Synthesis and In-vitro Antifungal Evaluation of 5- Pyrazolones

A series of 4-chloro-3-methyl-N-(substituted phenyl)-5-oxo-4,5-dihydro-1H-pyrazole-1- carbothioamide were synthesized using earmark reaction of thiosemicarbazides and ethyl-2-chloroacetoacetate in DMF. All structures of the synthesized compounds were distinguished on the basis of IR,1H-NMR,13C-NMR and also elemental analysis. Synthesized Compounds were examined their potent antifungal activity using disc diffusion technique against three fungal pathogens vizAspergillus niger, Candida albicansandCurvularia. Fluconazole were used as standard drug respectively. All compounds exhibited good to moderate activity.

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

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2020/3101324 ◽

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.

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Synthesis, Crystal Structure, and Biological Activity ofcis/transAmide Rotomers of (Z)-N′-(2-Oxoindolin-3-ylidene)formohydrazide

Journal of Chemistry ◽

10.1155/2014/760434 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 9

Author(s):

Hatem A. Abdel-Aziz ◽

Hazem A. Ghabbour ◽

Wagdy M. Eldehna ◽

Maha M. Qabeel ◽

Hoong-Kun Fun

Keyword(s):

Crystal Structure ◽

Human Tumor ◽

Cancer Cell Line ◽

Monoclinic Space Group ◽

Moderate Activity ◽

Standard Drug ◽

X Ray ◽

H Nmr ◽

Mcf 7

(Z)-N′-(2-Oxoindolin-3-ylidene)formohydrazide (2) was synthesized by the reaction of (Z)-3-hydrazonoindolin-2-one (1) with formic acid under reflux. The structure of2was characterized by IR, Mass,1H NMR, and X-ray crystal structure determination. Interestingly, compound2appeared in DMSO-d6ascisandtransamide rotomers in 25% and 75%, respectively. The X-ray analysis showed theZgeometrical isomer of2around –C=N– forcisandtransamide rotomers. The crystal of2belongs to monoclinic, space groupP21/c, witha=4.5206(1) Å,b=22.4747(7) Å,c=17.3637(5) Å,β=103.752(1)°,Z=8,V=1713.57(8) Å3,Dc=1.467 Mg m−3,μ=0.11 mm−1,F(000)=784,R=0.047, andwR=0.123for 3798 observed reflections withI>2σ(I). Compound2exhibited a moderate activity in its antimicrobial evaluation againstE. coliandP. aeruginosaand a good activity againstS. aureusclose to that of the standard drug ciprofloxacin. Thein vitroanticancer activity of2was evaluated against two human tumor cell lines, namely, HepG2 hepatocellular carcinoma and MCF-7 breast cancer. HepG2 cancer cell line was more susceptible to compound2than MCF-7.

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Synthesis of (E)-(4-(Aryl)phenyl)(3-(2-(1-phenyl-3-(thiophen-2-yl)-1Hpyrazol-4-yl)vinyl)benzofuran-2-yl)methanones by Claisen Schmidt-Suzuki Cross Coupling and their Antibacterial and Antifungal Activity

Journal of the Mexican Chemical Society ◽

10.29356/jmcs.v61i3.342 ◽

2017 ◽

Vol 61 (3) ◽

Author(s):

Ashok Dongamanti ◽

Mohammad Ziauddin ◽

Bommidi Vijaya Lakshmi ◽

Madderla Sarasija

Keyword(s):

Antifungal Activity ◽

Coupling Reaction ◽

Cross Coupling ◽

Bacterial Strains ◽

Mass Spectral ◽

H Nmr ◽

Cross Coupling Reaction ◽

Antibacterial And Antifungal ◽

C Nmr

A series of ten novel (E)-(4-(aryl)phenyl)(3-(2-(1-phenyl-3- (thiophen-2-yl)-1H-pyrazol-4-yl)vinyl)benzofuran-2-yl)methanones (7a-j) derivatives were prepared by traditional Claisen-Schmidt and Suzuki cross-coupling reaction under conventional and microwave irradiation conditions. The structures of all the newly synthesized compounds were established on the basis of FTIR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. The products were assayed for their in vitro antibacterial activity against different types of bacterial strains. Further the antifungal activity was examined by inhibitory action against three fungal strains such as Aspergillus niger, Aspergillus flavus and Fusarium oxysporum.

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Antimitotic activity of Piper nigrum on clinical isolates of candida

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v10i2.400 ◽

2019 ◽

Vol 10 (2) ◽

pp. 1167-1171

Author(s):

Gayathri Karthikeyan ◽

Geetha RV ◽

Lakshmi Thangavelu

Keyword(s):

Candida Albicans ◽

Antifungal Activity ◽

Ethanolic Extract ◽

Fungal Species ◽

Clinical Isolates ◽

Diffusion Method ◽

Piper Nigrum ◽

Disc Diffusion ◽

Antimitotic Activity ◽

Diffusion Technique

The objective of this study is to analyse the antimycotic activity of pepper on the clinical isolates of Candida. The extracts were prepared in the following concentrations in sterile water. 5mg/ml and 10mg/ml and 20mg/ml. 100µl of an extract of different concentrations were loaded on sterile filter paper discs measuring 6mm in diameter, so that the concentration of the extract on each disc was 500µg, 1000 µg and 2000µg respectively. The discs were dried and kept aseptically. Screening of antifungal activity [dis diffusion technique] The ethanolic extract of Piper nigrum was screened for antifungal activity by the disc diffusion method. Effect of three different concentrations (2000, 1000, 500,µg /disc) of the ethanolic extract Of Piper nigrum was tested against Candida albicans using disc diffusion technique. All the concentrations of the test solution inhibited the fungal species with varying degree of sensitivity. The inhibitory zone was measured with respect to the different concentration of the extracts which include 2000 µg/disc and 500 µg/disc at both room temperature and cold temperature (4-8°c). The inhibition zones were evaluated at 24 and 48 hrs. The result of this study revealed that the pepper oil has pronounced inhibitory activities against Candida albicans. This result is comparable with studies which have shown that Piper nigrum has a broad antibacterial activity. Since Piper nigrum is easily available and well-tolerated, it can be incorporated into medication for topical antifungal therapy as well.

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In vitro Antimicrobial Activity of Some Synthetic Isoindolinone and Isoquinolinone Derivatives

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v5i1.222 ◽

1970 ◽

Vol 5 (1) ◽

pp. 15-19 ◽

Cited By ~ 1

Author(s):

AFG Masud Reza ◽

Md. Wahab Khan ◽

Mohammad S Rahman ◽

Chowdhury M Hasan ◽

Mohammad A Rashid

Keyword(s):

Fungal Pathogens ◽

Moderate Activity ◽

Gram Negative Bacteria ◽

Disc Diffusion ◽

Gram Negative ◽

Key Words 2 ◽

Substituted Benzamides ◽

Substituted Benzamide ◽

Antimicrobial Assay

A total of six N-substituted benzamides, eight isoindolinone derivatives and six isoquinolinone analogs have been screened against five Gram positive and twelve Gram negative bacteria as well as four human fungal pathogens. From the antimicrobial screening, it is evident that 2-iodo-N-subustituted tetrahydro-1-oxo isoquinoline-3-carboxylic acids showed very prominent activity at a concentration 200 µg/disc, while the N-subtituted-3-alkyl isoindolin-1-one acetates showed weak to moderate activity. At the same time, 2-iodo-N-subustituted benzamides revealed very poor activity. Key words: 2-iodo-N-substituted benzamide, Isoindolinone, Isoquinolinone, Antimicrobial assay, Disc diffusion. Dhaka Univ. J. Pharm. Sci. Vol.5(1-2) 2006 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

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Synthesis and In Vitro Antimicrobial Activity of 3-(5-((2-Oxo-2H-Chromen-4-yl)Thio)-4-Phenyl-Thiazol-2-yl)-2-Substitutedphenyl Thiazolidin-4-One

International Letters of Chemistry Physics and Astronomy ◽

10.18052/www.scipress.com/ilcpa.51.135 ◽

2015 ◽

Vol 51 ◽

pp. 135-143

Author(s):

Himanshu R. Prajapati ◽

Harshad P. Lakum ◽

Kishor H. Chikhalia

Keyword(s):

Antimicrobial Activity ◽

Thioglycolic Acid ◽

Moderate Activity ◽

Mass Analysis ◽

Dilution Technique ◽

H Nmr ◽

Microbial Strain ◽

Broth Dilution ◽

C Nmr

An array of 3-(5-((2-oxo-2H-chromen-4-yl) thio)-4-phenyl thiazol-2-yl)-2-substitutedphenyl thiazolidin-4-one (7a-j) have been synthesized by using acetophenone, thiourea, 4-mercaptocoumarin and thioglycolic acid. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR and mass analysis. All the newly synthesized derivatives were evaluated for their in vitro antibacterial activity (against E.coli,P.aeruginosa,S.aureus, S. pyogenes) and antifungal activity against (C. albicans, A.niger, A.clavatus) using broth dilution technique. Some of the compounds showed good to moderate activity against the specific microbial strain.

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

Jurnal Ilmu Kedokteran ◽

10.26891/jik.v9i2.2015.71-77 ◽

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%.

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

Pharmaceutics ◽

10.3390/pharmaceutics13070998 ◽

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.

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Biodirected Synthesis of Silver Nanoparticles Using Aqueous Honey Solutions and Evaluation of Their Antifungal Activity against Pathogenic Candida Spp.

International Journal of Molecular Sciences ◽

10.3390/ijms22147715 ◽

2021 ◽

Vol 22 (14) ◽

pp. 7715

Author(s):

Grzegorz Czernel ◽

Dominika Bloch ◽

Arkadiusz Matwijczuk ◽

Jolanta Cieśla ◽

Monika Kędzierska-Matysek ◽

...

Keyword(s):

Silver Nanoparticles ◽

Antifungal Activity ◽

Fungal Pathogens ◽

Fungal Growth ◽

Disc Diffusion ◽

Candida Spp ◽

Antifungal Effect ◽

Synthesis Of Nanoparticles ◽

Honey Solution ◽

Diffusion Assay

Silver nanoparticles (AgNPs) were synthesized using aqueous honey solutions with a concentration of 2%, 10%, and 20%—AgNPs-H2, AgNPs-H10, and AgNPs-H20. The reaction was conducted at 35 °C and 70 °C. Additionally, nanoparticles obtained with the citrate method (AgNPs-C), while amphotericin B (AmB) and fluconazole were used as controls. The presence and physicochemical properties of AgNPs was affirmed by analyzing the sample with ultraviolet–visible (UV–Vis) and fluorescence spectroscopy, scanning electron microscopy (SEM), and dynamic light scattering (DLS). The 20% honey solution caused an inhibition of the synthesis of nanoparticles at 35 °C. The antifungal activity of the AgNPs was evaluated using opportunistic human fungal pathogens Candida albicans and Candida parapsilosis. The antifungal effect was determined by the minimum inhibitory concentration (MIC) and disc diffusion assay. The highest activity in the MIC tests was observed in the AgNPs-H2 variant. AgNPs-H10 and AgNPs-H20 showed no activity or even stimulated fungal growth. The results of the Kirby–Bauer disc diffusion susceptibility test for C. parapsilosis strains indicated stronger antifungal activity of AgNPs-H than fluconazole. The study demonstrated that the antifungal activity of AgNPs is closely related to the concentration of honey used for the synthesis thereof.

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Rhizosphere-enriched microbes as a pool to design synthetic communities for reproducible beneficial outputs

FEMS Microbiology Ecology ◽

10.1093/femsec/fiz138 ◽

2019 ◽

Cited By ~ 6

Author(s):

Maria-Dimitra Tsolakidou ◽

Ioannis A Stringlis ◽

Natalia Fanega-Sleziak ◽

Stella Papageorgiou ◽

Antria Tsalakou ◽

...

Keyword(s):

Antifungal Activity ◽

Fungal Pathogens ◽

Growth Parameters ◽

Tomato Plants ◽

Beneficial Effects ◽

Negative Effect ◽

Tomato Growth ◽

In Vitro Antifungal Activity

Abstract Composts represent a sustainable way to suppress diseases and improve plant growth. Identification of compost-derived microbial communities enriched in the rhizosphere of plants and characterization of their traits, could facilitate the design of microbial synthetic communities (SynComs) that upon soil inoculation could yield consistent beneficial effects towards plants. Here, we characterized a collection of compost-derived bacteria, previously isolated from tomato rhizosphere, for in vitro antifungal activity against soil-borne fungal pathogens and for their potential to change growth parameters in Arabidopsis. We further assessed root-competitive traits in the dominant rhizospheric genus Bacillus. Certain isolated rhizobacteria displayed antifungal activity against the tested pathogens and affected growth of Arabidopsis, and Bacilli members possessed several enzymatic activities. Subsequently, we designed two SynComs with different composition and tested their effect on Arabidopsis and tomato growth and health. SynCom1, consisting of different bacterial genera, displayed negative effect on Arabidopsis in vitro, but promoted tomato growth in pots. SynCom2, consisting of Bacilli, didn't affect Arabidopsis growth, enhanced tomato growth and suppressed Fusarium wilt symptoms. Overall, we found selection of compost-derived microbes with beneficial properties in the rhizosphere of tomato plants, and observed that application of SynComs on poor substrates can yield reproducible plant phenotypes.

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