On the synthesis of 4- and 5-pyrimidinyl-diphenyl-(1-imidazolyl)methanes and their antifungal activity

1980 ◽  
Vol 45 (2) ◽  
pp. 539-547 ◽  
Author(s):  
Zdeněk Buděšínský ◽  
Josef Vavřina ◽  
Leon Langšádl ◽  
Jiří Holubek
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Dimethyl Sulfoxide ◽  
Ethyl Ester ◽  
Ethylmagnesium Bromide ◽  
Dihydro Derivative ◽  
Phenylmagnesium Bromide

On reaction of phenylmagnesium bromide with ethyl ester of 5-chloro-2-methyl-, 5-chloro-2-methylthio-, 5-bromo-2-methylthio-4-pyrimidinecarboxylic acid and 2,4-dimethyl-5-pyrimidinecarboxylic acid (IIa, IIb, IIc, V) corresponding 4-pyrimidinyl- or 5-pyrimidinyl-diphenylmethanols (IIIa, IIIb, IIIc, VI) were obtained. On reaction of thionyl-bis-imidazole with these methanols (4- or 5-pyrimidinyl)-diphenyl-(1-imidazolyl)-methanes IVa, IVb, IVc and VII were prepared. Phenylmagnesium bromide reacted with ethyl 4-methyl-2-methylthio-5-pyrimidinecarboxylate (VIII) under formation of dihydro derivative IX. We were unable to prepare Grignard's reagent from 5-bromo-2-methylthiopyrimidine and magnesium; it reacted with ethylmagnesium bromide under formation of dihydro derivative I. 5-Chloro-2-methylthio-4-pyrimidinecarboxylic acid when heated with NaOH in dimethyl sulfoxide gave 5-hydroxy-2-methylsulfinyl-4-pyrimidinecarboxylic acid. Compounds IVb and IVc prevented the growth of Candida albicans in vitro at almost the same concentrations as clotrimazole.

Aktivitas Antifungi Air Perasan Bawang Merah (Allium ascalonicum L.) Terhadap Candida albicans Secara In Vitro

2017 ◽  
Vol 9 (2) ◽  
pp. 71
Author(s):  
Nurhasanah Nurhasanah ◽  
Fauzia Andrini ◽  
Yulis Hamidy
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Allium Sativum ◽  
Fungicidal Activity ◽  
Positive Control ◽  
Negative Control ◽  
Randomized Design ◽  
Significant Difference ◽  
Completely Randomized Design

Shallot (Allium ascalonicum L.) has been known as traditional medicine. Shallot which has same genus with garlic(Allium sativum L.) contains allicin that is also found in garlic and has been suspected has fungicidal activity toCandida albicans. It is supported by several researches. Therefore, shallot is suspected has antifungal activity too.The aim of this research was to know antifungal activity of shallot’s water extortion againsts Candida albicans invitro. This was a laboratory experimental research which used completely randomized design, with diffusion method.Shallot’s water extortion was devided into three concentrations, there were 50%, 100% and 200%. Ketoconazole 2%was positive control and aquadest was negative control. The result of this research based on analysis of varians(Anova), there was significant difference between several treatments and was confirmed with Duncan New MultipleRange Test (DNMRT) p<0,05, there was significant difference between 100% shallot’s water extortion with othertreatments, but there was no significant difference between 50% shallot’s water extortion with 200% shallot’s. Theconclusion was shallot’s water extortion had antifungal activity againsts Candida albicans with the best concentration100%, but it was lower than ketoconazole 2%.

scholarly journals Orodispersible Film Loaded with Enterococcus faecium CRL183 Presents Anti-Candida albicans Biofilm Activity In Vitro

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 998
Author(s):  
Virgínia Barreto Lordello ◽  
Andréia Bagliotti Meneguin ◽  
Sarah Raquel de Annunzio ◽  
Maria Pía Taranto ◽  
Marlus Chorilli ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Enterococcus Faecium ◽  
Potato Starch ◽  
Oral Candidiasis ◽  
Candida Spp ◽  
Sem Images ◽  
Control Film ◽  
In Vitro Antifungal Activity

Background: Probiotic bacteria have been emerging as a trustworthy choice for the prevention and treatment of Candida spp. infections. This study aimed to develop and characterize an orodispersible film (ODF) for delivering the potentially probiotic Enterococcus faecium CRL 183 into the oral cavity, evaluating its in vitro antifungal activity against Candida albicans. Methods and Results: The ODF was composed by carboxymethylcellulose, gelatin, and potato starch, and its physical, chemical, and mechanical properties were studied. The probiotic resistance and viability during processing and storage were evaluated as well as its in vitro antifungal activity against C. albicans. The ODFs were thin, resistant, and flexible, with neutral pH and microbiologically safe. The probiotic resisted the ODF obtaining process, demonstrating high viability (>9 log10 CFU·g−1), up to 90 days of storage at room temperature. The Probiotic Film promoted 68.9% of reduction in fungal early biofilm and 91.2% in its mature biofilm compared to the group stimulated with the control film. Those results were confirmed through SEM images. Conclusion: The probiotic ODF developed is a promising strategy to prevent oral candidiasis, since it permits the local probiotic delivery, which in turn was able to reduce C. albicans biofilm formation.

Biodegradable polymers-based nanoparticles to enhance the antifungal efficacy of fluconazole against Candida albicans

2021 ◽  
Vol 22 ◽  
Author(s):  
Noha Saleh ◽  
Soha Elshaer ◽  
Germeen Girgis
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Encapsulation Efficiency ◽  
Water Solubility ◽  
In Vitro Release ◽  
Double Emulsion ◽  
Dilution Method ◽  
Ft Ir ◽  
Antifungal Efficacy

Background: Fluconazole (FLZ), a potent antifungal medication, is characterized by poor water solubility that reduced its antifungal efficacy. Objective: This study aimed to prepare FLZ-loaded polymeric nanoparticles (NPs) by using different polymers and techniques as a mean of enhancing the antifungal activity of FLZ. Methods: NP1, NP2, and NP3 were prepared by the double emulsion/solvent evaporation method using PLGA, PCL, and PLA, respectively. The ionotropic pre-gelation technique was applied to prepare an alginate/chitosan-based formulation (NP4). Particle size, zeta potential, encapsulation efficiency, and loading capacity were characterized. FT-IR spectra of FLZ, the polymers, and the prepared NPs were estimated. NP4 was selected for further in-vitro release evaluation. The broth dilution method was used to assess the antifungal activity of NP4 using a resistant clinical isolate of Candida albicans. Results: The double emulsion method produced smaller-sized particles (<390 nm) but with much lower encapsulation efficiency (< 12%). Alternatively, the ionic gelation method resulted in nanosized particles with a markedly higher encapsulation efficiency of about 40%. The FT-IR spectroscopy confirmed the loading of the FLZ molecules in the polymeric network of the prepared NPs. The release profile of NP4 showed a burst initial release followed by a controlled pattern up to 24 hours with a higher percent released relative to the free FLZ suspension. NP4 was able to reduce the value of MIC of FLZ by 20 times. Conclusion: The antifungal activity of FLZ against C. albicans was enhanced markedly via its loading in the alginate/chitosan-based polymeric matrix of NP4.

Spilanthol as a promising antifungal alkylamide for the treatment of vulvovaginal candidiasis

2021 ◽  
Author(s):  
Rodrigo L Fabri ◽  
Jhamine C O Freitas ◽  
Ari S O Lemos ◽  
Lara M Campos ◽  
Irley O M Diniz ◽  
...  
Keyword(s):  
Cell Wall ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Cell Membrane ◽  
Multidrug Resistant ◽  
Fungal Strain ◽  
Vulvovaginal Candidiasis ◽  
Biofilm Matrix

Abstract Spilanthol is a bioactive alkylamide from the native Amazon plant species, Acmella oleracea. However, antifungal activities of spilanthol and its application to the therapeutic treatment of candidiasis remains to be explored. This study sought to evaluate the in vitro and in vivo antifungal activity of spilanthol previously isolated from A. oleracea (spilanthol(AcO)) against Candida albicans ATCC® 10231™, a multidrug-resistant fungal strain. Microdilution methods were used to determine inhibitory and fungicidal concentrations of spilanthol(AcO). In planktonic cultures, the fungal growth kinetics, yeast cell metabolic activity, cell membrane permeability and cell wall integrity were investigated. The effect of spilanthol(AcO) on the proliferation and adhesion of fungal biofilms was evaluated by whole slide imaging and scanning electron microscopy. The biochemical composition of the biofilm matrix was also analyzed. In parallel, spilanthol(AcO) was tested in vivo in an experimental vulvovaginal candidiasis model. Our in vitro analyses in C. albicans planktonic cultures detected a significant inhibitory effect of spilanthol(AcO), which affects both yeast cell membrane and cell wall integrity, interfering with the fungus growth. C. albicans biofilm proliferation and adhesion, as well as, carbohydrates and DNA in biofilm matrix were reduced after spilanthol(AcO) treatment. Moreover, infected rats treated with spilanthol(AcO) showed consistent reduction of both fungal burden and inflammatory processes compared to the untreated animals. Altogether, our findings demonstrated that spilanthol(AcO) is an bioactive compound against planktonic and biofilm forms of a multidrug resistant C. albicans strain. Furthermore, spilanthol(AcO) can be potentially considered for therapeutical treatment of vulvovaginal candidiasis caused by C. albicans. Lay Abstract This study sought to evaluate the antifungal activity of spilanthol against Candida albicans ATCC® 10 231™, a multidrug-resistant fungal strain. Our findings demonstrated that spilanthol(AcO) can be potentially considered for therapeutical treatment of vulvovaginal candidiasis caused by C. albicans.

scholarly journals In Vitro Antifungal Activity of (1)-N-2-Methoxybenzyl-1,10-phenanthrolinium Bromide against Candida albicans and Its Effects on Membrane Integrity

Mycobiology ◽  
2017 ◽  
Vol 45 (1) ◽  
pp. 25-30 ◽  
Author(s):  
Setiawati Setiawati ◽  
Titik Nuryastuti ◽  
Ngatidjan Ngatidjan ◽  
Mustofa Mustofa ◽  
Jumina Jumina ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Membrane Integrity ◽  
In Vitro Antifungal Activity

Antifungal activity of four commercially available intense sweeteners against candida albicans - An In vitro study

2013 ◽  
Vol 3 (2) ◽  
pp. 60
Author(s):  
Subramaniam Ramanarayanan ◽  
Sakeenabi Basha ◽  
Mahesh Hiregoudar ◽  
PrashantGoudar Manjunath ◽  
Simpy Mittal ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
In Vitro Study ◽  
Vitro Study

scholarly journals Antifungal Activity of the Essential Oil of Echinops kebericho Mesfin: An In Vitro Study

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Tamirat Bekele Beressa ◽  
Serawit Deyno ◽  
Paul E. Alele
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Cryptococcus Neoformans ◽  
Antioxidant Properties ◽  
Pathogenic Fungi ◽  
Diffusion Method ◽  
Potential Candidate ◽  
Standard Drug

Background. Echinops kebericho is an endemic medicinal plant in Ethiopia widely used in the treatment of infectious and noninfectious diseases. Essential oils are known for their antibacterial, antifungal, antiviral, insecticidal, and antioxidant properties. This study evaluated the antifungal activity of essential oil from E. kebericho against four common pathogenic fungi and two standard strains. Methods. The essential oil was obtained by hydrodistillation. The antifungal screening was done by agar well diffusion method. Minimal inhibitory concentrations (MICs) were determined by broth microdilution. Minimal fungicidal concentrations (MFCs) were determined by subculturing fungal strains with no visible growth onto a Sabouraud dextrose agar (SDA) plate. Results. Candida albicans and Cryptococcus neoformans were highly sensitive while Aspergillus flavus did not show sensitivity up to 1 mg/ml of essential oil; MICs ranged from 0.083 mg/ml to 0.208 mg/ml. Concentration and fungal species showed significant dose-dependent associations ( p < 0.0001 ) with antifungal activity. The MICs of essential oil were comparable to those of the standard drug (fluconazole) against C. glabrata and C. krusei. The lowest MFC of the essential oil was observed against Candida parapsilosis (0.145 mg/ml) while the highest MFC was against Candida krusei (0.667 mg/ml). Conclusion. Echinops kebericho essential oil showed noteworthy antifungal activity against Cryptococcus neoformans, Candida albicans, and Candida glabrata and could be a potential candidate for further antifungal drug development.

scholarly journals Antifungal activity of thymol against clinical isolates of fluconazole-sensitive and -resistant Candida albicans

2009 ◽  
Vol 58 (8) ◽  
pp. 1074-1079 ◽  
Author(s):  
Na Guo ◽  
Jingbo Liu ◽  
Xiuping Wu ◽  
Xingming Bi ◽  
Rizeng Meng ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Concentration Index ◽  
Inhibitory Concentration ◽  
Clinical Isolates ◽  
Standard Strain ◽  
Antagonistic Action ◽  
Microdilution Method ◽  
Interaction Intensity

Thymol (THY) was found to have in vitro antifungal activity against 24 fluconazole (FLC)-resistant and 12 FLC-susceptible clinical isolates of Candida albicans, standard strain ATCC 10231 and one experimentally induced FLC-resistant C. albicans S-1. In addition, synergism was observed for clinical isolates of C. albicans with combinations of THY–FLC and THY–amphotericin B (AMB) evaluated by the chequerboard microdilution method. The interaction intensity was determined by spectrophotometry for the chequerboard assay, and the nature of the interactions was assessed using two non-parametric approaches [fractional inhibitory concentration index (FICI) and ΔE models]. The interaction between THY–FLC or THY–AMB in FLC-resistant and -susceptible strains of C. albicans showed a high percentage of synergism by the FICI method and the ΔE method. The ΔE model gave results consistent with FICI, and no antagonistic action was observed in the strains tested.

In vitro anti-Candida albicans activity of new thiatriazole derivative agents

2017 ◽  
Vol 7 (1) ◽  
pp. 7-17
Author(s):  
Cecylia Łukaszuk ◽  
Andrzej Niewiadomy
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Enzymatic Activity ◽  
Reference Strain ◽  
Strain Atcc ◽  
Rpmi Medium ◽  
Three Samples ◽  
The Mean

Purpose: We tested the antifungal activity of N,N-phenyl-1,2,3,4-thiatriazole-5-yl-2,4-b-resorcyl-carbothioamide (PTR), of n-3-(1,2,4-dithiazole-5-thione)--resorcylcarbothioamide (DTRTA), of N,N-phenyl-1,2,3,4-thiatriazol-5-yl-2,4-b-resorcyl-carbothioamide (PHARA) against Candida albicans strains in vitro. Materials and methods: We synthesized PTR, DTRTA and PHARA at the Department of Chemistry University of Agriculture in Lublin. We tested the selected three samples with the lowest value of MIC - PTR, DTRTA and PHARA. A reference strain of C. albicans ATCC 10231 and 250 strains of C. albicans isolated from the patients was used. The enzymatic activity of the yeast-like fungi was performed by API ZYM test (bioMériux). Results: The mean MIC C. albicans ATCC 10231 on Sabouraud’s Medium was 12.5 mg/L and YNB Medium and RPMI medium - 6.25 mg/L. The mean MIC C. albicans on Sabouraud’s Medium - exposure to PTR - 19.77 mg/L; exposure to DTRTA -21.06 mg/L, exposure to PHARA - 21.54 mg/L; on YNB Medium - exposure to PTR - 17.79 mg/L; exposure to DTRTA - 16.23 mg/l, exposure to PHARA - 18.92 mg/L and RPMI Medium - exposure to PTR - 12.73 mg/L; exposure to DTRTA -10.93 mg/l, exposure to PHARA - 10.65 mg/L. The reference C. albicans strain ATCC 10231 had 5 enzymes inhibited - after exposure to PTR inhibited the enzymatic activity of 13 enzymes, exposure to DTRTA inhibited the enzymatic activity of 10 enzymes and exposure to PHARA inhibited the enzymatic activity of 13 enzymes. The C. albicans isolates had 3 enzymes inhibited - after exposure to PTR - 5 enzymes was inhibited, exposure to DTRTA - 9 enzymes was inhibited and exposure to PHARA - 4 enzymes was inhibited. Conclusion: The synthesized compounds PTR, DTRA and PHARA exert a moderate antifungal activity against the C. albicans strains in vitro.

scholarly journals An evaluation of the antifungal activity of some local medicinal plants against growth of Candida albicans in vitro

2010 ◽  
Vol 9 (2) ◽  
pp. 60
Author(s):  
J.S. Al-Hussaini, and A. M. G. Al-Mohana
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Culture Media ◽  
Aloe Vera ◽  
Ethanolic Extract ◽  
Diffusion Method ◽  
Thymus Vulgaris ◽  
Elettaria Cardamomum ◽  
Local Plants

The aim of this study was to evaluate the antifungal activity of the ethanolic extract of three local plants ( Elettaria cardamomum, Aloe vera, Thyme Vulgaris) against the growth of pathogenic Candida albicans in culture media. The antifungal activity was carried out by using agar well diffusion method. Ethanolic extracts of Elettaria cardamomum and Aloe vera inhibited the growth of Candida albicans isolates at all concentrations which tested in the present study (25, 50, 100, 150, 200, and 400) mg/ml, while the extract of Thymus vulgaris showed no activity against tested Candida albicans

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