scholarly journals Synthesis and Antifungal Activities of 5-(o-Hydroxy phenyl)-2-[4'aryl-3'chloro-2'azetidinon-1-yl]-1,3,4-thiadiazole

2011 ◽  
Vol 8 (2) ◽  
pp. 594-597 ◽  
Author(s):  
Shiv K. Gupta ◽  
P. K. Sharma ◽  
M. Bansal ◽  
B. Kumar
Keyword(s):  
Antifungal Activity ◽  
Spectral Data ◽  
Antifungal Activities ◽  
H Nmr ◽  
New Compounds

New series of 5-(o-hydroxy phenyl)-2-[4'aryl-3'chloro-2'azetidinon-1-yl]-1,3,4-thiadiazole have been synthesized and the structures of the new compounds were established on the basis of IR,1H NMR spectral data.In vitroantifungal activity (MIC activity) was evaluated and compared with standard drugs of ketoconazole. Compounds3cin the series has shown interesting antifungal activity against bothC. albicansandA. nigerfungus. In the gratifying result, most of the compounds were found to have moderate antifungal activity.

scholarly journals Synthesis, Characterization and Primary Antimicrobial, Antifungal Activity Evaluation of Schiff bases of 4-Chloro-(3-substituted-phenylimino) - methyl-[2H] - chromene-2-one

2010 ◽  
Vol 7 (2) ◽  
pp. 377-382 ◽  
Author(s):  
Amit Kasabe ◽  
Vijay Mohite ◽  
Jayesh Ghodake ◽  
Jaydeep Vidhate
Keyword(s):  
Antifungal Activity ◽  
Spectral Data ◽  
Schiff Bases ◽  
Chemical Structure ◽  
Structural Modification ◽  
Antifungal Activities ◽  
H Nmr ◽  
Antimicrobial And Antifungal Activity ◽  
Derivatives Of ◽  
Antimicrobial And Antifungal Activities

Coumarins show promising antimicrobial and antifungal activity, this prompted to us to synthesize new derivatives of coumarins. 4-Chloro-2-oxo-2H-chromene-3-carbaldehyde was reacted with substituted aniline and rectified spirit to obtain a new series of Schiff bases of 4-chloro-(3-substituted-phenylimino) -methyl- [2H]-chromene-2-one (3a-i). Their structures were confirmed by IR,1H NMR spectral data. The synthesized compounds were investigated for antimicrobial and antifungal activities. The data reported showed that the effect of variation in chemical structure was rather unpredictable. Seldom did a particular structural modification lead to uniform alteration in activity in all tests. The substitution which appeared to be most important for high order of activity in the number of test was the 3-chloro phenylimino group. The observed antimicrobial and antifungal activities are attributed to the substitution atrdposition of phenylimino moiety.

Design, Synthesis and Evaluate In Vitro Antifungal Activity of Novel Benzamide Derivatives

2019 ◽  
Vol 41 (3) ◽  
pp. 549-549
Author(s):  
Xuesong Wang and Xiaorong Tang Xuesong Wang and Xiaorong Tang
Keyword(s):  
Antifungal Activity ◽  
Pathogenic Fungi ◽  
Gibberella Zeae ◽  
Design Synthesis ◽  
Carboxylic Acid Amides ◽  
Almost All ◽  
Negative Controls ◽  
New Compounds ◽  
Benzamide Derivatives

A series of novel benzamide derivatives according to fluopicolide were designed and synthesized following the rule of combination carboxylic acid amides and amines derivatives together. The antifungal activity of the 15 new compounds were evaluated in vitro against five pathogenic fungi, including Sclerotinia sclerotiorum, Gibberella zeae, Rhizoctonia solani, Helminthosporium maydis and Botrytis cinerea. Almost all the structure have not been reported, except compounds 3, 5 and 6. A surprising finding is that all the five tested fungi breed faster than negative controls when supplementary with compound 715 , respectively.

scholarly journals Design, Synthesis and Fungicidal Activity of New 1,2,4-Triazole Derivatives Containing Oxime Ether and Phenoxyl Pyridinyl Moiety

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5852
Author(s):  
Hui Bai ◽  
Xuelian Liu ◽  
Pengfei Chenzhang ◽  
Yumei Xiao ◽  
Bin Fu ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Binding Modes ◽  
Oxime Ether ◽  
Single Crystal Diffraction ◽  
Design Synthesis ◽  
Antifungal Activities ◽  
Triazole Derivatives ◽  
Pyridine Moiety ◽  
New Compounds

A series of novel 1,2,4-triazole derivatives containing oxime ether and phenoxy pyridine moiety were designed and synthesized. The new compounds were identified by nuclear magnetic resonance (NMR) spectroscopy and high-resolution mass spectrometry (HRMS). Compound (Z)-1-(6-(4-nitrophenoxy)pyridin-3-yl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-one O-methyl oxime (5a18) was further confirmed by X-ray single crystal diffraction. Their antifungal activities were evaluated against eight phytopathogens. The in vitro bioassays indicated that most of the title compounds displayed moderate to high fungicidal activities. Compound (Z)-1-(6-(4-bromo-2-chlorophenoxy)pyridin-3-yl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-one O-methyl oxime (5a4) exhibited a broad-spectrum antifungal activities with the EC50 values of 1.59, 0.46, 0.27 and 11.39 mg/L against S. sclerotiorum, P. infestans, R. solani and B. cinerea, respectively. Compound (Z)-1-(6-(2-chlorophenoxy)pyridin-3-yl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-one O-benzyl oxime (5b2) provided the lowest EC50 value of 0.12 mg/L against S. sclerotiorum, which were comparable to the commercialized difenoconazole. Moreover, homologous modeling and molecular docking disclosed possible binding modes of compounds 5a4 and 5b2 with CYP51. This work provided useful guidance for the discovery of new 1,2,4-triazole fungicides.

Synthesis and Antifungal Activities of Some 2,6-Bis-(Un)Substituted Phenoxymethylpyridines

2010 ◽  
Vol 65 (7-8) ◽  
pp. 433-436
Author(s):  
Hui Xu ◽  
Huan Qu
Keyword(s):  
Antifungal Activity ◽  
Fusarium Oxysporum ◽  
Fusarium Graminearum ◽  
Broad Spectrum ◽  
Alternaria Alternata ◽  
Phytopathogenic Fungi ◽  
Alternaria Brassicae ◽  
Antifungal Activities

Several 2,6-bis-(un)substituted phenoxymethylpyridines were synthesized and evaluated in vitro against Fusarium graminearum, Helminthosporium sorokinianum, Alternaria brassicae, Alternaria alternata, and Fusarium oxysporum f. sp. vasinfectum. Among all derivatives, compound 3 a exhibited a broad-spectrum antifungal activity against the five phytopathogenic fungi.

Synthesis and Antimicrobial Evaluation of Some New 2-(6-Oxo-5,6- dihydro[1,3]thiazolo[3,2-b]-2-aryloxymethyl-1,2,4-triazol-5-yl)-Narylacetamides

2010 ◽  
Vol 65 (5) ◽  
pp. 617-624 ◽  
Author(s):  
Prajwal L. Lobo ◽  
Boja Poojary ◽  
Kumsi Manjunatha ◽  
Nalilu Suchetha Kumari
Keyword(s):  
Acetic Acid ◽  
Antifungal Activity ◽  
Spectral Data ◽  
Good Yield ◽  
Antibacterial And Antifungal Activity ◽  
Acid Media ◽  
Antimicrobial Evaluation ◽  
Antibacterial And Antifungal

A series of 2-(6-oxo-5,6-dihydro[1,3]thiazolo[3,2-b]-2-aryloxymethyl-1,2,4-triazol-5-yl)-Narylacetamides 6 were synthesized in good yield by condensing 5-aryloxymethyl-4H-1,2,4-triazole- 3-thiol 5 with various substituted N-phenyl-maleimides in acetic acid media. The newly synthesized compounds were characterized by spectral data and tested for their in vitro antibacterial and antifungal activity against a variety of microorganisms.

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.

2-Hydroxypropyl derivatives of 1,2,3-thiadiazole and 1,2,3-triazole: Synthesis and antifungal activity

2011 ◽  
Vol 83 (3) ◽  
pp. 715-722 ◽  
Author(s):  
Yury Morzherin ◽  
Polina E. Prokhorova ◽  
Dmitry A. Musikhin ◽  
Tatiana V. Glukhareva ◽  
Zhijin Fan
Keyword(s):  
Mass Spectrometry ◽  
Antifungal Activity ◽  
Ir Spectroscopy ◽  
Elemental Analysis ◽  
Antifungal Activities ◽  
Triazole Derivatives ◽  
New Compounds ◽  
Derivatives Of

A series of novel 5-(2-hydroxypropyl)amino-1,2,3-thiadiazole and 5-(2-hydroxy-propyl)sulfanyl-1,2,3-triazole derivatives were designed and synthesized as candidate fungicides. The new compounds were identified by NMR and IR spectroscopy, mass spectrometry, and elemental analysis. Their antifungal activities were evaluated.

scholarly journals Chemical characterization and determination of in vivo and in vitro antifungal activity of essential oils from four Eucalyptus species against the Hemileia vastatrix Berk and Br fungus, the agent of coffee leaf rust

2020 ◽  
pp. 1379-1384
Author(s):  
Alex Rodrigues Silva Caetano ◽  
Sara Maria Chalfoun ◽  
Mario Lúcio Vilela Resende ◽  
Caroline Lima Angélico ◽  
Wilder Douglas Santiago ◽  
...  
Keyword(s):  
Gas Chromatography ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Chemical Characterization ◽  
Eucalyptus Species ◽  
Hemileia Vastatrix ◽  
Antifungal Activities

Essential oils, also known as volatile oils, are substances produced through the secondary metabolism of plants. In this study, we determined the chemical composition and the in vitro and in vivo antifungal activity of the essential oils from four species of Eucalyptus, Eucalyptus citriodora, Eucalyptus camaldulensis, Eucalyptus grandis and Eucalyptus microcorys, against the Hemileia vastatrix fungus. The essential oils from these four species of Eucalyptus were extracted from their leaves by the hydrodistillation technique using a modified Clevenger apparatus. The chemical characterization was performed by gas chromatography coupled with a mass spectrometer detector and by gas chromatography using a flame ionization detector. The antifungal activities of the essential oils against H. vastatrix were studied by evaluating the percentage of spore germination using the microdilution test for in vitro assays. The curative and preventive effects were evaluated in in vivo tests. The principal constituents of the essential oil from E. citriodora were citronellal, citronellol and isopulegol, while E. camaldulensis produced 1,8-cineole, α-terpineol and α-pinene. 1,8-cineole, α-pinene and α-terpineol were obtained from E. grandis and 1,8-cineole, α-pinene and trans-pinocarveol were the principal components in the essential oil of E. microcorys. In vitro and in vivo antifungal activities against the fungus under study were observed for most of the essential oils, except the essential oil from E. microcorys, for which no preventive antifungal activity was observed. Only the curing of infection by the H. vastatrix fungus was observed with this oil.

scholarly journals Antioxidant and antifungal activities in vitro of essential oils and extracts of twelve Algerian species of Thymus against some mycotoxigenic Aspergillus genera

2022 ◽  
Author(s):  
Yamina Ben Miri ◽  
Aldjia Taoudiat ◽  
Mohamed Mahdid
Keyword(s):  
Antifungal Activity ◽  
Essential Oils ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antifungal Activities ◽  
Minimum Fungicidal Concentration ◽  
Ethanolic Extracts ◽  
Ethanol Extracts ◽  
Phenolic And Flavonoid

The aim of the study was to determine the phenolic and flavonoid content of essential oils (EOs), chloroform and ethanolic extracts of 12 Algerian Thymus species and evaluate their antioxidant and antifungal activities. EOs (1.73 ± 0.30–15.00 ± 1.24 μg/mg), chloroform extracts (33.8 ± 2.42–160.93 ± 3.88 μg/mg) and ethanol extracts (27.01 ± 3.56 –148.46 ± 4.40 μg/mg) showed considerable phenolic content. Flavonoids values of chloroform extracts ranged between 3.39± 0.17 and 20.27 ± 0.29 μg/ml while ethanolic extracts values ranged between 2.81 ± 0.11 and 26.64 ± 0.18 μg/mg. Results of DPPH showed that EOs, chloroform and ethanolic extracts exhibited strong radical scavenging activity (IC50 = 21.75 ± 6.54–338.22 ± 2.99 μg/ml, 22.91 ± 5.59–90.93 ± 1.36 μg/ml, and 33.51 ± 5.72–103.80 ± 4.54 μg/ml, respectively). Inhibition of β-carotene bleaching was potentially performed by all EOs (66.48 ± 2.41–94.06 ± 2.68 %), chloroform extracts (68.98± 1.58–95.30± 1.99%), and ethanolic extracts (62.15 ± 2.51–92.36± 1.15%). The antifungal activity of EOs and extracts was tested using the minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC). The EOs (0.1 ± 0.00 mg/ mL – 1.06 ± 0.46 mg/mL), chloroform (0.1 ± 0.00 mg/ mL –1.06 ± 0.46 mg/mL) and ethanol (0.1 ± 0.00 mg /mL–1.6 ± 0.00 mg/mL) showed remarkable antifungal activity against mycotoxigenic Aspergillus genera. The MFC of EOs (1.0 ± 0.34 mg/mL and > 4.8 mg/mL) , chloroform (0.26 ± 0.11 mg/mL and > 1.6 mg/mL) and ethanol (0.2 ± 0.00 mg/mL and > 1.6 mg/mL) were fungicidal in nature higher than MICs. The findings of the study indicated that Thymus spp. EOs and extracts could be used as natural alternatives for food industry.

IN VITRO CHARACTERIZATION OF ANTIFUNGAL ACTIVITY OF SELECTED ESSENTIAL OILS

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (12) ◽  
pp. 61-64
Author(s):  
C. Rath Chandi ◽  
A. Samal
Keyword(s):  
Antifungal Activity ◽  
Essential Oils ◽  
Inhibitory Concentration ◽  
Inhibition Mechanism ◽  
Active Components ◽  
Irreversible Damage ◽  
Antifungal Activities ◽  
In Vitro Characterization

Antifungal activity of seven essential oils was studied primarily against C. albicans and E. floccosum. Four essential oils viz. turmeric, palmarosa, lemongrass and citronella, that revealed better antifungal activities during screening, were characterized further. Minimum Inhibitory concentration (MIC) and phenol coefficient values of the oils ranged between 0.97 to 62.5 µl/ml and 0125 to 0.75 respectively. The oils retained the antifungal activities when treated at high temperature (1000 C for 1h) and pressure (autoclaved), indicating presence of thermostable and barostable active components in them. The oils also resisted sonication (33,000Hz for 30min) and revealed antifungal activities against the two pathogens. Immediate killing of E. floccosum, is attributable to an irreversible damage to the cells. Antifungal activity of these oils as recorded during the study, could be attributable to the membrane inhibition mechanism and was observed to be fungicidal in nature.

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