Development of Antibacterial and Antifungal Triazole Chromium(III) and Cobalt(II) Complexes: Synthesis and Biological Activity Evaluations

In this work, six complexes (2–7) of Cr(III) and Co(II) transition metals with triazole ligands were synthesized and characterized. In addition, a new ligand, 3,5-bis(1,2,4-triazol-1-ylmethyl)toluene (1), was synthesized and full characterized. The complexes were obtained as air-stable solids and characterized by melting point, electrical conductivity, thermogravimetric analysis, and Raman, infrared and ultraviolet/visible spectroscopy. The analyses and spectral data showed that complexes 3–7 had 1:1 (M:L) stoichiometries and octahedral geometries, while 2 had a 1:2 (M:L) ratio, which was supported by DFT calculations. The complexes and their respective ligands were evaluated against bacterial and fungal strains with clinical relevance. All the complexes showed higher antibacterial and antifungal activities than the free ligands. The complexes were more active against fungi than against bacteria. The activities of the chromium complexes against Candida tropicalis are of great interest, as they showed minimum inhibitory concentration 50 (MIC50) values between 7.8 and 15.6 μg mL−1. Complexes 5 and 6 showed little effect on Vero cells, indicating that they are not cytotoxic. These results can provide an important platform for the design of new compounds with antibacterial and antifungal activities.

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Ferrocene Derivatives Carrying Urea, Thiourea, and Sulfonamide Moieties: Synthesis and Evaluation of Antibacterial and Antifungal Activities

Journal of Chemistry ◽

10.1155/2013/149693 ◽

2013 ◽

Vol 2013 ◽

pp. 1-7 ◽

Cited By ~ 8

Author(s):

Serkan Yavuz ◽

Hilal Yıldırım

Keyword(s):

Inhibitory Concentration ◽

Antibacterial Activities ◽

Klebsiella Pneumonia ◽

Gram Negative Bacteria ◽

Ferrocene Derivatives ◽

Antifungal Activities ◽

Gram Positive Bacteria ◽

Antibacterial And Antifungal Activities ◽

Elemental Analyses ◽

Antibacterial And Antifungal

In the present study, some novel ferrocene derivatives carrying urea, thiourea, and sulfonamide groups were synthesized, and all compounds were characterized by spectral and elemental analyses. These compounds were screened for their antibacterial activities and also their minimum inhibitory concentration (MIC) against Gram-positive bacteria (Staphylococcus aureusandBacillus subtilis) and Gram-negative bacteria (Klebsiella pneumoniaandEscherichia coli) and antifungal activities againstSaccharomyces cerevisiaeandCandida albicans. Amongst the tested compounds,4b,4c,5b, and6bdisplayed excellent antimicrobial activity.

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Design, Synthesis, and Antimicrobial Evaluation of Novel Pyrazoles and Pyrazolyl 1,3,4-Thiadiazine Derivatives

Molecules ◽

10.3390/molecules23092092 ◽

2018 ◽

Vol 23 (9) ◽

pp. 2092 ◽

Cited By ~ 10

Author(s):

Ibrahim Radini

Keyword(s):

Antimicrobial Activity ◽

Minimum Inhibitory Concentration ◽

Elemental Analysis ◽

Inhibitory Concentration ◽

Diazonium Salts ◽

Design Synthesis ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antimicrobial Evaluation ◽

Antibacterial And Antifungal

A novel series of pyrazolyl 1,3,4-thiadiazines 5a–c, 8a–c, 12, 15a–c, 17a–c, and 20 was prepared from the reaction of pyrazole-1-carbothiohydrazide 1a,b with 2-oxo-N′-arylpropanehydrazonoyl chloride, 2-chloro-2-(2-arylhydrazono)acetate, and 3-bromoacetylcoumarin. Moreover, the regioselective reaction of 5-pyrazolone-1-carbothiohydrazide 1a with 4-substituted diazonium salts and 4-(dimethylamino)benzaldehyde gave the corresponding hydrazones 21a–c and 22. The newly prepared compounds were characterized by spectroscopy and elemental analysis. Many new synthesized compounds showed considerable antimicrobial activity against tested microorganisms. Hydrazones 21a–c and 22 showed remarkable antibacterial and antifungal activities. 4-(2-(p-tolyl)hydrazineylidene)-pyrazole-1-carbothiohydrazide 21a displayed the highest antibacterial and antifungal activities with minimum inhibitory concentration (MIC) values lower than standard drugs chloramphenicol and clotrimazole, in the range of 62.5–125 and 2.9–7.8 µg/mL, respectively.

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Comprehensive Evaluation of the Antibacterial and Antifungal Activities of Carlina acaulis L. Essential Oil and Its Nanoemulsion

Antibiotics ◽

10.3390/antibiotics10121451 ◽

2021 ◽

Vol 10 (12) ◽

pp. 1451

Author(s):

Antonio Rosato ◽

Alexia Barbarossa ◽

Ahmed M. Mustafa ◽

Giulia Bonacucina ◽

Diego Romano Perinelli ◽

...

Keyword(s):

Essential Oil ◽

Comprehensive Evaluation ◽

Antimicrobial Properties ◽

Homogenization Method ◽

Bacterial Strains ◽

Antifungal Activities ◽

Fungal Strains ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

New Compounds

Plants are considered to be an excellent source of new compounds with antibiotic activity. Carlina acaulis L. is a medicinal plant whose essential oil (EO) is mainly characterized by the polyacetylene carlina oxide, which has antimicrobial properties. The aim of this study was to evaluate the antimicrobial and antifungal activities of C. acaulis EO, carlina oxide, and nanoemulsion (NE) containing the EO. The EO was obtained through plant roots hydrodistillation, and carlina oxide was purified from it through silica gel column chromatography. The NE containing C. acaulis EO was prepared with the high-pressure homogenization method, and the minimum inhibitory concentration (MIC) was determined against several bacterial and fungal strains for all the C. acaulis-derived products. The latter resulted in activity active versus all the screened Gram-positive bacterial strains and also on all the fungal strains with low MIC values. For yeast, the EO and carlina oxide showed good MIC values. The EO-NE demonstrated a better activity than the pure EO on all the tested bacterial and fungal strains. The results suggest that C. acaulis-derived products could be potential candidates for the development of natural antibacterial and antifungal agents.

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Investigation of Bulb Extracts of Crinum jagus for Antibacterial and Antifungal Activities

Journal of Applied Sciences and Environmental Management ◽

10.4314/jasem.v25i1.16 ◽

2021 ◽

Vol 25 (1) ◽

pp. 113-117

Author(s):

T.T. Alawode ◽

L. Lajide ◽

B.J. Owolabi ◽

M.T. Olaleye

Keyword(s):

Minimum Inhibitory Concentration ◽

Inhibitory Concentration ◽

Methanol Extract ◽

Diffusion Method ◽

Zone Of Inhibition ◽

Antifungal Activities ◽

Agar Diffusion ◽

Antibacterial And Antifungal Activities ◽

Successive Extraction ◽

Antibacterial And Antifungal

This study investigates the bulb extracts of Crinum jagus for antimicrobial activities. The bulb samples were dried, ground and subjected to successive extraction using hexane, ethylacetate and methanol. The extracts were screened for activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, Salmonella typhi, Klebisidlae pneumonae, Candida albicans, Aspergillus niger, Penicillium notatum and Rhizopus stolonifer at concentrations between 6.25 and 200 mg/ml. Antimicrobial assays werecarried out using agar diffusion method. The Minimum Inhibitory Concentration (MIC) of the extracts was determined. The percentage yields obtained for the hexane, ethylacetate and methanol extracts of the bulbs are 0.28 %, 0.44% and 24.68 % respectively. Results showed that the methanolic extract had better antibacterial and antifungal activities than the other extracts. The methanol extract showed the highest antibacterial activity against S. aureus with a zone of inhibition of 28 mm at 200 mg/ml. Also, the methanol extract showed the highest antifungal activities against C. albicans, A. niger and P. notatum with a zone of inhibition of 20 mm at 200 mg/ml. The hexane and ethylacetate extracts had no activity against the microorganisms at 6.25 mg/ml.The methanol extract had the lowest Minimum Inhibitory Concentration (MIC) of 2.50 mg/ml against S. aureus, E. coli, B. subtilis, P. aeruginosa and S. typhi. The methanol extract could be a source of potent antimicrobial compounds. Keywords: Antibacterial, Antifungal, Crinum jagus, Agar diffusion, MIC

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Synthesis and Antimicrobial Activity of Novel Benzoxazoles

Zeitschrift für Naturforschung C ◽

10.1515/znc-2012-9-1004 ◽

2012 ◽

Vol 67 (9-10) ◽

pp. 466-472 ◽

Cited By ~ 7

Author(s):

Mustafa Arisoy ◽

Ozlem Temiz-Arpaci ◽

Fatma Kaynak-Onurdag ◽

Selda Ozgen

Keyword(s):

Antimicrobial Activity ◽

Inhibitory Concentration ◽

Antimicrobial Activities ◽

Microbial Pathogens ◽

Drug Resistant ◽

Dilution Technique ◽

Spectral Techniques ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

New Compounds

A series of 2-(p-substituted-benzyl)-5-[[4-(p-chloro/fluoro-phenyl)piperazin-1-yl]ace tamido] -benzoxazoles were synthesized in need of new compounds for the fight against microbial pathogens. Their structures were elucidated by spectral techniques. These new derivatives, along with previously synthesized 2-(p-substituted-benzyl)-5-substituted-benzoxazoles, were evaluated for their antibacterial and antifungal activities against standard strains and drugresistant isolates in comparison with ampicillin, gentamicin sulfate, ofloxacin, vancomycin, fluconazole, and amphotericin B trihydrate. The minimum inhibitory concentration (MIC) of each compound was determined by a two-fold serial dilution technique. The compounds were found to possess a broad spectrum of antimicrobial activities with MIC values of 32 - 256 μg/ml. Although standard drugs were more active against the pathogenes employed in this study, the activities of the new benzoxazoles and reference drugs against drug-resistant isolates of the microorganisms were largely similar

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Synthesis, Characterization and Biological Activity of 5-Arylidene-3-(6,7-dicloro-1,3-benzothiazol-2-yl)-phenyl-3,5-dihydro-4H-imidazol-4-ones

E-Journal of Chemistry ◽

10.1155/2010/264036 ◽

2010 ◽

Vol 7 (1) ◽

pp. 81-84

Author(s):

B. B. Baldaniya

Keyword(s):

Biological Activity ◽

Mass Spectra ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Elemental Analyses ◽

Bacteria And Fungi ◽

Different Strains ◽

Antibacterial And Antifungal

Some novel 5-arylidene-3-(6,7-dichloro-1,3-benzothiazol-2-yl)-2-phenyl-3,5-dihydro-4H-imidazol-4-ones (6a-q)have been synthesized and characterized by elemental analyses, IR, NMR, and mass spectra. The products have been evaluated for antibacterial and antifungal activities against different strains of bacteria and fungi.

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Synthesis, Absolute Configuration, Antibacterial, and Antifungal Activities of Novel Benzofuryl β-Amino Alcohols

Materials ◽

10.3390/ma13184080 ◽

2020 ◽

Vol 13 (18) ◽

pp. 4080

Author(s):

Agnieszka Tafelska-Kaczmarek ◽

Renata Kołodziejska ◽

Marcin Kwit ◽

Bartosz Stasiak ◽

Magdalena Wypij ◽

...

Keyword(s):

Saccharomyces Cerevisiae ◽

Absolute Configuration ◽

Aureobasidium Pullulans ◽

Inhibitory Concentration ◽

Theoretical Calculations ◽

Amino Alcohols ◽

Transfer Hydrogenation ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal

A series of new benzofuryl α-azole ketones was synthesized and reduced by asymmetric transfer hydrogenation (ATH). Novel benzofuryl β-amino alcohols bearing an imidazolyl and triazolyl substituents were obtained with excellent enantioselectivity (96–99%). The absolute configuration (R) of the products was confirmed by means of electronic circular dichroism (ECD) spectroscopy supported by theoretical calculations. Selected benzofuryl α-azole ketones were also successfully asymmetrically bioreduced by fungi of Saccharomyces cerevisiae and Aureobasidium pullulans species. Racemic and chiral β-amino alcohols, as well as benzofuryl α-amino and α-bromo ketones were evaluated for their antibacterial and antifungal activities. From among the synthesized β-amino alcohols, the highest antimicrobial activity was found for (R)-1-(3,5-dimethylbenzofuran-2-yl)-2-(1H-imidazol-1-yl)ethan-1-ol against S. aureus ATCC 25923 (MIC = 64, MBC = 96 μg mL−1) and (R)-1-(3,5-dimethylbenzofuran-2-yl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-ol against yeasts of M. furfur DSM 6170 (MIC = MBC = 64 μg mL−1). In turn, from among the tested ketones, 1-(benzofuran-2-yl)-2-bromoethanones (1–4) were found to be the most active against M. furfur DSM 6170 (MIC = MBC = 1.5 μg mL−1) (MIC—minimal inhibitory concentration, MBC—minimal biocidal concentration).

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Synthesis and Biological Activity of (Z) –n-(5-Benzylidene-4-oxo-2-substituted- phenylthiazolidin-3-yl)-5-((1, 3-dioxoisoindolin-2-yl)methyl)-2-hydroxybenzamide

E-Journal of Chemistry ◽

10.1155/2010/586984 ◽

2010 ◽

Vol 7 (4) ◽

pp. 1484-1490

Author(s):

M. C. Patel ◽

Dhameliya

Keyword(s):

Biological Activity ◽

Spectral Data ◽

Thioglycolic Acid ◽

Aromatic Aldehydes ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal

5-((1, 3-Dioxoisoindolin-2-yl)methyl-2-hydroxybenzohydrazide (1) undergoes facile condensation with aromatic aldehydes to afford the correspondingN'-substituted-phenyl-5-((1,3-dioxoisoindolin-2-yl) methyl)-2-hydroxybenzohydrazide (2a-h) in good yields. Cyclocondensation of compounds (2a-h) with thioglycolic acid yields 5-((1,3-dioxoisoindolin-2-yl) methyl)-2-hydroxy-N-(4-oxo-2-substituted phenylthiazolidin-3-yl)benzamide (3a-h). These (3a-h) compounds were further reacted with benzaldehyde in the presence of sodium ethanolate affords, (Z) –N-(5-benzylidene-4-oxo-2-substituted phenyl-thiazolidin-3-yl)-5-((1,3-dioxoisoindolin-2-yl)methyl)-2-hydroxybenzamdie(4a-h). The structures of these compounds were established on the basis of analytical and spectral data. All the newly synthesized compounds were evaluated for their antibacterial and antifungal activities.

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Derivatization Does Not Influence Antimicrobial and Antifungal Activities of Applanoxidic Acids and Sterols from Ganoderma spp.

Zeitschrift für Naturforschung C ◽

10.1515/znc-2006-1-206 ◽

2006 ◽

Vol 61 (1-2) ◽

pp. 31-34 ◽

Cited By ~ 10

Author(s):

Artur Smania ◽

Elza F. A. Smania ◽

Franco Delle Monache ◽

Moacir G. Pizzolatti ◽

Giuliano Delle Monache

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Inhibitory Concentration ◽

Trichophyton Mentagrophytes ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Microdilution Method ◽

Antibacterial And Antifungal ◽

Antimicrobial And Antifungal Activities ◽

And Staphylococcus Aureus

Abstract Applanoxidic acids and sterols, isolated from Ganoderma spp., were acetylated and/or methylated. The antibacterial activity against Escherichia coli and Staphylococcus aureus and the antifungal activity against Candida albicans and Trichophyton mentagrophytes of the derivatives were investigated by a microdilution method, and compared with those of the natural products. Both natural and modified compounds exhibited comparable antibacterial and antifungal activities in a range of 1.0 to > 2.0 mg/ml minimal inhibitory concentration

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Antimicrobial Activity of Crude Extract Obtained from the Root of Plumbago zeylanica

Bangladesh Journal of Microbiology ◽

10.3329/bjm.v24i1.1244 ◽

1970 ◽

Vol 24 (1) ◽

pp. 73-75 ◽

Cited By ~ 9

Author(s):

M Shafiqur Rahman ◽

M Nural Anwar

Keyword(s):

Antimicrobial Activity ◽

Minimum Inhibitory Concentration ◽

Inhibitory Concentration ◽

Ethanolic Extract ◽

Phytopathogenic Fungi ◽

Plumbago Zeylanica ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

Mic Value

Ethanolic extract of Plumbago zeylanica root was investigated for its antimicrobial activities against 11 human pathogenic bacteria and 6 phytopathogenic fungi using disc diffusion method and poisoned food technique respectively. The extract exhibited good antibacterial and antifungal activities against the test organisms. Among the test bacteria, Vibrio cholerae was found to be the most sensitive to the extract showing the highest diameter of zone of inhibition and lowest minimum inhibitory concentration (MIC) value (200 Î¼g/ml). The extract was also very effective against Escherichia coli and Pseudomonas aeruginosa showing MIC value of 250 Î¼g/ml. Among the phytopathogenic fungi tested, Curvularia lunata exhibited the highest sensitivity to the extract with an MIC value of 150 Î¼g/ml, which was followed next by Colletotrichum corchori and Fusarium equiseti (MIC value 250 Î¼g/ml). The root extract from P. zeylanica seems promising since it showed both antibacterial and antifungal activities. Keywords: Antimicrobial activity, Plumbago zeylanica, Ethanolic extract, Minimum inhibitory concentration (MIC)DOI: http://dx.doi.org/10.3329/bjm.v24i1.1244 Bangladesh J Microbiol, Volume 24, Number 1, June 2007, pp73-75

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