scholarly journals Attempts to Access a Series of Pyrazoles Lead to New Hydrazones with Antifungal Potential Against Candida Species Including Azole-Resistant Strains

2021 ◽  
Author(s):  
Georgiana NEGRU ◽  
Laure KAMUS ◽  
Elena Bîcu ◽  
Sergiu Shova ◽  
Boualem SENDID ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
Pyrazole Derivatives ◽  
Mammalian Cell Line ◽  
Cell Toxicity ◽  
Candida Spp ◽  
X Ray ◽  
Antifungal Potential ◽  
Resistant Strains

The treatment of benzylidenemalononitriles 3a-c with phenylhydrazines 4a-n in refluxing ethanol did not provide pyrazole derivatives but furnished hydrazones 1a-o. The structure of hydrazones was secured by X-Ray analysis. Newly synthesized hydrazones 1a-o were tested against 8 Candida spp. strains in a dose response assay to determine the minimum inhibitory concentration (MIC99). Five compounds 1c, 1d, 1i, 1k and 1l were identified as promising antifungal agents against Candida spp. (C. albicans SC5314, C. glabrata, C. tropicalis, C. parapsilosis and C. glabrata (R azoles)) with MIC99 values ranging from 16 to 32 µg/mL. To further evaluate the antifungal potential of the active compounds, they have been assayed against a mammalian cell line HEK293 to determine general cell toxicity and on NCI-60 cancer cell lines panel, demonstrating selectivity antifungal activity over cytotoxicity.

scholarly journals Attempts to Access a Series of Pyrazoles Lead to New Hydrazones with Antifungal Potential against Candida Species Including Azole-Resistant Strains

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5861
Author(s):  
Georgiana Negru ◽  
Laure Kamus ◽  
Elena Bîcu ◽  
Sergiu Shova ◽  
Boualem Sendid ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
Direct Reaction ◽  
Pyrazole Derivatives ◽  
Candida Spp ◽  
X Ray ◽  
Antifungal Potential ◽  
Resistant Strains

The treatment of benzylidenemalononitriles with phenylhydrazines in refluxing ethanol did not provide pyrazole derivatives, but instead furnished hydrazones. The structure of hydrazones was secured by X-ray analysis. The chemical proof was also obtained by direct reaction of 3,4,5-trimethoxybenzaldehyde with 2,4-dichlorophenylhydrazine. Newly synthesized hydrazones were tested against eight Candida spp. strains in a dose response assay to determine the minimum inhibitory concentration (MIC99). Five compounds were identified as promising antifungal agents against Candida spp. (C. albicans SC5314, C. glabrata, C. tropicalis, C. parapsilosis and C. glabrata (R azoles)), with MIC99 values ranging from 16 to 32 µg/mL and selective antifungal activity over cytotoxicity.

scholarly journals Inhibitory Effect of (-)-myrtenol alone and in combination with antifungal agents on Candida spp.

2021 ◽  
Vol 10 (15) ◽  
pp. e35101522434
Author(s):  
Bruno Bezerra Cavalcanti ◽  
Hermes Diniz Neto ◽  
Walicyranison Plinio da Silva-Rocha ◽  
Edeltrudes de Oliveira Lima ◽  
José Maria Barbosa Filho ◽  
...  
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Antifungal Agent ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Antifungal Drugs ◽  
Additive Effects ◽  
Candida Spp ◽  
Minimum Fungicidal Concentration ◽  
Fungicide Activity

The aim of this study was to examine the effects of (-)-myrtenol alone and combined with antifungal agents against Candida spp. The Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration of (-)-myrtenol and fluconazole against C. albicans and C. parapsilosis strains was obtained using CLSI guidelines. Combination of (-)-myrtenol with antifungal drugs was determined by checkboard test. The (-) myrtenol showed MIC ranging from 256 to 512 µg/mL against both species assay. And the MFC was 512 µg/mL, demonstrated nature fungicidal (MFC/MIC < 4). In addition, combination of antifungal agents (amphotericin B and fluconazole) and (-) myrtenol showed synergistic and additive effects on strains assays. Based on these results, the present study demonstrates that (-) myrtenol showed strong fungicide activity against Candida spp. In addition, Combination of antifungal agents and (-) myrtenol reduces the effective concentrations of both the agents with synergistic to additive effects. Therefore, (-) myrtenol has potential to be developed into an antifungal agent.

Preparation and disinfection properties of graphene oxide/trichloroisocyanuric acid disinfectant

2021 ◽  
Author(s):  
li li jiang ◽  
Su Xu ◽  
Haitao Yu ◽  
Qi Cui ◽  
Rui Cao
Keyword(s):  
Electron Microscopy ◽  
Graphene Oxide ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Kinetic Curve ◽  
X Ray ◽  
Bacterial Inhibition ◽  
E Coli ◽  
Blending Method ◽  
Trichloroisocyanuric Acid

Abstract In this study, graphene oxide (GO) was first prepared by the modified Hummer method. Then, the GO/trichloroisocyanuric acid (TCCA) composite was prepared by loading TCCA into GO with the blending method. X-ray diffraction, scanning electron microscopy, transmission electron microscopy, X-ray photoelectron spectroscopy and atomic force microscopy were used to characterize the composite. The results showed that TCCA was successfully loaded on the surface of GO or intercalated among GO layers. Next, the antibacterial performance of the composite against Escherichia coli and Staphylococcus aureus was tested by the 96-well plate assay. A bactericidal kinetic curve, bacterial inhibition tests, and the mechanism of bacterial inhibition is discussed. The results showed that the minimum inhibitory concentration of the GO/TCCA composite (GO:TCCA ratio = 1:50) was 327.5 µg/mL against E. coli and 655 µg/mL against S. aureus. At the minimum inhibitory concentration, the inhibition rate of the GO/TCCA composite exceeded 99.46% against E. coli and 99.17% against S. aureus. The bactericidal kinetic curves indicate that the GO/TCCA composite has an excellent bactericidal effect against E. coli and S. aureus.

scholarly journals Synthesis and Antimicrobial Studies of Coumarin-Substituted Pyrazole Derivatives as Potent Anti-Staphylococcus aureus Agents

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2758 ◽  
Author(s):  
Rawan Alnufaie ◽  
Hansa Raj KC ◽  
Nickolas Alsup ◽  
Jedidiah Whitt ◽  
Steven Andrew Chambers ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Minimum Inhibitory Concentration ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Concentration ◽  
Fatality Rate ◽  
Pyrazole Derivatives ◽  
Methicillin Resistant ◽  
Antimicrobial Studies ◽  
Mrsa Strains

In this paper, synthesis and antimicrobial studies of 31 novel coumarin-substituted pyrazole derivatives are reported. Some of these compounds have shown potent activity against methicillin-resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration (MIC) as low as 3.125 µg/mL. These molecules are equally potent at inhibiting the development of MRSA biofilm and the destruction of preformed biofilm. These results are very significant as MRSA strains have emerged as one of the most menacing pathogens of humans and this bacterium is bypassing HIV in terms of fatality rate.

scholarly journals Antistaphylococcal Activity of CB-181963 (CAB-175), an Experimental Parenteral Cephalosporin

2004 ◽  
Vol 48 (10) ◽  
pp. 4037-4039 ◽  
Author(s):  
Dianne B. Hoellman ◽  
Glenn A. Pankuch ◽  
Peter C. Appelbaum
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Methicillin Resistant ◽  
Antistaphylococcal Activity ◽  
Resistant Strains ◽  
Vancomycin Resistant

ABSTRACT Among 265 methicillin-susceptible and -resistant staphylococci, CB-181963 (CAB-175) had a 50% minimum inhibitory concentration of 2 μg/ml and a 90% minimum inhibitory concentration of 4 μg/ml. All strains except two vancomycin-resistant S. aureus and 5 vancomycin-intermediate S. aureus strains were also susceptible to vancomycin and teicoplanin, and all were susceptible to linezolid, ranbezolid, tigecycline, and quinupristin-dalfopristin. Most methicillin-resistant strains were levofloxacin resistant. CB-181963 was bactericidal against all six methicillin-resistant strains at four times the MIC after 24 h.

Bismuth(III) Thiobenzoates and their Activity against Helicobacter pylori

2012 ◽  
Vol 65 (7) ◽  
pp. 883 ◽  
Author(s):  
Philip C. Andrews ◽  
Richard L. Ferrero ◽  
Peter C. Junk ◽  
Jonathan G. Maclellan ◽  
Roshani M. Peiris
Keyword(s):  
Helicobacter Pylori ◽  
Solid State ◽  
Minimum Inhibitory Concentration ◽  
Bactericidal Activity ◽  
Inhibitory Concentration ◽  
X Ray ◽  
X Ray Crystallography ◽  
Thiobenzoic Acid ◽  
High Level ◽  
Solid State Structures

Two new substituted thiobenzoic acids, m-nitrothiobenzoic and m-sulfothiobenzoic acid, and six (four new) homo- and heteroleptic bismuth(iii) compounds derived from thiobenzoic acid and substituted thiobenzoic acid have been synthesised and fully characterised using both solvent free and solvent mediated methods; Bi(SC(=O)C6H5)3 (3), PhBi(SC(=O)C6H5)2 (4), Ph2Bi(SC(=O)C6H5) (5), Bi(SC(=O)C6H4-m-NO2)3 (6), PhBi(SC(=O)C6H4-m-NO2)2 (7), and PhBi(SC(=O)C6H4-m-SO3) (8). The solid-state structures of the previously reported Bi(SC(=O)C6H5)3 (3) and PhBi(SC(=O)]C6H5)2 (4) complexes have now been confirmed by X-ray crystallography. In the solid-state complex 3 forms a column-like polymeric structure resembling stacked bowls through pyramidal intermolecular Bi–S3 bonds of distance 3.359 Å, providing a Bi(iii) centre with a nine coordinate environment. Complex 4 forms discrete tetrameric units cemented by long intermolecular Bi–S (3.774 Å), Bi–O(= C) (3.030, 3.071 Å) and Bi–C bonds (3.627 Å). The complexes were assessed for their activity against three strains of Helicobacter pylori and all show a minimum inhibitory concentration of 6.25 µg mL–1, indicating that the high level of bactericidal activity is insensitive to the degree of substitution at the Bi(iii) centre.

Synthesis and Antifungal Activity of New Dihydropyrazoles of Designed Curcumin Analogues

2019 ◽  
Vol 4 (2) ◽  
pp. 94-100
Author(s):  
Vishwa Deepak Tripathi ◽  
Nisha Saxena
Keyword(s):  
Biological Activity ◽  
Minimum Inhibitory Concentration ◽  
Phenyl Ring ◽  
Mass Spectra ◽  
Inhibitory Concentration ◽  
Pyrazole Ring ◽  
Optically Active ◽  
1H And 13C Nmr ◽  
Curcumin Analogues ◽  
Antifungal Potential

A library of new dihydropyrazole derivatives have been synthesized from well designed curcumin analogues by reaction of chalcone derivatives with phenylhydrazine. All the synthesized compounds were characterized by spectroscopic (1H and 13C NMR, IR spectra), spectrometric (Mass spectra) data and elemental analysis. Dihydro-pyrazoles exhibited characteristic dd (double doublet) due to presence of optically active carbon of pyrazole ring. All the synthesized compounds were also evaluated for their antifungal potential against six different fungal starins. Evaluated heterocyles showed potent inhibitory property against tested fungal strains with minimum inhibitory concentration (MIC) values upto 3.12 μg/mL. Heterocyles with nitro and methoxy substitutions were showing best antifungal activities. Among 20 different derivatives tested for biological activity SAR has been developed between the various substitutions at phenyl ring of synthesized heterocycles.

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