scholarly journals Synthesis and In Vitro Antimicrobial Evaluation of New 1,3,4-Oxadiazoles Bearing 5-Chloro-2-methoxyphenyl Moiety

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Basavapatna N. Prasanna Kumar ◽  
Kikkeri N. Mohana ◽  
Lingappa Mallesha ◽  
Kikkeri P. Harish
Keyword(s):  
Mass Spectra ◽  
Significant Activity ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Antimicrobial Studies ◽  
Antimicrobial Evaluation ◽  
Oxadiazole Derivatives ◽  
Ft Ir ◽  
Antibacterial And Antifungal

A series of new 1,3,4-oxadiazole derivatives, 4(a–h), containing 5-chloro-2-methoxy benzohydrazide moiety were synthesized by the reaction of 5-chloro-2-methoxybenzoate with different aromatic carboxylic acids. These newly synthesized compounds were characterized by FT-IR, 1H NMR, mass spectra, and also by elemental analysis. All the newly synthesized compounds were screened for their antibacterial and antifungal activities. Antimicrobial studies revealed that compounds 4c, 4f, and 4g showed significant activity against tested strains.

scholarly journals Synthesis and Antimicrobial Activity of Pyrimidine Salts with Chloranilic and Picric Acids

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
C. Mallikarjunaswamy ◽  
D. G. Bhadregowda ◽  
L. Mallesha
Keyword(s):  
Antimicrobial Activity ◽  
The Other ◽  
Spectral Studies ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Ft Ir ◽  
Uv Visible ◽  
Antibacterial And Antifungal

Pyrimidine salts such as 2-methyl-5-nitro-phenyl-(4-pyridin-3-yl-pyrimidin-2-yl)-amine (1) and 4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-yl-amino)-phenyl-amine (2) with chloranilic and picric acids were synthesized, and theirin vitroantibacterial and antifungal activities were evaluated. The synthesized compounds were characterized by elemental analyses, UV-visible, FT-IR, and1H NMR spectral studies. Compound2aexhibited good inhibition towards antimicrobial activity compared to the other compounds.

scholarly journals Synthesis, structural characterization and antimicrobial evaluation of some novel piperidin-4-one oxime esters

2015 ◽  
Vol 80 (9) ◽  
pp. 1101-1111 ◽  
Author(s):  
Gokula Krishnan ◽  
R. Sivakumar ◽  
V. Thanikachalam
Keyword(s):  
Biologically Active ◽  
Good Activity ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Xrd Study ◽  
Antimicrobial Evaluation ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Fifteen novel biologically active piperidin-4-one oxime esters (8-22) have been synthesized with good yields. These compounds were prepared from in-situ activated carboxylic acids using POCl3 and pyridine with piperidin-4- one oximes. The structure of the title compounds were elucidated on the basis of FT-IR, NMR (1D and 2D) and mass spectral analyses. The single crystal XRD study of compounds 12 and 20 were the further evidence for the proposed structure unambiguously. All the synthesized compounds were tested for in vitro antibacterial and antifungal activities. Many of these derivatives exhibited good activity against Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Trigoderma veride and Aspergillus flavus.

scholarly journals Synthesis and antimicrobial evaluation of 3-hydrazino-quinoxaline derivatives and their cyclic analoaues

2004 ◽  
Vol 72 (2) ◽  
pp. 175-185 ◽  
Author(s):  
E. R. EI-Bendary ◽  
F. E. Goda ◽  
A. R. Maarouf ◽  
F. A. Badria
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Chloroacetyl Chloride ◽  
Antibacterial And Antifungal Activities ◽  
Piperazine Derivatives ◽  
Quinoxaline Derivatives ◽  
Antimicrobial Evaluation ◽  
Antibacterial And Antifungal

A series of quinoxaline derivatives has been synthesized by reacting 3-hydrazinoquinoxalines 1a,b with many bifunctional reagents. Reaction of 1a,b with chloroacetyl chloride and ethyl chloroacetate afforded 1-chloromethyl[1,2,4]tnazoIo[4,3-a]quinoxalines 2a,b and dihydro[1,2,4]triazino[4,3-a]quinoxalin-2-ones 3a,b respectively. Condensation of 1a,b with ethyl acetoacetate and acetylacetone yielded 2-quinoxalinylhydrazonobutanoates 4a,b and 2-quinoxalinylhydrazono-2-pentanones 5a,b respectively. Cyclization of 5a,b gave 3,5-dimethylpyrazolylquinoxalines 6a,b. Moreover, reaction of compounds 2a,b with N-phenyl piperazine derivatives afforded 4-(4-Arylpiperazin-1-yl)-1-[(4-arylpiperazin-1-yl) methyl)]triazoloquinoxalines 7a−e. The prepared compounds were screened for in vitro antibacterial and antifungal activities. None of the tested compounds showed significant activity towards Pseudomonas aeruginosa. However, remarkable activities were noticed for compounds 5a and 5b against Eschenchia coli. Staphylococcus aureus and Candida albicans. Compounds 6a and 6b lacked any antimicrobial activities against the tested microorganisms.

scholarly journals Synthesis, Characterization and Molecular Docking of 1,2,4-Triazole Derivatives as Potential Antimicrobial Agents

2020 ◽  
Vol 32 (6) ◽  
pp. 1437-1442
Author(s):  
Panneerselvam Kalaivani ◽  
Jayaraman Arikrishnan ◽  
Mannuthusamy Gopalakrishnan
Keyword(s):  
Antimicrobial Agents ◽  
Docking Study ◽  
Binding Mode ◽  
Zone Of Inhibition ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Inhibition Concentration ◽  
Ft Ir ◽  
Antibacterial And Antifungal

In this study, a new series of (E)-N-(4-(3-(3,5-dialkylphenyl)acryloyl)phenyl)-2-(1H-1,2,4-triazol-1- yl)acetamide (32-41) was synthesized, characterized by FT-IR, 1H NMR, 13C NMR and Mass spectral analysis and evaluated for their in vitro antibacterial and antifungal activities. The docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of 1T9U protein. The zone of inhibition concentration was tested for the synthesized compounds against five bacterial and three fungal strains. Compounds 34 and 37 have good antibacterial activity. Compounds 3, 4 and 6 shows moderate inhibition against the antifungal activity.

Infrared, 1H-NMR Spectral Studies of some Methyl 6-O-Myristoyl-α-D-Glucopyranoside Derivatives: Assessment of Antimicrobial Effects

2015 ◽  
Vol 58 ◽  
pp. 122-136 ◽  
Author(s):  
Sarkar M.A. Kawsar ◽  
Khaleda Mymona ◽  
Refat Asma ◽  
Mohammad A. Manchur ◽  
Yasuhiro Koide ◽  
...  
Keyword(s):  
Pathogenic Fungi ◽  
Spectral Studies ◽  
Bacterial Strains ◽  
Substitution Product ◽  
Antifungal Activities ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Fungal Phytopathogens ◽  
Antibacterial And Antifungal

This study was carried out to regioselective myristoylation of methyl α-D-glucopyranoside (1) using the direct acylation method gave the corresponding methyl 6-O-myristoyl-α-D-glucopyranoside (2) in fair yield. A number of 2,3,4-tri-O-acyl derivatives (3-15) of this 6-O-substitution product using a wide variety of acylating agents were also prepared in order to obtain newer derivatives of synthetic and biological importance. The reaction conditions are reasonably simple and yields were very good. The structures of the title compounds (2-15) were established by using analytical, physicochemical techniques and spectroscopic data (IR and 1H-NMR). All the synthesized compounds were employed as test chemicals for in vitro antimicrobial functionality test against Gram-positive Bacillus subtilis, Staphylococcus aureus, Gram-negative Escherichia coli, Pseudomonas aeruginosa bacteria and plant pathogenic fungi Aspergillus niger and Candida albicans. For comparative studies, antimicrobial activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the human bacterial strains. Encouragingly, a number of tested chemicals showed nearest antibacterial and antifungal activities with the standard antibiotics employed.

scholarly journals Antibacterial and Antifungal Evaluation of Chloroflavones

2018 ◽  
Vol 10 (1) ◽  
pp. 67-76
Author(s):  
M. A. Rahim ◽  
M. M. H. Bhuiyan ◽  
M. M. Matin ◽  
M. R. Alam
Keyword(s):  
Pathogenic Bacteria ◽  
Salmonella Typhi ◽  
Aspergillus Ochraceus ◽  
Diffusion Method ◽  
Dilution Method ◽  
Significant Activity ◽  
Filter Paper Disc ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Two chloroflavones, 6 and 7 along with their corresponding chalcones, 4 and 5 have been tested for antibacterial and antifungal activities against six human pathogenic bacteria viz. Bacillus cereus (G+), Staphylococcus aureus (G+), Escherichia coli (G-), Vibrio choloriae (G-), Pseudomonas aeruginosa (G-), and Salmonella typhi (G-), and four plant as well as mold fungi viz. Aspergillus flavus, Aspergillus ochraceus, Aspergillus niger and Rhizopus spp.. The antibacterial and antifungal screens of the synthesized compounds were performed in vitro by the filter paper disc diffusion method and the poisoned food technique, respectively. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of these synthesized compounds in comparison to ampicillin were also determined by broth micro-dilution method. Some of them were found to possess significant activity, when compared to standard drugs.

scholarly journals Microwave-Assisted Synthesis of Some 1,3,4-Oxadiazole Derivatives and Evaluation of Their Antibacterial and Antifungal Activity

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Deepak Swarnkar ◽  
Rakshit Ameta ◽  
Ritu Vyas
Keyword(s):  
Acid Hydrazide ◽  
Antibacterial Activities ◽  
Microwave Assisted Synthesis ◽  
Standard Drug ◽  
Antifungal Activities ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Diphenylacetic Acid ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal

A series of substituted 1,3,4-oxadiazole derivatives (3a–f) and (6a–f) have been synthesized from diphenylacetic acid hydrazide under microwave irradiation in various reaction conditions. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, and 1H NMR. These targeted compounds have been tested for their antibacterial and antifungal activities compared to ampicillin and griseofulvin as standard drug. Compounds 3a, 3e, 3f, 6c, 6d, 6e, and 6d exhibited the maximum antibacterial activities while 3b, 3c, 3d, 3e, 6a, 6d, and 6e exhibited the maximum antifungal activities.

scholarly journals Synthesis and Biological Activity of Some 3,4-Dihydro-4-(4-substituted aryl)-6-(naptho[2,1-b]furan-2-yl pyrimidine-2(1H)-one Derivatives

2012 ◽  
Vol 9 (1) ◽  
pp. 175-180 ◽  
Author(s):  
Sanjeevan S. Gaikwad ◽  
Venkat S. Suryawanshi ◽  
Kishan S. Lohar ◽  
Dhanaji V. Jadhav ◽  
Narayan D. Shinde
Keyword(s):  
Biological Activity ◽  
Potassium Hydroxide ◽  
Alcoholic Solution ◽  
Significant Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Reflux Temperature

A series of new oxopyrimidine were prepared by cyclocondensation route with various substituted chalcones in presence of alcoholic solution of potassium hydroxide at reflux temperature. The synthesized oxopyrimidine derivatives were characterized by means of their IR,1H NMR, mass spectral data and elemental analysis. The synthesized oxopyrimidines derivatives were evaluated for antibacterial and antifungal activities, some of them were found to possess significant activity.

scholarly journals Synthesis and Antimicrobial Studies of Pyrimidine Pyrazole Heterocycles

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Rakesh Kumar ◽  
Jyoti Arora ◽  
Sonam Ruhil ◽  
Neetu Phougat ◽  
Anil K. Chhillar ◽  
...  
Keyword(s):  
Genetic Material ◽  
Oxidative Cyclization ◽  
Antifungal Drugs ◽  
Mass Spectral ◽  
H Nmr ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Derivatives Of

Prompted from the diversity of the wider use and being an integral part of genetic material, an effort was made to synthesize pyrimidine pyrazole derivatives of pharmaceutical interest by oxidative cyclization of chalcones with satisfactory yield and purity. A novel series of 1,3-dimethyl-6-hydroxy-2,4-dioxo-5-(1′-phenyl-3′-aryl-1H-pyrazol-5′-yl)-1,2,3,4-tetrahydropyrimidines (5a–d) and 1,3-diaryl-6-hydroxy-4-oxo-2-thioxo-5-(1′-phenyl-3′-aryl-1H-pyrazol-5′-yl)-1,2,3,4-tetrahydropyrimidines (5e–l) has been synthesized. The structures of these compounds were established on the basis of FT-IR, 1H NMR, 13C NMR, and mass spectral analysis. All the synthesized compounds were screened for their antimicrobial activity against bacteria and fungi. Among all the compounds, 5g was found to be the most active as its MIC was 31.25 µg/mL against S. aureus and B. cereus. The compounds 5h, 5c, and 5e also possess antibacterial activity with MIC values as 62.50, 125.00, and 500.00 µg/mL, respectively. The compounds 5c and 5j were found to have antifungal activity against Aspergillus spp. As antifungal drugs lag behind the antibacterial drugs, therefore we tried in vitro combination of these two compounds with standard antifungal drugs (polyene and azole) against Aspergillus spp. The combination of ketoconazole with 5c and 5j showed synergy at 1 : 8 (6.25 : 50.00 µg/mL) and 1 : 4 (25 : 100 µg/mL) against A. fumigatus (ITCC 4517) and A. fumigatus (VPCI 190/96), respectively.

scholarly journals Synthesis and antimicrobial evaluation of some 1-(4-arylthiazol-2-yl)-1′-(aryl/heteroaryl)-3,3′-dimethyl-[4,5′-bi-1H-pyrazol]-5-ols

2017 ◽  
Vol 82 (2) ◽  
pp. 127-139 ◽  
Author(s):  
Satbir Mor ◽  
Rajni Mohil ◽  
Savita Nagoria ◽  
Ashwani Kumar
Keyword(s):  
Antibacterial Activities ◽  
Bacterial Strains ◽  
Antifungal Activities ◽  
Docking Simulations ◽  
Antibacterial And Antifungal Activities ◽  
Dehydroacetic Acid ◽  
Antimicrobial Evaluation ◽  
High Yields ◽  
Antibacterial And Antifungal

A series of sixteen 1-(4-arylthiazol-2-yl)-1?-(aryl/heteroaryl)-3,3?-dimethyl-[ 4,5?-bi-1H-pyrazol]-5-ols (7a?p) was synthesized starting from dehydroacetic acid (DHA, 1) via the stepwise formation of thiosemicarbazone (2), 3-(1-(2-(4-arylthiazol-2-yl)hydrazono)ethyl)-4-hydroxy-6-methyl-2H-pyran- -2-ones (4a?d) and 1-(1-(4-arylthiazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol- -4-yl)butane-1,3-diones (5a?d) in high yields. The in vitro antibacterial and antifungal activities of the synthesized bipyrazoles 7a?p were investigated against two Gram-positive bacterial strains, viz. Bacillus subtilis (MTCC 441) and Staphylococcus aureus (MTCC 7443), one Gram-negative bacterial strain, viz. Escherichia coli (MTCC 42), and two fungal strains, viz. Candida albicans (MTCC 183) and Aspergillus niger (MTCC 282). The compounds 7a and 7e were found to exhibit better inhibitory activity against A. niger than the reference fluconazole. Moreover, the antifungal activities of the title compounds were more prolific than their antibacterial activities. Furthermore, in order to study binding interactions, docking simulations of compounds 7a, 7m and 7o were performed into the active site of S. aureus 1,4-dihydroxy-2-naphthoyl- -CoA synthase. Keywords: bipyrazoles; antibacterial; antifungal; docking simulations.

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