scholarly journals Synthesis, Characterization and Antimicrobial Evaluation of some 1,2,4-Triazolo-5-Thione Derivatives

2021 ◽  
Vol 11 (1) ◽  
pp. 24-30
Author(s):  
Gurdeep Singh ◽  
◽  
Neetesh K. Jain ◽  
Kiran Sahu ◽  
◽  
...  

Due to this increasing predicament of antibiotic confrontation, the lot of distinct antibiotics available is dwindling and there are only smatterings of new antibiotics in the drug development channel. Therefore, an intense necessitate for new antimicrobial drugs. In current study, substituted 1,2,4-triazolo-5-thione derivatives were synthesized from substituted aromatic aldehydes, succinic acids and the structure of synthesized compounds were established by physicochemical (Melting Point, Rf value) and spectral analysis (IR, NMR & Mass). The title compounds were then evaluated for their antimicrobial activity against ciprofloxacin as a standard drug using agar plate method. Among all synthesized derivatives A5 and A6 found were found to possess very promising antimicrobial activity. Keywords: 1,2,4-triazolo-5-thione, anti-microbial, antibiotic, thione, Ciprofloxacin.

2020 ◽  
Vol 17 ◽  
Author(s):  
Cheenu Chaudhary ◽  
Sushil Kumar ◽  
Surendra Kumar ◽  
S. Riaz Hashim

: The present investigation aim to synthesize quinazoline-4(3H)-one derivatives (B1-10) and evaluation for their antimicrobial activity. The test compounds (B1-10) were obtained by reaction of 2-phenyl-4H-benzo[d] [1, 3]oxazin-4-one (1) with 4-aminophenol (2) to afford 3-(4-hydroxyphenyl)-2-phenylquinazoline-4(3H)-one (3) which further reacted with different N-phenylacetamide (4) in presence of anhydrous potassium carbonate and catalytic amount of potassium iodide in ethylmethylketone. The test compounds (B1-10) were characterized by spectroscopic method and evaluated for their antimicrobial activity using cup plate method by measuring zone of inhibition. Among the compounds, compound B1, B2, B4, B6 and B8 showed maximum zone of inhibition as compare with standard drug ciprofloxacin and fluconazole against Bacillus subtilis, Escherichia coli and Aspergillus niger. Molecular docking was also performed for test compounds to predict their binding affinities in the target protein and results showed good drug-like properties


Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.


2008 ◽  
Vol 5 (3) ◽  
pp. 461-466 ◽  
Author(s):  
Y. Rajendra Prasad ◽  
A. Lakshmana Rao ◽  
R. Rambabu

In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR,1H-NMR spectral data and elemental analysis. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.


Author(s):  
Khabat Noori Hussein ◽  
Tímea Molnár ◽  
Richard Pinter ◽  
Adrienn Toth ◽  
Emna Ayari ◽  
...  

AbstractThis work aimed to study the antimicrobial activity of eight various components of plant origin on the growth of Pseudomonas lundensis and Listeria monocytogenes. Different in vitro methods were used: agar plate diffusion, micro atmosphere, agar hole diffusion, micro-dilution, and gradient-plate method. In the first agar plate assay, p-cymene and γ-terpinene did not inhibit the growth of the tested bacteria therefore they were not used in further experiments. Both α-pinene and limonene were only partially effective, but these were screened only for their partial inhibition. The other four components completely inhibited the growth of the tested bacteria. Using the agar-well diffusion method showed that carvacrol and thymol were found to be the most effective active components, thymol had minimum inhibitory concentration (MIC) at 1.563 mg/mL, however, in the case of carvacrol, MIC was 7.813 μL/mL. Additionally, eugenol and camphor show the same results but in higher concentrations. Gradient plate method was used to determine MIC values, in which it has been proved that carvacrol and thymol possess strong antimicrobial activity, no growth of tested bacteria was observed with carvacrol (100 μL/mL), while thymol exhibited MIC of 1.887 mg/mL against P. lundensis and 0.943 mg/mL needed to show complete inhibition of Listeria monocytogenes. Further experiments are needed to determine the optimum concentrations of the active components against P. lundensis and L. monocytogenes.


Author(s):  
Dr.Pravina B. Piste

In the designing and synthesis of new heterocyclic compounds, containing two different pharmacophores, we have carried out new series of 3-(4-chlorophenyl)-4-methylidene-4,8-dihydro-2H,5H-1,3-thiazino[5,4-e]-1,3-oxazine-2,5,7(3H)-trione derivatives (5a-5k) in good yields from the cyclization of 5-[(1E)-N- (4-chlorophenyl) ethanimidoyl] -4-hydroxy- 2H-1,3- thiazine-2,6(3H)-dione derivatives (4a-4k) with triphosgene. All the synthesized compounds (5a-5k) were confirmed by spectral analysis. The synthesized compounds (5a-5k) were screened in vitro for their antibacterial activities against S. subtilis (gram positive) and E. coli. (gram negative) while antifungal activity against C. albicans by cup plate method. Some of the products of series were found to have quite good activities as compared to the standard drug streptomycin and flucanozole.


2019 ◽  
Vol 17 (3) ◽  
pp. 39-46 ◽  
Author(s):  
Evgeny A. Zorin ◽  
Marina S. Kliukova ◽  
Olga A. Kulaeva ◽  
Alexey M. Afonin ◽  
Igor A. Tikhonovich ◽  
...  

Background. The active and careless applying of antibiotics in medicine and agriculture leads to the emergence of resistance to the existing antimicrobial drugs, which reduces the effectiveness of their use. One of the ways to solve this problem is the development of new antibiotics based on plant peptides with antimicrobial activity, for example plant defensins (which identified in all plants) and NCR peptides that are specifically synthesized in nodules of some leguminous plants. Materials and methods. In the present study, a meta-assembly of a transcriptome was constructed based on publicly available RNA-sequencing transcriptomes of pea nodules (Pisum sativum L.). This meta-assembly was used to search for sequences encoding antimicrobial peptides. Results. As a result, 55 and 908 unique sequences encoding defensins and NCR peptides, respectively, were identified. The recognition site for the signal peptidase was predicted and sequences were divided into the signal and mature part of the peptide. Among mature defensins, 22 peptides possess in silico predicted antimicrobial activity, and for the NCR peptides family their number was 422. Conclusion. Sequences encoding defensins and NCR peptides expressed in nitrogen-fixing pea nodules were identified. They are candidates for testing their antimicrobial activity in vitro.


2018 ◽  
Vol 18 (17) ◽  
pp. 1506-1513 ◽  
Author(s):  
Kashmiri Lal ◽  
Lokesh Kumar ◽  
Ashwani Kumar ◽  
Anil Kumar

Background: Oxazolones and 1,2,3-triazoles are among the extensively studied heterocycles in medicinal chemistry. Both of these moieties are reported to possess a broad spectrum of biological activity including antimicrobial. Objective: The objective of the current work is to design, synthesize and antimicrobial evaluation of some new oxazolone-1,2,3-triazole hybrids. Methods: The designed oxazolone-1,2,3-triazole hybrids were synthesized using copper(I)-catalyzed azide-alkyne cycloaddition. The antimicrobial evaluation was carried out using serial dilution method. Results: Most of the synthesized hybrids showed significant antimicrobial properties. Some of the compounds were found to be possessing better or comparable activity to that of the standards used. The docking simulations results are also in agreement with the antimicrobial activity data. Conclusion: Sixteen new hybrids were synthesized and tested in vitro for their antimicrobial activity. Some of the tested compounds exhibited promising antimicrobial activity and could be utilized for the development of the lead compounds for new and more potent antimicrobial drugs.


2009 ◽  
Vol 6 (1) ◽  
pp. 196-200 ◽  
Author(s):  
B. A. Baviskar ◽  
Bhagyesh Baviskar ◽  
M. R. Shiradkar ◽  
U. A. Deokate ◽  
S. S. Khadabadi

Some novel benzimidazolyl chalcones were synthesized by condensation ofN-(4-(1H-benzo[d]imidazol-2-yl)phenyl)acetamide with aromatic aldehydes in presence of aqueous potassium hydroxide solution at room temperature. All the synthesized compounds were characterized on the basis of their IR,1H NMR spectroscopic data and elemental analysis. All the compounds have been screened for antimicrobial activity by the cup-plate method.


2010 ◽  
Vol 3 (1) ◽  
pp. 111 ◽  
Author(s):  
M. H. Bhuiyan ◽  
A. F. M. H. Rahman

Reaction of 2-amino-4-phenylthiazole with various aromatic aldehydes afforded 2-arylideneamino-4-phenylthiazoles. On the other hand treatment of 2-amino-4-phenylthiazole with several acyl halides furnished N-(thiazol-2-yl)-amides. The synthesized compounds have been screened for their antimicrobial activity against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Shigella dysenteriae, Salmonella typhi, Pseudomonous sp. bacteria and Aspergillus niger, Penicillium notatum, Aspergillus funiculosus, Collectrichum corchori Ikata (Yoshida) and Curvularia lunata fungi respectively. Some of the synthesized compounds exhibited pronounced antimicrobial activities.Keywords:  Aminothiazole; Arylideneaminothizole; N-(Thiazol-2-yl)-amide; Antimicrobial activity.© 2011 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi:10.3329/jsr.v3i1.5419                J. Sci. Res. 3 (1), 111-119 (2011)


Author(s):  
Hitesh Makwana ◽  
Yogesh T. Naliapara

Some new N’-benzylidene-5-bromothiophene-2-carbohydrazide derivatives possessing thiophene nucleus were synthesized and characterized by IR, NMR and mass spectral analysis. All synthesized compounds were screened for antimicrobial activity using cup plate method. All the compounds showed moderate to good antimicrobial activity and anti fungal activity


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