Evaluation Of Antifungal Activity Research Articles

Synthesis and antifungal activity evaluation of novel pyridine derivatives as potential succinate dehydrogenase inhibitors

Two series of novel pyridine derivatives (1a−l, 2a−l) were synthesized and characterized by IR, 1H NMR, 13C NMR, and HRMS. The crystal structures of compounds 1 h and 2l were characterized by single crystal X-ray diffraction and crystallized in the monoclinic and orthorhombic system, respectively. The in vitro antifungal activity of synthesized compounds were determined against five plant pathogenic fungi namely Gibberella zeae, Helminthosporium maydis, Rhizoctonia solani, Botrytis cinerea, and Sclerotinia sclerotiorum and most of the target compounds revealed significant antifungal activity at 20 mg/L. Of these, the inhibitory rate and the median effect concentrations (EC50) of compounds 1 m, 2i, 2o, and 2p were more close to fluopyram against B. cinerea. Meanwhile, the half inhibitory concentrations (IC50) of compounds 1 m, 2i, 2o, and 2p against succinate dehydrogenase (SDH) and their score in molecular docking were also more close to fluopyram, indicating the stronger antifungal activities of the four compounds were well associated with the affinities of these compounds in interacting with SDH. Therefore, we concluded that compounds 1 m, 2i, 2o, and 2p might be potential succinate dehydrogenase inhibitors (SDHIs), which was been reported for the first time.

Chemical Composition and Biological Activities of Anethum graveolens L. Essential Oil from Algeria

Anethum graveolens commonly known as dill plant is a very important shrub which is widely acknowledged in traditional and modern medicine for its capacity to treat colic pain and flatulence. The purpose of this work is the study of the chemical composition and the evaluation of antibacterial, antifungal and antioxidant activities of A. graveolens essential oil. The samples were collected from the chellal region in Algeria and submitted to hydrodistillation. The essential oil extracted was analyzed by GC and GC/MS. The antibacterial and antifungal activities were tested by the disc diffusion method; seven bacteria and four phytopathogenic fungi were used. The evaluation of the antioxidant activity was carried out by the 2,2-diphenyl-1-picrylhydrazyl scavenging method. The results of the GC and GC/MS analysis allowed the identification of 22 components with carvone(34.33%), α-phellendrene (22.03%), dill ether (18.84%), limonene (6.93%) and dill apiol (5.01%) as major components. The results of the disc difusion method show that Anethum graveolens essential oil exhibits strong antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and moderate antifungal activity against Fusarium graminum and Alternaria alternata. The pure essential oil showed a moderate antioxidant activity with inhibition percentages of 49.93 ± 4.58%. This study highlights the importance of chemical constituents of A. graveolens essential oil which possesses important pharmacological effects on different pathogenic strains and could be used as substitute for synthetic antimicrobial drugs in pharmaceutical industries.

Computer-aided molecular design, synthesis and evaluation of antifungal activity of heterocyclic compounds

Outpatient complications for fungal infections in immunocompromised patients and the development of antimicrobial drug resistance mechanisms demonstrate the need to develop new antifungal agents. In this perspective, heterocyclic compounds namely thiazolylhydrazones, furan, tetrazole, triazole and thiadiazoline derivatives were synthesized and tested in vitro against seven clinical importance Cryptococcus and Candida species. In this study, virtual screening techniques were applied using a scaffold-hopping database, FDA approved drugs and a ZINC subset. Some of the compounds evaluated showed promising antifungal activity against C. albicans, C. glabrata, C. krusei, C. parapsilosis, C. tropicalis, C. neoformans and C. gatti, displaying minimal inhibitory concentration (MIC) values in the range of 0.12–250 µM.

Novel α-Aminophosphonates and α-Aminophosphonic Acids: Synthesis, Molecular Docking and Evaluation of Antifungal Activity against Scedosporium Species.

The Scedosporium genus is an emerging pathogen with worldwide prevalence and high mortality rates that gives multidrug resistance to antifungals; therefore, pharmacological alternatives must be sought for the treatment of diseases caused by this fungus. In the present project, six new α-aminophosphates were synthesized by the Kabachnik–Fields multicomponent reaction by vortex agitation, and six new monohydrolyzed α-aminophosphonic acids were synthesized by an alkaline hydrolysis reaction. Antifungal activity was evaluated using the agar diffusion method as an initial screening to determine the most active compound compared to voriconazole; then it was evaluated against 23 strains of the genus Scedosporium following the M38-A2 protocol from CLSI (activity range: 648.76–700 µg/mL). Results showed that compound 5f exhibited the highest antifungal activity according to the agar diffusion method (≤1 mg/mL). Cytotoxicity against healthy COS-7 cells was also evaluated by the MTT assay and it was shown that compound 5f exhibits a lower toxicity in comparison to voriconazole at the same concentration (1000 µM). A docking study was conducted afterwards, showing that the possible mechanism of action of the compound is through the inhibition of allosteric 14-α-demethylase. Taking these results as a basis, 5f is presented as a compound with attractive properties for further studies.

Synthesis of Coumarin and Homoisoflavonoid Derivatives and Analogs: The Search for New Antifungal Agents.

A set of twenty-four synthetic derivatives, with coumarin and homoisoflavonoid cores and structural analogs, were submitted for evaluation of antifungal activity against various species of Candida. The broth microdilution test was used to determine the Minimum Inhibitory Concentration (MIC) of the compounds and to verify the possible antifungal action mechanisms. The synthetic derivatives were obtained using various reaction methods, and six new compounds were obtained. The structures of the synthesized products were characterized by FTIR spectroscopy: 1H-NMR, 13C-NMR, and HRMS. The coumarin derivative 8 presented the best antifungal profile, suggesting that the pentyloxy substituent at the C-7 position of coumarin ring could potentiate the bioactivity. Compound 8 was then evaluated against the biofilm of C. tropicalis ATCC 13803, which showed a statistically significant reduction in biofilm at concentrations of 0.268 µmol/mL and 0.067 µmol/mL, when compared to the growth control group. For a better understanding of their antifungal activity, compounds 8 and 21 were submitted to a study of the mode of action on the fungal cell wall and plasma membrane. It was observed that neither compound interacted directly with ergosterol present in the fungal plasma membrane or with the fungal cell wall. This suggests that their bioactivity was due to interaction involving other pharmacological targets. Compound 8 was also subjected to a molecular modeling study, which showed that its antifungal action mechanism occurred mainly through interference in the redox balance of the fungal cell, and by compromising the plasma membrane; not by direct interaction, but by interference in ergosterol synthesis. Another important finding was the antifungal capacity of homoisoflavonoids 23 and 24. Derivative 23 presented slightly higher antifungal activity, possibly due to the presence of the methoxyl substituent in the meta position in ring B.

Evaluation of antibacterial and antifungal activities of N-benzylthienopyrimidinone derivatives

This study is part of the biological investigation of the chemical library of molecules already described by the Laboratory of Organic Chemistry and Therapeutic Chemistry of the University of Bordeaux. The main objective was to explore the contribution of a thienyl moiety attached to the pyrimidinone nucleus, in the expression of an antimicrobial activity.
 The structural modifications mainly concerned the conservation or not of the benzo fragment attached to the thienyl, the saturation or not in position-1,2 of the pyrimidinone ring, the substitution on N-benzyl with more or less lipophilic units, the modification of the orientation of the thienyl fragment with, on the one hand, the compounds in which the sulfur is located near the N1 nitrogen (series of thieno[2,3-d]pyrimidin-4-ones) and on the other hand, compounds in which the sulfur is located near the ketone group (series of thieno[3,2-d]pyrimidin-4-ones).
 In general, thienyl fragment with sulfur located near the ketone group and the unsaturated pyrimidinone nucleus in the 1,2-position, seem to promote a broad spectrum of antibacterial activity, with compound 9c which is active on both Gram + bacteria and Gram – bacteria studied. The same pattern was observed for antifungal activity, which is maximum with the compounds of the thieno[3,2-d]pyrimidin-4-ones series for an MIC of 31.25 μg/ml on the strains of Candida albicans and Candida kruzei studied.
 Keywords: Thienopyrimidinones, antibacterial activity, antifungal activity.

Chemical Composition and Evaluation of the Antibacterial and Antifungal Activities of Pre-Rif Teucrium polium Essential Oil

As part of the valorization of Aromatic and Medicinal Plants (AMP) in Morocco, we studied the chemical composition and the antibacterial and antifungal activities of Teucrium polium Essential Oil harvested in a region of Pre-Rif, Taza in Morocco (BniKrama). After extraction of the essential oil (EO) by hydro-distillation process, the study of the chemical composition of this EO was carried out by gas chromatography (GPC) and GC/MS (gas chromatography- mass spectrometry), and the evaluation of antibacterial and antifungal activity was carried out against eleven microbial strains by determining the minimum concentration inhibitor. The yield after extraction by hydro-distillation is 0.71%. After (CPG) of the essence of this plant, sixty-eight components have been identified, of which α-Pinene is the major component (21.96%). It is followed by Limonene (18.77%), and β-Pinene (8.46%). The essential oil of T. polium (EOTP) has shown strong antibacterial and antifungal activity. This bioactivity is mainly due to the richness of this essence in terpenes known by their effectiveness against microbial agents. This essential oil is very rich in chemical molecules. Antimicrobial tests show that this EOTP has a broad spectrum on molds, fungi and bacteria.

ANTIFUNGAL ACTIVITY OF ESSENTIAL OILS FROM NATIVE TREE SPECIES IN SOUTHERN BRAZIL

The objective of this exploratory work was to analyze the yield and chemical composition of essential oils (EO) from Blepharocalyx salicifolius [BS] and from two pools of EO obtained from Nectandra megapotamica [NM1 and NM2], as well as to evaluate their antifungal properties against the fungi Pycnoporus sanguineus (white-rot) and Gloeophyllum trabeum (brown-rot). The EO were obtained by hydrodistillation and its components were identified by gas chromatography coupled to mass spectrometry (GC-MS) and quantified with flame ionization detection (GC-FID). For the evaluation of antifungal activity, the mycelial growth index (MGI) and the mycelial growth inhibition (GI) of BS were determined at concentrations of 1, 2 and 5 µL.mL-1, and 0.25; 0.5 and 1 µL.mL-1 for MN1 and NM2. The yield of EOs was 2.29% (BS), 0.14% (NM1) and 0.17% (NM2). The major components of BS EO were eucalyptol (63.44%) and β-caryophyllene (13.68%), from NM1 were bicyclogermacrene (16.14%) and α-pinene (15.93%), and for NM2, α-pinene (19.04%) and sabinene (16.66%). EO NM1 (1μL.mL-1) showed the best result for antifungal activity, inhibiting about 57.55 ± 0.68 % of P. sanguineus growth and 58.82 ± 0.78 % in the test with G. trabeum.

Bio-waste eggshell membrane assisted synthesis of NiO/ZnO nanocomposite and its characterization: Evaluation of antibacterial and antifungal activity

This paper presents the synthesis of NiO/ZnO nanocomposite using a bio-waste eggshell membrane as a template, which is used to control the particle size. It is a two-step process, soaking followed by the calcination method. The synthesized NiO/ZnO nanocomposite was characterized by the following techniques: Powdered X-ray diffraction analysis (PXRD), Ultra-Violet Visible spectroscopy (UV–Visible), Fourier transformed infra-red spectroscopy (FT-IR), Raman spectroscopy, Dynamic Light Scattering analysis (Zeta potential & particle size), Field Emission Scanning Electron Microscope (FE-SEM) with Energy Dispersive X-ray Analysis (EDX), and Hi-ResolutionTransmission electron microscope (HR-TEM) respectively. The NiO/ZnO nanocomposite exists in both face-centered cubic (NiO) and hexagonal wurtzite (ZnO) structures, according to PXRD results. The crystallite size was equal to 14.12 nm (NiO) and 14.70 nm (ZnO). The UV–Visible spectrum showed the wavelength at 302 nm and 372 nm, which indicates the presence of NiO and ZnO. The peaks at 449 cm−1 and 550 cm−1 are due to the stretching vibration of (Ni-O) NiO2 octohedral in the cubic NiO and the stretching vibration of ZnO. A Raman vibrational mode confirms the formation of the NiO/ZnO nanocomposite. The zeta potential analysis of the NiO/ZnO nanocomposite was equal to −42.7 mV, which indicates good stability, and the particle size distribution was equal to be 205.8 nm with a polydispersity index value of 0.5940. The SEM images of the NiO/ZnO nanocomposite appeared aggregated with small rods. The EDX spectra confirmed the presence of nickel, oxygen, and zinc, respectively. TEM images of the NiO/ZnO nanocomposite showed the particle size is less than 50 nm. The synthesized NiO/ZnO nanocomposite was subjected to antibacterial and antifungal activity by the agar-well diffusion method. The results demonstrated that the zone of inhibition of NiO/ZnO nanocomposite was high in Bacillus subtilis (30 ± 0.88 mm) for bacterial pathogens and Aspergillus terreus (30 ± 0.0 mm) for fungal pathogens, respectively. The minimum inhibition concentration (MIC) of NiO/ZnO nanocomposite was tested for bacterial pathogens. The results showed that the synthesized NiO/ZnO nanocomposite inhibited cell growth even at the lowest concentration (9.37 μg/mL). So it is inferred that the NiO/ZnO nanocomposite could act as an antifungal and antibacterial agent for a wide range of diseases.

DFT Studies and Quantum Chemical Calculations of Benzoyl Thiourea Derivatives Linked to Morpholine and Piperidine for the Evaluation of Antifungal Activity

Background: Benzoyl thiourea derivatives linked to morpholine and piperidine have been reported to possess good antifungal activity. Objective: The aim of the study was to find the correlations between the quantum chemical calculations and the antifungal activity of the benzoyl thiourea derivatives linked to morpholine and piperidine. Methods: Optimization of six compounds BTP 1-3 and BTM 4-6 was carried out with DFT using B3LYP method utilizing 6-31G(d,p) basis set. The structural parameters of the compounds as molecular geometry, bond lengths, bond angles, atomic charges and HOMOLUMO energy gap have been investigated and compared with the reported experimental results. Results: A good correlation between the quantum chemical calculations and the antifungal activity of the benzoyl thiourea derivatives linked to morpholine and piperidine was found. Conclusion: The DFT study of benzoyl thiourea derivatives linked to morpholine and piperidine conducted with respect to their Quantum chemical parameters for evaluation of their antifungal activity showed good correlations between the antifungal activity and the quantum chemical parameters.

Evaluation of antimicrobial and antifungal activity of hydroethanolic extracts of in vitro and ex vitro seedlings of Dionaea muscipula J. Ellis

Objective: To evaluate the antibacterial and antifungal activity of hydroethanolic extracts of Dionaea muscipula J. Ellis against bacteria models and fungi of agricultural importance. Design/Methodology/Approach: In vitro plants of D. muscipula were propagated and acclimatized for three months. The antibacterial activity of the hydroethanolic extracts against Escherichia coli and Bacillus cereus was evaluated, and the antifungal activity against Aspergillus niger, Fusarium oxysporum and Pseudocercospora fijiensis. Analysis of variance (ANOVA) was carried out to compare the means obtained with Tukey’s test (p≤0.05). Results: The hydroethanolic extracts of in vitro and acclimatized D. muscipula presented bacteriostatic activity against the bacteria E. coli (65.20 and 69.78 % of inhibition) and B. cereus (91.75 and 92.61 % of inhibition), and antifungal activity against the fungus P. fijiensis of 7.56 and 14.21 % of inhibition, respectively. Study Limitations/Implications: The hydroethanolic extracts of in vitro and acclimatized D. muscipula did not show antifungal activity against A. niger and F. oxysporum. Findings/Conclusions: The hydroethanolic extracts of in vitro and acclimatized D. muscipula presented bacteriostatic activity against bacteria E. coli and B. cereus and antifungal activity against the fungus P. fijiensis.

Design, synthesis, and biological evaluation of novel spiro[pyrrolidine-2,3′-quinolin]-2′-one derivatives as potential chitin synthase inhibitors and antifungal agents

A series of novel spiro-quinolinone derivatives were designed and synthesized and their structures were confirmed by spectroscopic methods. The enzymatic experiments showed that all the seventeen synthesized compounds had inhibition potency against chitin synthase, among them five compounds had excellent inhibition potency that equal to that of polyoxin B. The Kinetic parameters of enzymatic assays indicated that these compounds were non-competitive inhibitors of chitin synthase. The antimicrobial experiments displayed that the synthesized compounds had selectively and broad-spectrum antifungal activity in vitro Among them, two compounds had stronger antifungal activity against C. albicans than that of fluconazole meanwhile five others compounds showed antifungal activity against C. albicans being equal to that of fluconazole. Moreover, there are four or five compounds that possessed antifungal activities against C. neoformans, A. fumigatus and A. flavus as high as fluconazole had, respectively. The sorbitol protection assay and evaluation of antifungal activity against micafungin-resistant strain further verified that these compounds possessed antifungal activity through inhibiting the synthesis of chitin of cell wall. The evaluation of antifungal activity against others drug-resistant fungi variants showed these designed compounds had significant antifungal activity against these tested variants. The combination use experiments exhibited that the synthesized compounds had synergistic effects or additive effects with current used drugs in clinic. These results demonstrated that these synthesized compounds were chitin synthase inhibitors and had selective and broad-spectra antifungal activities.

Evaluation of antifungal activity of some plant essential oils against tomato grey mould disease

Evaluation of antifungal activity of some plant essential oils against tomato grey mould disease

Phytochemical evaluation and investigation of anti-Fungal activity of turnip top extracts

To evaluate the activity of Ethanolic and Aqueous extracts of leaves of against three fungal strains i.e. MTCC3814, and Candida tropicalis MTCC9038 in-vitro.Phytochemical analysis of belonging to family brassicacaea was examined using Ethanolic and Aqueous extracts. Ethanolic and Aqueous extracts of leaves of were investigated individually for antifungal activity by Agar well diffusion method. Both the extracts were tested against selected fungal strains i.e. and to find the inhibitory activities of fungal growth at the dose level of 50 and 100 μg/ml.The phytochemical analysis of ethanolic and aqueous extracts confirmed the presence of phenolic compounds, glycosides, tannins, carbohydrates, proteins, amino acids, tannins, reducing suger, non-reducing suger and inorganic compounds such as calcium, magnesium, iron, carbonate & sulphates. Ethanolic extract of showed considerably high antifungal activities against selected microorganisms than aqueous extract.Although the active components were not isolated but antifungal active plant principles such as flavonoids, glycosides and tannins were observed in the extract. Ethanolic extract of possess effective antifungal properties for selected fungal strains i.e.

Evaluation of Anti-microbial and Anti-fungal Activities of Nano-TiO2 Assembled with Graphene Composites

Nanocomposites assembled with TiO2 and graphene were synthesised under solvent free conditions. The calcinated nanocomposites have been characterized by PXRD, SEM-EDAX, HRTEM and Nitrogen adsorption-desorption techniques. Nanotitania was found to be formed in anatase phase with larger surface area (268.2 m2g-1) and with increase in graphene content, the absorbance increased towards visible region. Their biological applicability has been evaluated by examining their anti-bacterial activity against E. coli (ATCC29181), S. aurues (ATCC6538) and their anti-fungal activity against C. albicans, C. rugosa (ATCC10231) organisms. It has been observed that the biological activity has increased with increase in % graphene from 0.1 to 0.5 and showed a steady decrease with 1.0 % graphene. Compared, to the anti-fungal activity, anti-bacterial activity was identified to be major in the present studies.

Investigation of chemical composition and evaluation of antioxidant, antibacterial and antifungal activities of ethanol extract from Bidens pilosa L.

Investigation of chemical composition and evaluation of antioxidant, antibacterial and antifungal activities of ethanol extract from Bidens pilosa L.

Evaluation of Antifungal Activity of Some Plant Extractives

In vitro antifungal activity of thirty two extractives of seven plants obtained using hexane, ethyl acetate and methanol were tested against the mycelial growth of Colletotrichum gloeosporioides. Among these extractives, ethyl acetate extractives of onion seeds, chilli seeds and chilli pericarps and methanol extractives of chilli seeds and chilli pericarps exhibited more than 20 % mycelial growth inhibition at a concentration of 0.5 % level. Methanol extractives of Solanum viarum berries and ethyl acetate extractive of soybean leaves exhibited more than 20 % mycelial growth inhibition at a concentration of 1.0 % level. Thin layer chromatographic bioautography showed that hexane and ethyl acetate extractives of onion seeds, chilli seeds and chilli pericarps exhibited spore germination inhibition of Cladosporium cucumerinum at a dose of 1.0 mg.

Evaluation of Antifungal Activity of Moringa oleifera Seeds on Oral Candida Isolated from Type 2 Diabetic and Nondiabetic Complete Denture Wearers

Evaluation of Antifungal Activity of Moringa oleifera Seeds on Oral Candida Isolated from Type 2 Diabetic and Nondiabetic Complete Denture Wearers

Syntheses, structures, in vitro cytostatic activity and antifungal activity evaluation of four diorganotin(iv) complexes based on norfloxacin and levofloxacin

Four organotin(iv) complexes have been designed and synthesized from the reactions of R2SnO (R = Me, Ph) with the corresponding ligands norfloxacin and levofloxacin. And the cytostatic and antifungal activity test have been done.

N-acetylation of 2-aminobenzothiazoles with Acetic Acid for Evaluation of Antifungal Activity and In Silico Analysis

Acetamides (S30A1 and S30) were synthesized from benzo[d]thiazol-2-amine and 6-nitrobenzo[d]thiazol-2-amine by direct use of acetic acid instead of acetylating agents. The usual acetylating agents, acetic anhydride and acetyl chloride are very unstable especially because of their high sensitivity to environmental moisture. Thus, acetylation by direct use of acetic acid was searched as an alternative approach for synthesizing acetanilides. In this study, acetamides were synthesized with a yield of 88% and 82% respectively. The synthesized compounds were then screened for antifungal activity. At a concentration of 300 µg/disc, S30A1 showed 18 mm, 28 mm, 20 mm, and 16 mm zone of inhibitions against Penicillium notatum, Candida albicans, Aspergillus flavus, and Aspergillus niger, respectively. The standard miconazole was used at 50 µg/disc concentration. An in silico analysis was done for the possible binding modes in the C. albicans N-myristoyltransferase enzyme.