibacterial Agents

2020 ◽  
Vol 17 (2) ◽  
pp. 136-143
Author(s):  
Yan-Ling Tang ◽  
Yong-Kun Li ◽  
Min-Xin Li ◽  
Hui Gao ◽  
Xiao-Bi Yang ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Good Antibacterial Activity ◽  
In Vitro Antibacterial Activity ◽  
Global Threat

Background: Infection is a global threat to human health, and there is an urgent need to develop new effective antibacterial drugs to treat bacterial infections. Objective: To study the antibacterial activity of piperazine substituted chalcone sulphonamides. Materials and Methods: A series of novel piperazine substituted chalcone sulphonamides have been prepared, and in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli strains were evaluated. Results: The results showed that derivatives 6a, 6c and 6h displayed good antibacterial activity against Bacillus subtilis with MIC values of 4.0-8.0 mg/mL. Conclusion: Piperazine substituted chalcone sulphonamides may be used as potential antibacterial agents.

In vitro and in vivo Activity of Coumermycin and Other Antibacterial Agents against Methicillin-Resistant Strains of Staphylococcus aureus

Chemotherapy ◽  
1986 ◽  
Vol 32 (6) ◽  
pp. 499-505 ◽  
Author(s):  
Joel Unowsky ◽  
Pranatharth H. Chandrasekar ◽  
William DeLorenzo ◽  
Donald P. Levine
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Agents ◽  
Methicillin Resistant ◽  
Resistant Strains

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.

scholarly journals Synthesis of New Heterocyclic Compounds Derived from Anthrone and Evaluation of Their Biological Activity

2008 ◽  
Vol 5 (4) ◽  
pp. 627-637
Author(s):  
Baghdad Science Journal
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Heterocyclic Amines ◽  
Pathogenic Microorganism ◽  
Standard Strain ◽  
Chemical Structures ◽  
Heterocyclic Derivatives

In this research, Schiff bases derived from the reaction of anthrone with different heterocyclic amines have been described. The resulted Schiff base compounds were reacted with various nucleophiles in order to obtain new heterocyclic derivatives. Chemical structures of all products were confirmed by IR, 1H-, 13C-NMR spectral data and elemental analysis. All synthesized compounds were in vitro tested against a standard strain of pathogenic microorganism including Gram +ve bacteria (Staphylococcus aureus), Gram –ve bacteria (Escherichia coli), and fungi (Candida albicans).

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