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

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.

Synthesis and Biological Evaluation of Benzothiazole-piperazinesulfonamide Conjugates and Their Antibacterial and Antiacetylcholinesterase Activity

2019 ◽  
Vol 16 (9) ◽  
pp. 723-734
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana R. Katiki ◽  
Kommula Dileep ◽  
C. Ganesh Kumar ◽  
G. Narender Reddy ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Reference Drug ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation

Two series of N-2-benzothiazolyl-4-(arylsulfonyl)-1-piperazineacetamides/propanamides were synthesized from substituted 2-aminobenzothiazoles and were assayed for their in vitro antimicrobial activities against a panel of different pathogenic bacterial strains such as Micrococcus luteus, S. aureus, S. aureus MLS-16, B. subtilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella planticola and Candida albicans. Among the synthesized compounds 5e,f,g and 6g,h,i showed promising antifungal activity against C. albicans as compared to the reference drug, miconazole. Further, compounds 6g,h,i showed broad spectrum antibacterial activity against all the tested bacterial strains, while the compounds 6a-f,j-m showed significant antibacterial activity against all the tested bacterial strains as compared to the reference drug, ciprofloxacin. In addition, the target compounds were evaluated for their acetylcholinesterase (AChE) inhibitory activity, and, among the tested, compounds 5j,k,l and 6i showed promising AChE inhibitory activity.

scholarly journals BIOLOGICAL EVALUATION, QSAR AND MOLECULAR MODELING STUDIES OF 2,4-DICHLOROBENZOIC ACID DERIVATIVES AS ANTIMICROBIAL AGENTS

2019 ◽  
pp. 98-105
Author(s):  
SAMRIDHI THAKRAL ◽  
VIKRAMJEET SINGH
Keyword(s):  
Molecular Modeling ◽  
Antimicrobial Agents ◽  
Structural Characteristics ◽  
Docking Simulation ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Bacterial Strains ◽  
Qsar Studies ◽  
Antimicrobial Potential

Objective: The aim of this study was to evaluate 2,4-dichlorobenzoic acid derivatives as antimicrobial agents through in vitro, QSAR and molecular docking studies. Methods: The compounds were subjected to in vitro antimicrobial screening by test tube dilution method and the structural characteristics governing the antimicrobial potential were studied using QSAR methodology. These compounds were also screened for docking simulation to find out binding confirmation of reported compounds with PDB 1aj0 and 5fsa using AutoDock tools and discovery studio. Results: The antimicrobial evaluation data indicated that compounds 13 and 18 were found to be the most effective against all the bacterial strains and Aspergillus niger while compounds 1 and 14 exhibited more antifungal potential against Candida albicans. QSAR studies confirmed the role of molar refractivity and Balaban index (J) as controlling parameters for antimicrobial potential. Molecular modeling study revealed that compounds interact with the active site of PDB by hydrophobic, hydrogen bonding, and Van der Wall interactions. Conclusion: These test compounds were identified as potent candidates for the control of microbial strains tested, and structural relationship with activity may provide valuable information for further design and synthesis of compounds with antimicrobial potential.

scholarly journals Synthesis of sulfonamides bearing 1,3,5-triarylpyrazoline and 4-thiazolidinone moieties as novel antimicrobial agents

2020 ◽  
Vol 85 (2) ◽  
pp. 155-162
Author(s):  
Thi-Dan Thach ◽  
Thi Le ◽  
Thien-Annguyen Nguyen ◽  
Chi-Hien Dang ◽  
Van-Su Dang ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Significant Inhibition ◽  
Mercaptoacetic Acid ◽  
Bacterial Strains ◽  
Reference Drug ◽  
E Coli ◽  
Yeast Strains ◽  
Microbial Strains

Two series of sulfonamides were synthesized from 4-hydrazinylbenzenesulfonamide as the key starting material. 1,3,5-Triarylpyrazoline sulfonamides (2a?i) were obtained by cyclocondensation of various chalcones in 53? ?64 % yields, while 4-thiazolidinone derivatives (4a?e) were synthesized by cyclocondensation between mercaptoacetic acid and different phenylhydrazones in 43?62 % yields. The synthesized compounds were characterized based on FTIR, 1H-NMR, 13C-NMR and HRMS data. The sulfonamides were evaluated for their in vitro antimicrobial activities against four bacterial strains (E. coli, P. aeruginosa, B. subtillis and S aureus), two filamentous fungal strains (A. niger and F. oxysporum) and two yeast strains (C. albicans and S. cerevisiae). Seven pyrazolines, 2a?c and 2e?h, exhibited significant inhibition of different microbial strains. Among them, compound 2b displayed good antifungal activity against A. niger (MIC value at 12.5 ?g mL-1) over the reference drug.

scholarly journals Novel 2,4,6-Trimethylbenzenesulfonyl Hydrazones with Antibacterial Activity: Synthesis and In Vitro Study

Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2723
Author(s):  
Łukasz Popiołek ◽  
Sylwia Szeremeta ◽  
Anna Biernasiuk ◽  
Monika Wujec
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Potential Application ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Condensation Reaction ◽  
In Vitro Study ◽  
In Vitro Bioactivity ◽  
Bacterial Strains

This research describes the synthesis and in vitro antimicrobial activity study of a series of 2,4,6-trimethylbenzenesulfonyl hydrazones. Twenty-five hydrazones (2–26) were synthesized on the basis of condensation reaction. The in vitro bioactivity study confirmed the potential application of obtained derivatives as antimicrobial agents. Among the tested compounds, the highest activity was discovered for derivative 24, which possessed minimal inhibitory concentration (MIC) ranging from 7.81 to 15.62 µg/mL against Gram-positive reference bacterial strains. Synthesized benzenesulfonyl hydrazones can be applied as potential ligands for the synthesis of bioactive metal complexes.

scholarly journals Promising Antidiabetic and Antimicrobial Agents Based on Fused Pyrimidine Derivatives: Molecular Modeling and Biological Evaluation with Histopathological Effect

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2370
Author(s):  
Fatma Bassyouni ◽  
Mohammad Tarek ◽  
Abeer Salama ◽  
Bassant Ibrahim ◽  
Sawsan Salah El Dine ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
In Vivo Studies ◽  
Total Serum ◽  
Histopathological Study ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Pyrimidine Derivatives ◽  
Reference Drug

Diabetes is the most common metabolic disorder in both developing and non-developing countries, and a well-recognized global health problem. The WHO anticipates an increase in cases from 171 million in 2000 to 366 million by 2030. In the present study, we focus on the preparation of pyrimidine derivatives as potential antidiabetic and antimicrobial agents. Thein vivoeffect on total serum glucose concentration, cholesterol and antioxidant activity was assessed in adult male albino Wister rats and compared to the reference drug glimperide. Promising results were observed for compound 5. The histopathological study confirms that compound 5 results in significant activity with liver maintenance. The antimicrobial activities were evaluated against several bacterial strains such as Salmonella typhimurium ATCC 25566, Bacillus cereus, Escherichia coli NRRN 3008, Pseudomonas aeruginosa ATCC 10145, Staphylococcus aureus ATCC 6538and fungi such as Rhizopus oligosporus, Mucor miehei and Asperillus niger. Compounds 4 and 5 showed a good inhibition of the bacterial zone compared to the reference drug cephradine. Finally, we suggest protein targets for these drugs based on computational analysis, and infer their activities from their predicted modes of binding using molecular modeling. The molecular modeling for compounds 4 and 5 resulted in improved docking scores and hydrogen bonding. The docking studies are in good agreement with the in vitro and in vivo studies.

scholarly journals Synthesis and biological evaluation of some new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as antimicrobial agents

2022 ◽  
Vol 11 (1) ◽  
pp. 75-82 ◽  
Author(s):  
Iryna Myrko ◽  
Taras Chaban ◽  
Vasyl Matiychuk
Keyword(s):  
Mass Spectrometry ◽  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Synthesis And Biological Evaluation

A series of some new pyrazole-substituted 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines was synthesized in this study. The structures of target substances were confirmed by using 1H and 13С NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds have been evaluated for antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial screening studies of synthesized substances established that 2 of 12 compounds show pronounced antibacterial activity against the strain Staphylococcus aureus.

scholarly journals A Chimeric Cationic Peptide Composed of Human β-Defensin 3 and Human β-Defensin 4 Exhibits Improved Antibacterial Activity and Salt Resistance

2021 ◽  
Vol 12 ◽  
Author(s):  
Wenjing Yu ◽  
Nianzhi Ning ◽  
Ying Xue ◽  
Yanyu Huang ◽  
Feng Guo ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
A549 Cells ◽  
Multidrug Resistant ◽  
Salt Resistance ◽  
High Salt ◽  
Resistant Isolate ◽  
Klebsiella Pneumonia ◽  
Staphyloccocus Aureus

Human beta-defensins (hBDs) play an important role in the host defense against various microbes, showing different levels of antibacterial activity and salt resistance in vitro. It is of interest to investigate whether can chimeric hBD analogs enhanced antibacterial activity and salt resistance. In this study, we designed a chimeric human defensin, named H4, by combining sequences of human beta-defensin-3 (hBD-3) and human beta-defensin-4 (hBD-4), then evaluated its antibacterial activity, salt resistance, and cytotoxic effects. The result showed that the antibacterial activity of H4 against most tested strains, including Klebsiella pneumonia, Enterococcus faecalis, Staphyloccocus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumonia, and Acinetobacter baumannii was significantly improved compared to that of hBD-3 and hBD-4. Notably, H4 exhibited significantly better antibacterial activity against multidrug resistant isolate A. baumannii MDR-ZJ06 than commonly used antibiotics. Chimeric H4 still showed more than 80% antibacterial activity at high salt concentration (150 μM), which proves its good salt tolerance. The cytotoxic effect assay showed that the toxicity of H4 to Hela, Vero, A549 cells and erythrocytes at a low dose (<10 μg/ml) was similar to that of hBD-3 and hBD-4. In conclusion, given its broad spectrum of antibacterial activity and high salt resistance, chimeric H4 could serve as a promising template for new therapeutic antimicrobial agents.

Modifications of Isoalantolactone Leading to Effective Antibacterial and Antiviral Compounds

2020 ◽  
Vol 17 ◽  
Author(s):  
Sergey S. Patrushev ◽  
Lyubov G. Burova ◽  
Anna A. Shtro ◽  
Tatyana V. Rybalova ◽  
Dmitry S. Baev ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antiviral Activity ◽  
Influenza A ◽  
Antimicrobial Agents ◽  
Sesquiterpene Lactones ◽  
Biological Properties ◽  
Bacterial Strains ◽  
E Coli ◽  
Wide Range

Background: Natural sesquiterpene lactones are an important class of heterocyclic compounds in drug discovery since they are possessed a wide range of biological properties including antibacterial activity. Objective: The objective of this study was to synthesize of isoalantolactone derivatives with a furo[2,3-d]pyrimidin-2-оne moiety and to evaluate their antibacterial and antiviral activity. Methods: The Sonogashira cross-coupling and subsequent Ag-catalyzed cyclization reactions were the main routes of synthesis. The antibacterial activity and the ability to inhibit biofilms formation on E. coli, S. aureus, A. viscosus, P. aeruginosa and E. faecalis bacterial strains were evaluated. A study of the molecular interactions of new compounds with the multiple virulence factor regulators was performed using docking simulations. The antiviral activity against influenza A virus and human orthopneumovirus H-2А was also studied. Results: The in vitro antibacterial activity for 4 (MIC = 58.33±4.41 μg/mL) concerning E. coli and 5 (MIC = 96.5±3.25 μg/mL) against A. viscosus and the inhibition of biofilm formation for compounds 2, 4, and 5 on E. coli, S. aureus, P. aeruginosa and E. faecalis bacterial strains has been of interest for the search of improved antimicrobial agents. Compound 3 was endowed with antiviral activity to human orthopneumovirus H-2А with SI >33. The activity of the new type of hybrid compounds is depended on the substituent in the 6th position of furo[2,3-d]pyrimidin-2-one fragment. Conclusion: The decoration of isoalantolactone with a furo[2,3-d]pyrimidin-2-one fragment led to perspective antiviral and antimicrobial agents. Due to antimicrobial activity, pyridine-4-yl substituted isoalantolactone-furopyrimidinone hybrid is considered as a candidate compound to participate in further research.

Evaluation of Antibacterial Activity of Acer syriacum by Bioautography Method

1970 ◽  
Vol 9 (2) ◽  
pp. 3215-3219
Author(s):  
B. Al Asfour ◽  
R. Al-kayali ◽  
A. Kitaz
Keyword(s):  
Antibacterial Activity ◽  
Methanolic Extract ◽  
Ethyl Acetate Extract ◽  
Diffusion Method ◽  
Klebsiella Pneumonia ◽  
Bacterial Strains ◽  
In Vitro Antibacterial Activity ◽  
Inhibition Zones ◽  
Layer Chromatography

antibacterial activity of leaves, fruits and bark of acer syriacum was evaluated against both negative and positive gram bacterial strains. The powder of above parts were sequentially extracted with aqueous methanol 80%, acetone and petroleumether by maceration. The in vitro antibacterial activity of A. syriacum extracts (in concentration of 200 mg/mL) was performed by agar well diffusion method. Among the tested extracts, leaves methanolic extract has shown the highest growth inhibition. Further, the extract was fractionated, separated by thin layer chromatography (TLC) and submitted to bioautography. the results indicate that the ethyl acetate extract had  the most efficient antibacterial  compounds that displayed inhibition zones (25 mm) against Staphylococcus aureus ATCC25923 and (28mm) against Klebsiella pneumonia ATCC700603. the clear zones were located at RF= 0.15.

scholarly journals Chemical Composition and Antibacterial Activity of Melaleuca bracteata Essential Oil from India: A Natural Source of Methyl Eugenol

2017 ◽  
Vol 12 (6) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Prakash Goswami ◽  
Sajendra K. Verma ◽  
Amit Chauhan ◽  
KT Venkatesha ◽  
Ram S. Verma ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
Methyl Eugenol ◽  
Klebsiella Pneumonia ◽  
Moderate Activity ◽  
Bacterial Strains ◽  
Indian Origin ◽  
Total Oil ◽  
Autumn And Winter

The aim of this study was to investigate the chemical composition and antibacterial activity of the essential oil of Melaleuca bracteata F. Muell from India. The hydrodistilled essential oils of M. bracteata in spring, summer, rainy, autumn and winter seasons were analyzed using GC-FID and GC-MS. Altogether, 25 constituents, comprising 97.3–99.7% of the total oil were identified with methyl eugenol (87.2–89.5%), ( E)-methyl cinnamate (2.8–5.4%), methyl chavicol (0.2–0.5%), and elemicin (0.2–0.4%) as major constituents. The antibacterial efficacy of the essential oil was evaluated against nine pathogenic bacterial strains. Zone of inhibition and MIC of the essential oil ranged from 5–10 mm and 500–1000 μg/mL against the tested pathogens, respectively. Results showed that essential oil of M. bracteata from Indian origin possessed good activity against Salmonella typhimurium, Staphylococcus epidermidis, and moderate activity against Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumonia, and Streptococcus mutans. Results of the present seasonal variation study clearly indicated that M. bracteata grown in foothills of Uttarakhand, India could be classified as seasonally stable ‘methyl eugenol’ chemotype (>85.0%), hence may be considered as a novel natural resource for methyl eugenol rich essential oil for flavor, fragrance and pharmaceutical applications.

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