Synthesis and Biological Activity Evaluation of Novel 5-Methyl-7-phenyl-3H-thiazolo[4,5-b]pyridin-2-ones

A series of 5-methyl-7-phenyl-3H-thiazolo[4,5-b]pyridin-2-ones has been designed, synthesized, and characterized by spectral data. Target compounds were screened for their antimicrobial activity against some pathogenic bacteria and fungi, and most of them showed moderate activity, especially compound 3g, which displayed the potent inhibitory effect against Pseudomonas aeruginosa and Escherichia coli with MIC value of 0.21 μM. The active thiazolopyridine derivatives 3c, 3f, and 3g were screened for their cytotoxicity effects on HaCat, Balb/c 3T3 cells using MTT assay, which revealed promising results. In silico assessment for compounds 3c, 3f, and 3g also revealed suitable drug-like parameters and ADME properties. The binding interactions of the most active compound 3g were performed through molecular docking against MurD and DNA gyrase, with binding energies and an inhibitory constant compared to the reference drug ciprofloxacin. The tested thiazolo[4,5-b]pyridines constitute an exciting background for the further development of new synthetic antimicrobial agents.

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Preliminary in Vitro Investigations on The Inhibitory Activity of The Original Dietary Supplement Oxidal® on Pathogenic Bacterial Strains

JOURNAL OF ADVANCES IN AGRICULTURE ◽

10.24297/jaa.v11i.8693 ◽

2020 ◽

Vol 11 ◽

pp. 37-43

Author(s):

Prof. Teodora P. Popova ◽

Toshka Petrova ◽

Ignat Ignatov ◽

Stoil Karadzhov

Keyword(s):

Dietary Supplement ◽

Broad Spectrum ◽

Pathogenic Bacteria ◽

Antimicrobial Agents ◽

Clinical Effectiveness ◽

Inhibitory Effect ◽

Diffusion Method ◽

Bacterial Strains ◽

Microbial Strains

The antimicrobial action of the dietary supplement Oxidal® was tested using the classic Bauer and Kirby agar-gel diffusion method. Clinical and reference strains of Staphylococcus aureus and Escherichia coli were used in the studies. The tested dietary supplement showed a well-pronounced inhibitory effect against the microbial strains commensurable with that of the broad-spectrum chemotherapeutic agent Enrofloxacin and showed even higher activity than the broad spectrum antibiotic Thiamphenicol. The proven inhibitory effect of the tested dietary supplement against the examined pathogenic bacteria is in accordance with the established clinical effectiveness standards for antimicrobial agents.

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Evaluation of antibacterial, teratogenicity and antibiofilm effect of sulfated chitosans extracted from marine waste against microorganism

Journal of Bioactive and Compatible Polymers ◽

10.1177/08839115211014225 ◽

2021 ◽

pp. 088391152110142

Author(s):

Velu Gomathy ◽

Venkatesan Manigandan ◽

Narasimman Vignesh ◽

Aavula Thabitha ◽

Ramachandran Saravanan

Keyword(s):

Biofilm Formation ◽

Pathogenic Bacteria ◽

Antimicrobial Agents ◽

Inhibitory Effect ◽

Diffusion Method ◽

Marine Litter ◽

Ionization Time ◽

Gram Positive Bacteria ◽

Mineral Components ◽

Ft Ir

Biofilms play a key role in infectious diseases, as they may form on the surface and persist after treatment with various antimicrobial agents. The Staphylococcus aureus, Klebsiella pneumoniae, S. typhimurium, P. aeruginosa, and Escherichia coli most frequently associated with medical devices. Chitosan sulphate from marine litter (SCH-MW) was extracted and the mineral components were determined using atomic absorption spectroscopy (AAS). The degree of deacetylation (DA) of SCH was predicted 50% and 33.3% in crab and shrimp waste respectively. The elucidation of the structure of the SCH-MW was portrayed using FT-IR and 1H-NMR spectroscopy. The molecular mass of SCH-MW was determined with Matrix-Assisted Laser Desorption/Ionization-Time of Flight (MALDI-TOF). The teratogenicity of SCH-MW was characterized by the zebrafish embryo (ZFE) model. Antimicrobial activity of SCH-MW was tested with the agar well diffusion method; the inhibitory effect of SCH-MW on biofilm formation was assessed in 96 flat well polystyrene plates. The result revealed that a low concentration of crab-sulfated chitosan inhibited bacterial growth and significantly reduced the anti-biofilm activity of gram-negative and gram-positive bacteria relatively to shrimp. It is potentially against the biofilm formation of pathogenic bacteria.

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N-(Hydroxyalkyl) Derivatives of tris(1H-indol-3-yl)methylium Salts as Promising Antibacterial Agents: Synthesis and Biological Evaluation

Pharmaceuticals ◽

10.3390/ph13120469 ◽

2020 ◽

Vol 13 (12) ◽

pp. 469

Author(s):

Sergey N. Lavrenov ◽

Elena B. Isakova ◽

Alexey A. Panov ◽

Alexander Y. Simonov ◽

Viktor V. Tatarskiy ◽

...

Keyword(s):

Antibacterial Activity ◽

Antimicrobial Agents ◽

Carbon Chain ◽

Biological Evaluation ◽

Carbon Chain Length ◽

Klebsiella Pneumonia ◽

Moderate Activity ◽

Bacterial Strains ◽

Reference Drug

The wide spread of pathogens resistance requires the development of new antimicrobial agents capable of overcoming drug resistance. The main objective of the study is to elucidate the effect of substitutions in tris(1H-indol-3-yl)methylium derivatives on their antibacterial activity and toxicity to human cells. A series of new compounds were synthesized and tested. Their antibacterial activity in vitro was performed on 12 bacterial strains, including drug resistant strains, that were clinical isolates or collection strains. The cytotoxic effect of the compounds was determined using an test with HPF-hTERT (human postnatal fibroblasts, immortalized with hTERT) cells. The activity of the obtained compounds depended on the carbon chain length. Derivatives with C5–C6 chains were more active. The minimum inhibitory concentration (MIC) of the most active compound on Gram-positive bacteria, including MRSA, was 0.5 μg/mL. Compounds with C5–C6 chains also revealed high activity against Staphylococcus epidermidis (1.0 and 0.5 μg/mL, respectively) and moderate activity against Gram-negative bacteria Escherichia coli (8 μg/mL) and Klebsiella pneumonia (2 and 8 μg/mL, respectively). However, they have no activity against Salmonella cholerasuis and Pseudomonas aeruginosa. The most active compounds revealed higher antibacterial activity on MRSA than the reference drug levofloxacin, and their ratio between antibacterial and cytotoxic activity exceeded 10 times. The data obtained provide a basis for further study of this promising group of substances.

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DETERMINATION OF ANTIMICROBIALACTIVITY USING METHANOLIC EXTRACT OF PITHECELLOBIUM DULCE PLANT LEAVES.

10.36106/ijar/3204353 ◽

2020 ◽

pp. 1-3

Author(s):

Mithaiwala Idris A. ◽

Suthar Hetal S. ◽

Hetvi Soni ◽

Ojha Sunil ◽

Agrawal Amit

Keyword(s):

Pathogenic Bacteria ◽

Inhibitory Effect ◽

Plant Leaves ◽

Bacterial Diseases ◽

Gram Positive Bacteria ◽

Soxhlet Method ◽

Bacteria And Fungi ◽

Antibacterial And Antifungal ◽

Constitutional Analysis

Present days due to the pathogenic bacteria and fungi, the human mortality rate has increased in number. The synthetic antimicrobial and antifungal are used in the treatment of various fungal and bacterial diseases, but have various side effects which limit's their use. Traditionally Pithecellobium dulce plant has been used for treatment of antifungal and antimicrobial infection. In this article we are comparing the activity of antimicrobial and antifungal properties of Pithecellobium dulce plant using leaves extract on gram negative bacteria,gram positive bacteria and fungi.Methanolic extraction of Pithecellobium dulce leaves was carried out using Soxhlet method and the phyto constitutional analysis was carried out for presenceof alkaloids, avonoids, glycosides, saponins, phytosterols, and triterpenoids.The inhibitory effect was determined by Cup plate method, by the measurement of zone of inhibition.The outcome was the leaves extract consisted of active phytoconstituents which were phenols, glycoside, sugar and avanoid due to which the extract showed signicant zone of inhibition,by which property of antibacterial and antifungal was listed. It can be concluded that the leaves of Pithecellobium dulce consist of active phytoconstituents which can be used as potent antimicrobials

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Antibacterial and antifungal activities of essential oils from medicinal plants found in the South Pacific

The South Pacific Journal of Natural and Applied Sciences ◽

10.1071/sp17002 ◽

2017 ◽

Vol 35 (1) ◽

pp. 10 ◽

Cited By ~ 1

Author(s):

R. R. Chand ◽

A. D. Jokhan ◽

R. D. Gopalan ◽

T. Osborne

Keyword(s):

Medicinal Plants ◽

Essential Oils ◽

Pathogenic Bacteria ◽

South Pacific ◽

Inhibitory Effect ◽

Diffusion Method ◽

The South ◽

Inhibition Zones ◽

Bacteria And Fungi ◽

Antibacterial And Antifungal

Natural products such as essential oils have been studied since ancient times to understand their biological properties. Essential oils are noted for their antimicrobial activity. Thus, the focus of this study was to evaluate the antimicrobial effect of five essential oils (EOs) from selected medicinal plants found in the South Pacific, on selected human pathogenic bacteria and fungi affecting agricultural industries. The disc diffusion method was carried out and the diameter of inhibition zones (mm) (DZI) using 0.25, 0.5, 5, 25, 50 and 100% (v/v) of essential oil concentrations were reported. The activity of Cananga odorata essential oils against Thermus thermophiles and Pseudomonas aeruginosa were among the selected bacteria that only showed the susceptibility at the lowest concentration (0.25% v/v). The diameter inhibition zones were 1.60 mm and 4.20 mm, respectively. The inhibitory effect of Ocimum tenuiflorum L essential oils at the highest concentration (100%) showed DZI ranging above 14 mm for all the selected bacteria and above 25 mm for the all selected fungi. The inhibitory effect of selected bacteria and fungi increased with stronger concentrations of essential oils. Hence, the essential oils from medicinal plants found in the South Pacific hold great potential for the antibacterial and antifungal properties.

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Investigating the Inhibitory Effect of Silver Nanoparticles against Some Species of Candida and Pathogenic Bacteria

Cihan University-Erbil Scientific Journal ◽

10.24086/cuesj.v4n1y2020.pp32-36 ◽

2020 ◽

Vol 4 (1) ◽

pp. 32-36

Author(s):

Alaa M. Hasan ◽

Sura M. Abdul Majeed ◽

Rusol M. Al-Bahrani

Keyword(s):

Escherichia Coli ◽

Silver Nanoparticles ◽

Pathogenic Bacteria ◽

Inhibition Zone ◽

Inhibitory Effect ◽

Candida Guilliermondii ◽

Candida Krusei ◽

Maximum Inhibition ◽

Bacteria And Fungi ◽

Candida Zeylanoides

Silver nanoparticles synthesized from aqueous extract of mushroom Pleurotus ostreatus exhibited inhibitory effect at the concentration of 12.5, 25, 50, and 100 mg/ml against some pathogenic bacteria and fungi such as Candida albicans, Candida guilliermondii, Candida krusei, Candida zeylanoides, Geotrichum klebahnii, Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli. The maximum inhibition zone was observed against C. zeylanoides at the concentration of 100 mg/ml was 24.5 mm, while the minimum inhibition zone was observed against Geotrichum at the concentration of 25 mg/ml was 8 mm and the concentration of 12.5 mg/ml was not effective against some species.

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Antipyrine cationic surfactants capping silver nanoparticles as potent antimicrobial agents against pathogenic bacteria and fungi

Journal of Molecular Liquids ◽

10.1016/j.molliq.2017.08.072 ◽

2017 ◽

Vol 243 ◽

pp. 572-583 ◽

Cited By ~ 6

Author(s):

I. Aiad ◽

Magda I. Marzouk ◽

Soheir A. Shaker ◽

Nagwa E. Ebrahim ◽

Ali A. Abd-Elaal ◽

...

Keyword(s):

Silver Nanoparticles ◽

Cationic Surfactants ◽

Pathogenic Bacteria ◽

Antimicrobial Agents ◽

Bacteria And Fungi

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Novel (+)-Neoisopulegol-Based O-Benzyl Derivatives as Antimicrobial Agents

International Journal of Molecular Sciences ◽

10.3390/ijms22115626 ◽

2021 ◽

Vol 22 (11) ◽

pp. 5626

Author(s):

Tam Minh Le ◽

Thu Huynh ◽

Fatima Zahra Bamou ◽

András Szekeres ◽

Ferenc Fülöp ◽

...

Keyword(s):

Antimicrobial Activity ◽

Antimicrobial Agents ◽

Substituent Effects ◽

Moderate Activity ◽

Gram Negative Bacteria ◽

Gram Positive Bacteria ◽

Urgent Task ◽

Bacteria And Fungi ◽

Antibacterial And Antifungal ◽

Derivatives Of

Discovery of novel antibacterial agents with new structures, which combat pathogens is an urgent task. In this study, a new library of (+)-neoisopulegol-based O-benzyl derivatives of aminodiols and aminotriols was designed and synthesized, and their antimicrobial activity against different bacterial and fungal strains were evaluated. The results showed that this new series of synthetic O-benzyl compounds exhibit potent antimicrobial activity. Di-O-benzyl derivatives showed high activity against Gram-positive bacteria and fungi, but moderate activity against Gram-negative bacteria. Therefore, these compounds may serve a good basis for antibacterial and antifungal drug discovery. Structure–activity relationships were also studied from the aspects of stereochemistry of the O-benzyl group on cyclohexane ring and the substituent effects on the ring system.

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