scholarly journals Synthesis, isomerisation and biological properties of mononuclear ruthenium complexes containing the bis[4(4′-methyl-2,2′-bipyridyl)]-1,7-heptane ligand

2018 ◽  
Vol 47 (7) ◽  
pp. 2422-2434 ◽  
Author(s):  
Biyun Sun ◽  
Hannah M. Southam ◽  
Jonathan A. Butler ◽  
Robert K. Poole ◽  
Alexandre Burgun ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Ruthenium Complexes ◽  
Biological Properties ◽  
Good Antibacterial Activity

The strained complexes cis-β-[Ru(phen′)(bb7)]2+ isomerise to the corresponding cis-α isomers, with cis-α-[Ru(Me4phen)(bb7)]2+ showing good antibacterial activity.

Synthesis and Biological Properties of New Piperidine Substituted Benzothiazole Derivatives

2021 ◽  
Vol 6 (3) ◽  
pp. 181-185
Author(s):  
S. Syed Shafi ◽  
R. Rajesh ◽  
S. Senthilkumar
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Carboxylic Acid ◽  
Biological Properties ◽  
The Novel ◽  
Photoluminescence Spectra ◽  
Benzothiazole Derivatives ◽  
Chemical Structures ◽  
Good Antibacterial Activity ◽  
Biological Studies

In present work, ethyl 2-aminobenzo[d]thiazole-6-carboxylate was reacted to piperidine using copper(II) bromide to get ethyl 2-(piperidin-1-yl)benzo[d]thiazole-6-carboxylate. The reaction of ethyl 2-(piperidin- 1-yl)benzo[d]thiazole-6-carboxylate with NaOH produces 2-(piperidin-1-yl)benzo[d]thiazole-6- carboxylic acid. The inter-mediate 2-(piperidin-1-yl)benzo[d]thiazole-6-carboxylic acid have been isolated as stable compounds. The chemical structures of synthesized compounds were established based on the 1H & 13C NMR and IR spectral data. The mass of the novel compounds was established with the help of the LC-MS technique. The photoluminescence spectra explain the optical property of the compound. The biological studies of synthesized compounds show that the compound 5e possesses good antibacterial activity and compound 5d has good antifungal activity.

Synthesis and SAR Evaluation of Mercapto Triazolobenzothiazole

2021 ◽  
Vol 18 (4) ◽  
pp. 362-374
Author(s):  
Mamatha S.V ◽  
S.L. Belagali ◽  
Mahesh Bhat
Keyword(s):  
Antibacterial Activity ◽  
Biological Activities ◽  
Antibacterial Activities ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Step Method ◽  
Good Antibacterial Activity ◽  
Anti Inflammatory ◽  
Mic Value

Background: Benzothiazoles possess a vast sphere of biological activities including anti- inflammatory, antibacterial activities whereas triazoles display various pharmacological properties including antimicrobial and antitubercular activities. Hence, triazole conjugated benzothiazole side-chain anticipating their interesting biological properties has been focused upon. Objective: The objective of the current work is synthesis and biological evaluation of a new series of benzothiazole appended triazole derivatives. Methods: The target compounds were prepared via a multi-step method involving the treatment of 2-amino benzothiazole with hydrazine followed by cyclization with carbon disulfide to give the corresponding triazol-2-thiol derivatives and then alkylation of these derivatives. All the synthesized compounds were characterized by FT-IR, Mass, 1H and 13C NMR spectra and were screened for their antibacterial, antioxidant, anti-inflammatory and anti-tubercular (anti-TB) activities in vitro. These molecules were also docked into the enoyl acyl carrier reductase (Inha, PDB ID-1ZID) in silico. Results: While all the synthesized compounds were active against M. tuberculosis at 50 μg/ml, the pyrrolidine and piperidine appended benzothiazolyltriazoles showed the superior activity (MIC values 12.5 to 1.6 μg/ml). Compound 5a (5-CH3 with piperidine), 5b (7-CH3 with piperidine) and 7b (7-CH3 with pyrrolidine) showed good antibacterial activity against Staphylococcus aureus with MIC value 31.25μg/ml, while compounds 7a (5-CH3 with pyrrolidine), 6b (7-CH3 with morpholine) and 8c (7-Br with pyridine) exhibited good antibacterial activity against E-coli with MIC value 62.5μg/ml. Compounds 7b (7-CH3 with pyrrolidine) and 5c (7-Br with piperidine) showed good anti-oxidant activities with IC50 values 93.25 and 82.25, respectively. Notably, these compounds were non-toxic to the normal cells even at high concentrations with IC50 value 238μg/ml. Conclusion: The compound 7b, a benzothiazolyltriazole having a pyrrolidine group (five membered ring) attached to two CH2 groups and methyl substituent at 7th position of the benzothiazole ring emerged as a novel and promising hit molecule that showed anti-TB, antimicrobial and antiinflammatory activities in vitro.

Recent Advances in 1,3,5-Triazine Derivatives as Antibacterial Agents

2020 ◽  
Vol 17 (8) ◽  
pp. 991-1041
Author(s):  
Divya Utreja ◽  
Jagdish Kaur ◽  
Komalpreet Kaur ◽  
Palak Jain
Keyword(s):  
Antibacterial Activity ◽  
Heterocyclic Compounds ◽  
Antibacterial Agents ◽  
Rapid Development ◽  
Pharmacological Action ◽  
Biological Properties ◽  
Vast Array ◽  
Bacterial Diseases ◽  
New Class ◽  
Triazine Derivatives

Triazine, one of the nitrogen containing heterocyclic compounds has attracted the considerable interest of researchers due to the vast array of biological properties such as anti-viral, antitumor, anti-convulsant, analgesic, antioxidant, anti-depressant, herbicidal, insecticidal, fungicidal, antibacterial and anti-inflammatory activities offered by it. Various antibacterial agents have been synthesized by researchers to curb bacterial diseases but due to rapid development in drug resistance, tolerance and side effects, there had always been a need for the synthesis of a new class of antibacterial agents that would exhibit improved pharmacological action. Therefore, this review mainly focuses on the various methods for the synthesis of triazine derivatives and their antibacterial activity.

Synthesis of Chalcones and Nucleosides Incorporating [1, 3, 4]Oxadiazolenone Core and Evaluation of their Antifungal and Antibacterial Activities

2020 ◽  
Vol 15 (6) ◽  
pp. 665-679
Author(s):  
Alok K. Srivastava ◽  
Lokesh K. Pandey
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Good Antibacterial Activity

Background: [1, 3, 4]oxadiazolenone core containing chalcones and nucleosides were synthesized by Claisen-Schmidt condensation of a variety of benzaldehyde derivatives, obtained from oxidation of substituted 5-(3/6 substituted-4-Methylphenyl)-1, 3, 4-oxadiazole-2(3H)-one and various substituted acetophenone. The resultant chalcones were coupled with penta-O-acetylglucopyranose followed by deacetylation to get [1, 3, 4] oxadiazolenone core containing chalcones and nucleosides. Various analytical techniques viz IR, NMR, LC-MS and elemental analysis were used to confirm the structure of the synthesised compounds.The compounds were targeted against Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and Aspergillus flavus, Aspergillus niger and Fusarium oxysporum for antifungal activity. Methods: A mixture of Acid hydrazides (3.0 mmol) and N, Nʹ- carbonyl diimidazole (3.3 mmol) in 15 mL of dioxane was refluxed to afford substituted [1, 3, 4]-oxadiazole-2(3H)-one. The resulted [1, 3, 4]- oxadiazole-2(3H)-one (1.42 mmol) was oxidized with Chromyl chloride (1.5 mL) in 20 mL of carbon tetra chloride and condensed with acetophenones (1.42 mmol) to get chalcones 4. The equimolar ratio of obtained chalcones 4 and β -D-1,2,3,4,6- penta-O-acetylglucopyranose in presence of iodine was refluxed to get nucleosides 5. The [1, 3, 4] oxadiazolenone core containing chalcones 4 and nucleosides 5 were tested to determined minimum inhibitory concentration (MIC) value with the experimental procedure of Benson using disc-diffusion method. All compounds were tested at concentration of 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, 0.62 mg/mL, 0.31 mg/mL and 0.15 mg/mL for antifungal activity against three strains of pathogenic fungi Aspergillus flavus (A. flavus), Aspergillus niger (A. niger) and Fusarium oxysporum (F. oxysporum) and for antibacterial activity against Gram-negative bacterium: Escherichia coli (E. coli), and two Gram-positive bacteria: Staphylococcus aureus (S. aureus) and Bacillus subtilis(B. subtilis). Result: The chalcones 4 and nucleosides 5 were screened for antibacterial activity against E. coli, S. aureus and B. subtilis whereas antifungal activity against A. flavus, A. niger and F. oxysporum. Compounds 4a-t showed good antibacterial activity whereas compounds 5a-t containing glucose moiety showed better activity against fungi. The glucose moiety of compounds 5 helps to enter into the cell wall of fungi and control the cell growth. Conclusion: Chalcones 4 and nucleosides 5 incorporating [1, 3, 4] oxadiazolenone core were synthesized and characterized by various spectral techniques and elemental analysis. These compounds were evaluated for their antifungal activity against three fungi; viz. A. flavus, A. niger and F. oxysporum. In addition to this, synthesized compounds were evaluated for their antibacterial activity against gram negative bacteria E. Coli and gram positive bacteria S. aureus, B. subtilis. Compounds 4a-t showed good antibacterial activity whereas 5a-t showed better activity against fungi.

scholarly journals Curcumin-loaded polyvinyl butyral film with antibacterial activity

e-Polymers ◽  
2020 ◽  
Vol 20 (1) ◽  
pp. 673-681
Author(s):  
Yanchao Qiao ◽  
Lijie Duan
Keyword(s):  
Mechanical Property ◽  
Thermal Stability ◽  
Antibacterial Activity ◽  
Polyvinyl Butyral ◽  
Counting Method ◽  
E Coli ◽  
Antibacterial Materials ◽  
Good Antibacterial Activity ◽  
Colony Counting ◽  
Widespread Interest

AbstractAntibacterial materials have found widespread interest in different fields nowadays. In this study, curcumin (Cur) was incorporated into the polyvinyl butyral (PVB) matrix by dissolving in ethanol for improving the functional properties of a pure PVB film. We found that Cur was uniformly dispersed in the PVB matrix, which showed good compatibility. Moreover, the incorporation of Cur could also improve thermal stability, hydrophilicity, and mechanical property. The UV-vis spectra of the PVB–Cur film demonstrated that the film could block ultraviolet radiation. Subsequently, the antibacterial activity of the PVB–Cur film was measured by the colony-counting method against S. aureus and E. coli. The results showed that the PVB–Cur film exhibited good antibacterial activity. Therefore, the PVB–Cur film was considered as a promising material for food and medical packaging applications.

scholarly journals Multidisciplinary Studies of Folk Medicine “Five Thieves’ Oil” (Olejek Pięciu Złodziei) Components

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2931
Author(s):  
Przemysław Siejak ◽  
Wojciech Smułek ◽  
Farahnaz Fathordobady ◽  
Anna Grygier ◽  
Hanna Maria Baranowska ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Membrane Permeability ◽  
Significant Contribution ◽  
Spectroscopic Analysis ◽  
Folk Medicine ◽  
Cell Activity ◽  
Biological Properties ◽  
Cell Membrane Permeability ◽  
Comparable Activity ◽  
Terpene Derivatives

To meet the growing interest in natural antibacterial agents, we evaluated the physicochemical and biological properties of the folk medicine known as “five thieves’ oil” (Polish name: olejek pięciu złodziei). Five thieves’ oil consists of a mixture of five oils: rosemary, lemon, clove, eucalyptus, and cinnamon. In this study, we performed gas chromatography, FTIR, and UV–vis spectroscopic analysis, as well as L-a-b color tests, contact angle determination, and surface tension determination. To verify its antibacterial activity, the metabolic activity and changes in cell membrane permeability of bacteria of the genus Pseudomonas were studied. As a result, it was found that among the constituent oils, the oils of clove and cinnamon were the least volatile and, at the same time, had the strongest antibacterial activity. However, a mix of all the oils also showed comparable activity, which was even more pronounced for the oils after 4 weeks of aging. This effect can be linked to the high content of terpene derivatives such as eugenol and cinnamaldehyde, which can cause changes in bacterial membrane permeability, affecting cell activity and survival. This study is the first to characterize the constituents of the popular folk medicine five thieves’ oil, confirming and explaining its strong antibacterial activity, thus constituting a significant contribution to contemporary health education.

The Preparation of Carbon Microspheres Loading Silver Antimicrobial Agent and the Study of its Properties

2012 ◽  
Vol 550-553 ◽  
pp. 1026-1029
Author(s):  
Jian Xi Ren ◽  
Jing Ya Li ◽  
Zhi Feng Cai ◽  
Jin Ming Dai ◽  
Mei Niu ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Electron Microscope ◽  
Antibacterial Agent ◽  
Chemical Adsorption ◽  
Carbon Microspheres ◽  
Bacterial Inhibition ◽  
Good Antibacterial Activity ◽  
Scanning Electron

Carbon microspheres (CMSs) were used as the carrier to prepare the Ag-loading CMSs (Ag/CMSs) antibacterial agent through the method of chemical adsorption. The morphologies and structures of modified CMSs were characterized by using the field emission Scanning Electron Microscope (SEM). The results showed that silver was absorbed on the surface of CMSs. The bacterial inhibition ring experiment showed that Ag/CMSs had good antibacterial activity against Staphylococcus aureus and Escherichia coli, meanwhile the diameters of the bacterial inhibition rings were 19 mm against Staphylococcus aureus and 21 mm against Escherichia coli, respectively.

Preparation, Characterisation, Crystal Structure and Antibacterial Activity of two Bis-Schiff Bases Containing a Piperazine Ring

2018 ◽  
Vol 42 (10) ◽  
pp. 512-514
Author(s):  
Rui-bo Xu ◽  
Xiao-tian Yang ◽  
Hai-nan Li ◽  
Peng-cheng Zhao ◽  
Jiao-jiao Li ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Schiff Bases ◽  
Piperazine Ring ◽  
X Ray ◽  
X Ray Crystallography ◽  
Good Antibacterial Activity

Two new bis-Schiff bases containing a piperazine ring, N,N‘-bis(4-chlorobenzylidene)- and N,N‘-bis(4-cyanobenzylidene)-1,4-bis(3-aminopropyl)piperazine, were prepared by the reaction of N,N‘-bis(3-aminopropyl)piperazine with 4-chloro- and 4-cyanobenzaldehyde, respectively. The dichloro compound was fully identified by X-ray crystallography and it exhibited good antibacterial activity against Escherichia coli, Staphylococcus aureus and Bacillus subtilis.

scholarly journals GC-MS Analysis and Antibacterial Activity of different Solvent Extracts of Shuteria involucrata

2018 ◽  
Vol 7 (2) ◽  
pp. 116-120
Author(s):  
Senthamizh Selvan N ◽  
◽  
Isaiah S ◽  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Ethanolic Extract ◽  
Disc Diffusion ◽  
Plant Materials ◽  
Gram Negative ◽  
Good Antibacterial Activity ◽  
Ms Analysis ◽  
Diffusion Technique

The present study was focused to examine the presence of phytoconstituents in the ethanolic extract of Shuteria involucrata plant using GC-MS analysis and Antibacterial activity. The GC-MS analysis of S. involucrata leaf was performed using Agilent 6890-JEOL GC-Mate-II Mass Spectrometer. The result of the study showed the presence of six bioactive compounds in the ethanolic extract. The antimicrobial activity was carried out by disc diffusion technique against the four selected pathogens. Among the four, tested for Antibacterial Activity Staphylococcus aureus, and Pseudomonas aeruginosa and were more susceptible to the extract, whereas the others are less susceptible. Ethanol and methanol extracts of plant materials exhibited good antibacterial activity against gram positive, gram negative bacterias

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