scholarly journals An Efficient Synthesis of Thiophene Conjugated Benzothiazepines: in vitro Screening for their Antimicrobial Activity

2020 ◽  
Vol 32 (10) ◽  
pp. 2601-2605
Author(s):  
K.R. Raghavendra ◽  
P. Sudeep ◽  
K. Ajay Kumar ◽  
H.P. Jayadevappa
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Spectroscopic Studies ◽  
In Vitro Screening ◽  
Efficient Synthesis ◽  
Citrus Juice ◽  
E Coli ◽  
Antimicrobial Evaluation ◽  
New Compounds

A series of novel thiophene conjugated benzothiazepines were synthesized by the reaction of chalcones with 2-aminobenzenethiol in citrus juice medium. The new compounds were characterized by spectroscopic studies. Results of in vitro antimicrobial evaluation of newly synthesized compounds 5a-j shows that the compounds 5a and 5c have excellent antimicrobial inhibition in the range of 12.5-25.0 μg/mL against bacteria S. aureus, E. coli, P. aeruginosa and fungi A. niger, A. flavus organisms comparable to ciprofloxacin and nystatin and therefore these compounds might acts as lead molecules as antimicrobial agents.

Synthesis and Antimicrobial Evaluation of 2-(Substituted-phenyl)-3-(4-(4- Nitrophenyl)Thiazol-2-yl)Thiazolidin-4-One Derivatives

2019 ◽  
Vol 15 (1) ◽  
pp. 114-119 ◽  
Author(s):  
Rakesh Kumar ◽  
Shailendra Patil
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Public Health Issue ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Microbial Infections ◽  
Antimicrobial Evaluation ◽  
Potential Antimicrobial Activity ◽  
Tube Dilution

Background:Diseases caused by microbial infections are very common worldwide. Although the search of innovative antimicrobial agents is the current focus for the researchers, the treatment of infectious diseases remains an important public health issue and a challenging problem in front of medicinal chemist.Methods:A series of 2-(4-hydroxyphenyl)-3-(4-(4-nitrophenyl) thiazol-2-yl)thiazolidin-4-one derivatives (T1-T10) was designed and synthesized. All the titled compounds were evaluated for their antimicrobial potential. Antimicrobial activity was performed by tube dilution methods against Gram negative Escherichia coli MTCC 443 (E. Coli), Gram positive bacteria: Staphylococcus aureus MTCC 3160 (S. aureus) and Bacillus subtilis MTCC 441 (B. Subtilis), and fungal strains: Aspergillus niger MTCC 281 (A. niger) and Candida albicans MTCC 227 (C. albicans).Results:Among the synthesized derivatives, compounds 2, 4 and 10 were found to be most active antimicrobial agents.Conclusion:In conclusion, a series of 2-(phenyl)-3-(4-(phenyl)thiazol-2-yl)thiazolidin-4-ones have been designed and synthesized. All the titled compounds were evaluated for their in vitro antimicrobial activity against five representative microorganisms. The results of antimicrobial study indicated that the presence of nitro and chloro groups in aromatic ring improved antibacterial activity, whereas the presence of hydroxy group improved antifungal activity of substituted 4-thiazolidinone derivatives.

scholarly journals Synthesis and Study of Some Newer Analogues ofQuinolin-8-ol as Potent Antimicrobial Agents

2008 ◽  
Vol 5 (s1) ◽  
pp. S1008-S1014
Author(s):  
Jyoti Sharma ◽  
Sabir Hussain ◽  
Mohammad Amir
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Antifungal Agents ◽  
Gram Negative ◽  
E Coli ◽  
H Nmr ◽  
Gram Negative Organisms ◽  
New Compounds

New series of 4-(substituted phenyl)-5-[(quinolin-8-yloxy) methyl]-4H-1,2,4-triazole-3-thiol(4a-c),N³-(4-substituted phenyl)-5-[(quinolin-8-yloxy) methyl]-4H-1,2,4-triazole-3,4-diamine(5a-c)andN-(4-substituted phenyl)-5-[(quinolin-8-yloxy) methyl]-1,3,4-thiadiazol-2-amine(6a-g)have been synthesized and the structures of the new compounds were established on the basis of IR,1H NMR spectral data.In vitroantimicrobial activity (MIC activity) was evaluated and compared with standard drugs of loxacin and ketoconazole. Compounds5aand6ein the series have shown interesting antibacterial activity against bothS. aureus(gram-positive) andE. coli(gram-negative) organisms. In this paper, we also describe studies leading to identification of antifungal agents. In the gratifying result, most of the compounds were found to have moderate antimicrobial activity.

scholarly journals Synthesis, Antimicrobial Activity and Molecular Docking of Novel Thiourea Derivatives Tagged with Thiadiazole, Imidazole and Triazine Moieties as Potential DNA Gyrase and Topoisomerase IV Inhibitors

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2766 ◽  
Author(s):  
Heba E. Hashem ◽  
Abd El-Galil E. Amr ◽  
Eman S. Nossier ◽  
Elsayed A. Elsayed ◽  
Eman M. Azmy
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Topoisomerase Iv ◽  
Thiourea Derivatives ◽  
E Coli ◽  
Cytotoxicity Studies ◽  
Ic50 Values

To develop new antimicrobial agents, a series of novel thiourea derivatives incorporated with different moieties 2–13 was designed and synthesized and their biological activities were evaluated. Compounds 7a, 7b and 8 exhibited excellent antimicrobial activity against all Gram-positive and Gram-negative bacteria, and the fungal Aspergillus flavus with minimum inhibitory concentration (MIC) values ranged from 0.95 ± 0.22 to 3.25 ± 1.00 μg/mL. Furthermore, cytotoxicity studies against MCF-7 cells revealed that compounds 7a and 7b were the most potent with IC50 values of 10.17 ± 0.65 and 11.59 ± 0.59 μM, respectively. On the other hand, the tested compounds were less toxic against normal kidney epithelial cell lines (Vero cells). The in vitro enzyme inhibition assay of 8 displayed excellent inhibitory activity against Escherichia coli DNA B gyrase and moderate one against E. coli Topoisomerase IV (IC50 = 0.33 ± 1.25 and 19.72 ± 1.00 µM, respectively) in comparison with novobiocin (IC50 values 0.28 ± 1.45 and 10.65 ± 1.02 µM, respectively). Finally, the molecular docking was done to position compound 8 into the E. coli DNA B and Topoisomerase IV active pockets to explore the probable binding conformation. In summary, compound 8 may serve as a potential dual E. coli DNA B and Topoisomerase IV inhibitor.

scholarly journals Synthesis and Antimicrobial Evaluations of Sulfur Inserted Fluoro-Benzimidazoles

2021 ◽  
Vol 33 (7) ◽  
pp. 1525-1529
Author(s):  
Parmesh Kumar Dwivedi ◽  
Devdutt Chaturvedi
Keyword(s):  
Antimicrobial Agents ◽  
Bacterial Strains ◽  
Substituted Anilines ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
New Compounds ◽  
Derivatives Of ◽  
Multiple Step

A new series of fluorinated sulfur inserted benzimidazole analogues Za-i were synthesized and characterized. The new compounds were screened for their antimicrobial and antioxidant potential. The synthesized compounds were obtained by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol X. The compounds Ya-i prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF. Finally, the compound X was reacted with different derivatives of 2-chloro-N-phenylacetamide resulting in formation of titled compounds Za-i. The synthesized compounds (Za-Zi) were characterized by spectral analysis viz.1H & 13C NMR, mass spectra, elemental analysis and IR. The in vitro antimicrobial potential against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans) was recorded for the obtained compounds. Some of the compounds exhibited encouraging results (in MIC) against Gram-positive and Gram-negative bacterial strains. These studies thus suggest that the designed sulfur inserted fluoro-benzimidazoles scaffold may serve as new promising template for further amplification as antimicrobial agents.

scholarly journals Amidoalkylation of heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]- 2'-chloroacetamide and antimicrobial activity of derivatives

2021 ◽  
Vol 10 (4) ◽  
pp. 427-434 ◽  
Author(s):  
Turdibek Toshmurodov ◽  
Abdukhakim Ziyaev ◽  
Sobirdjan Sasmakov ◽  
Jaloliddin Abdurakhmanov ◽  
Mavluda Ziyaeva ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Inhibition Zone ◽  
Heterocyclic Amines ◽  
Gram Negative Bacteria ◽  
In Vitro Screening ◽  
Gram Negative ◽  
Inhibition Zone Diameter ◽  
Gram Positive Bacteria ◽  
New Compounds

Amidoalkylation of secondary heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-chloroacetamide resulted the new compounds 5-10 that contain 1,3,4-thiadiazole-5-thione moiety alongside pyperidine, morpholine, and cytisine fragments. In vitro screening of antimicrobial activity of synthesized compounds showed that N-[5-(amylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-morpholinacetamide exhibited an appreciable antibacterial activity against gram-negative bacteria of Escherichia coli (inhibition zone diameter of 16 mm) and gram-positive bacteria of Staphylococcus aureus and Bacillus subtilis (10-13 mm).

Preparation of a Novel Complex Antimicrobial Agent and its Antimicrobial Activity In Vitro

2012 ◽  
Vol 550-553 ◽  
pp. 1030-1038
Author(s):  
Peng Li ◽  
Wei Guo Wang ◽  
Yu Jia Cui ◽  
Yong Liang Zhao ◽  
Ya Nan Gu ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antimicrobial Agent ◽  
Antimicrobial Agents ◽  
E Coli ◽  
Orthogonal Experiments ◽  
Novel Complex ◽  
Cefoperazone Sodium ◽  
Complex Antimicrobial Agent

Purpose To develop a novel complex antimicrobial agent and determine the optimal components of the composite antimicrobial agents and its antimicrobial activity in vitro. Methods According to antimicrobial mechanisms，antibacterial spectrums，physical and chemical properties and applicabilities of existing antimicrobial agents in clinical use, select out cefoperazone sodium, sulbactam sodium and cephradine as the basic components to make a novel complex antimicrobial agent. Utilize yeast, staphylococcus aureus and E. coli bacteria as test bacteria. Do the three factors four-level orthogonal experiments by the maximum amount, the middle amount, low amount and Minimum amount of the three-component agent to research the optimum ratio of the drug. Measure the titer of the compound antimicrobial agent by the way of tube-plate method (2 doses). With known contents of Penicillin Sodium for Injection as control, and determine its minimum inhibitory concentration against staphylococcus aureus, E. coli and yeast by using the agar doubling dilution method. The experimental results were analysized by statistical analysis software SPSS16.0. Results The results of the three factors four-level orthogonal experiments indicate the optimum ratios of Cefoperazone Sodium, Sulbactam Sodium and Cephradine against E. coli, yeast and staphylococcus aureus were 2:2:3, 1:2:2 and 2:6:5, their titers were 1353.9U/mg, 982.7U/mg and 1015.5U/mg. With the highest titer proportion 2:2:3 as the composition of the antimicrobial compound. This compound antimicrobial agent had a good antimicrobial activity against Gram-positive bacteria, Gram-negative bacteria and Fungi, its minimal inhibitory concentration (MIC) against staphylococcus aureus, E. coli and yeast were 2.000μg/ml, 0.500μg/ml and 16.000μg/ml. Conclusion This research acquires a composite of antibiotics. This antimicrobial compound has a broader spectrum and higher antimicrobial activity in vitro comparing with traditional common single antibiotics, and it especially has a good antimicrobial activity against fungi. The results set a scientific foundation for enriching clinical medicines.

scholarly journals Synthesis and antimicrobial evaluation of some 4-quinolinylazo-N-pyrimidinyl benzenesulfonamide derivatives

2019 ◽  
Vol 10 (1) ◽  
pp. 4846-4852
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Antimicrobial Agents ◽  
Chloroacetyl Chloride ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Chemical Structures ◽  
Antimicrobial Evaluation ◽  
New Compounds

Ten new compounds of quinoline clubbed with sulfonamide moiety were synthesized to be used as antimicrobial agents. Therefore, the diazotized N-(pyrimidin-2-yl)-benzenesulfonamide was diazocoupled with 8-hydroxyquinoline to furnish 4-(8-hydroxyquinolin-5-yl)-N-(pyrimidin-2-yl)benzenesulfonamide (3) which underwent chloroacetylation by chloroacetyl chloride to give the corresponding O-chloroacetylated product 6. The reactions of quinolinyl 2-chloroacetate derivative 6 with different nucleophiles (ethyl 2-mercaptoacetate, 2-mercapto-4,6-dimethylnicotinonitrile, o-aminothiophenol and/or malononitrile) were studied and utilized to pick up various heterocyclic systems 7, 10, 12 and 14. The chemical structures of newly prepared quinoline-containing scaffolds have been confirmed based on their spectral data (IR, 1H NMR and MS) and have been tested for their antimicrobial activity. The results showed that compounds 5d, 6, 7 and 14 displayed the highest activity against Gram-positive bacteria.

scholarly journals Anti-microbial activity of heterocyclic cationic surface-active substances

2020 ◽  
Vol 24 (1) ◽  
pp. 36-40
Author(s):  
V. V. Pantyo ◽  
M. M. Fizer ◽  
O. I. Fizer ◽  
G. M. Koval ◽  
E.M. Danko
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Pathogenic Microorganisms ◽  
Disk Diffusion Method ◽  
E Coli ◽  
Quantitative Studies ◽  
Ionic Associates ◽  
Surface Active

Annotation. The development and rapid pace of the spread of resistance to antimicrobial agents predetermines the search for new methods of counteracting pathogenic and conditionally pathogenic microorganisms. In this context, studies of the antimicrobial activity of newly synthesized chemicals, which in the future can be considered as candidates for antiseptic and disinfectants, are relevant. The aim of the work was to determine the antimicrobial activity of new ionic associates based on the surface-active cetylpyridinium cation with respect to certain opportunistic microorganisms. The antimicrobial activity of four ionic associates based on the cetylpyridinium cation with respect to clinical isolates of E. coli, P. vulgaris, K. pneumonia, P. aeruginosa, S. aureus, as well as the collection test strains of S. aureus ATCC 25923, E. coli ATCC 29522 and P. aeruginosa ATCC 27853 was studied. Screening studies were performed by the disk diffusion method. With substances that showed an antimicrobial effect, quantitative studies were carried out by the method of serial macro-dilutions in a liquid nutrient media. Screening studies revealed the antibacterial activity of the substances against E. coli ATCC 25923, E. coli (clinical isolate), P. vulgaris and K. pneumonia. With these microorganisms quantitative studies were carried out with the determination of the minimum inhibitory and minimum bactericidal concentrations. The most pronounced antimicrobial activity for the investigated microflora was shown by tetraphenylborate and cetylpyridinium perchlorate. The MIC and MBC values of these substances ranged between 1.625–3.125 mmol / L and 3.125–12.5 mmol / L, respectively. The studied associates showed high antimicrobial activity against representatives of the Enterobacteriaceae family in in vitro studies. Promising is the further study of the effect of the counter-anion associates of cationic surfactants on the biofilm formation of conditionally pathogenic microorganisms.

scholarly journals Synthesis and in vitro antimicrobial activity of new steroidal hydrazone derivatives

2022 ◽  
Vol 8 (1) ◽  
Author(s):  
Shailesh Mistry ◽  
Akhilesh Kumar Singh
Keyword(s):  
Antimicrobial Activity ◽  
Infectious Diseases ◽  
Antimicrobial Agent ◽  
Spectral Data ◽  
Induced Resistance ◽  
Antimicrobial Agents ◽  
In Vitro Antimicrobial Activity ◽  
Bacteria And Fungi ◽  
New Compounds

Abstract Background For many years, various drugs have been used for the treatment of infectious diseases but some bacterial microorganisms have induced resistance to several drugs. In a search of new antimicrobial agents, a series of new steroidal hydrazones were designed and synthesized. Result The structures of the compounds were established based on the spectral data. The in vitro antimicrobial activity of some newly synthesized compounds against bacteria and fungi was studied. Conclusion New compounds showed better or similar antimicrobial activity. Designing more efficient steroidal hydrazones from ketosteroid based on the current study may successfully lead to the development of antimicrobial agent. Graphical abstract

Synthesis and Structural Elucidation of Aminoacetylenic Derivatives of 7-Methoxy- 2-Naphthole as Antimicrobial Agents

2017 ◽  
Vol 9 (08) ◽  
Author(s):  
Abu- Safieh Rana ◽  
Muhi- Eldeen Zuhair ◽  
Alsarahni Aseel ◽  
Al-Kaissi Elham
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Naphthalene Derivatives ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi ◽  
Aminoacetylenic Derivatives ◽  
Derivatives Of ◽  
Mic Value

A new series of 7-methoxy-2-[4-(t-amino-1-yl)oxy]-naphthalene derivatives; 7-methoxy-2-{[4-(2-methylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ2), 7-methoxy-2-{[4-(2,6-dimethylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ3), 7-methoxy-2{[4-(piperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ4), 7-methoxy-2-{[4-(pyrrolidine)but-2-yn-1-yl]oxy}-naphthalene (RZ5), 7-methoxy-2-{[4-(N-methylpiperazine)but-2-yn-1-yl]oxy}-naphthalene (RZ6), 7-methoxy -2-{[4-(hexamethyleneimine)but-2-yn-1-yl]oxy}-naphthalene (RZ7) were synthesized and screened in vitro as potential antimicrobial agents. Antimicrobial activity were evaluated by measuring the minimum inhibitory and bactericidal/fungicidal concentration (MIC, MBC and MFC). RZ2, RZ5, RZ6 and RZ7 showed the highest antimicrobial activity against S. aureus with MIC value 62.5 µg/ml, compounds RZ2, RZ4, RZ5, and RZ7 have the highest antimicrobial activity against B. subtilis with MIC vale 62.5 µg/ml, RZ3, RZ6 have the same antimicrobial activity with MIC value 125µg/ml, compounds. RZ4, RZ5, RZ6 and RZ7 have the highest antimicrobial activity against E. coli with MIC value 125 µg/ml, all compounds have the same MIC value against P. aeruginosa (125 µg/ml). RZ2, RZ4, RZ5, RZ6, RZ7 showed the highest antifungal activity with MIC of 62.5 µg/ml. In conclusion, the synthesized compounds showed good antimicrobial activity and promising potency against gram positive bacteria, gram negative bacteria and fungi.

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