scholarly journals Synthesis, characterization and antifungal testing of 3,4-dihydropyrimidin-2(1H)-(thio)ones containing boronic acids and boronate esters

2008 ◽  
Vol 6 (4) ◽  
pp. 562-568 ◽  
Author(s):  
Dominique Duguay ◽  
Matthew Zamora ◽  
Johanna Blacquiere ◽  
Francis Appoh ◽  
Christopher Vogels ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Acid Catalyst ◽  
Boronic Acids ◽  
Boronate Esters ◽  
Pure Cultures ◽  
Lewis Acid Catalyst ◽  
Moderate Yield

AbstractThe addition of formylphenylboronic acid derivatives to thiourea and ethyl acetoacetate proceeds in the presence of an additional Lewis acid catalyst to give the corresponding 3,4-dihydropyrimidin-2(1H)-(thio)ones (Biginelli products) in moderate yield. Compounds were tested for antifungal activity against pure cultures of Aspergillus niger, Aspergillus flavus, Candida albicans and Saccharomyces cerevisiae but, unfortunately, none showed any appreciable activity.

Synthesis and Antimicrobial Screening of Some Novel 5-Substituted-1,10b-dihydroimidazole[1,2-c]quinazoline Derivatives

2021 ◽  
Vol 14 (2) ◽  
pp. 5406-5411
Author(s):  
Haribhai Rabari ◽  
Hetal Vankar ◽  
Beenkumar Prajapati
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Antifungal Compound ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Quinazoline Derivatives

The emergence of multidrug microbial resistance is the main challenges that the modern scientists have so far been facing in the recent era. In this respect, new series of drug classes having potential to give antimicrobial effect have been synthesized. A new series of 5- substituted-1,10 b-dihydroimidazole[1,2-c]quinazoline derivatives 8a-e have been synthesized and screened for antibacterial activity and antifungal activity. Synthesized derivatives were characterized by IR, MASS and 1H-NMR spectroscopy. Synthesized compounds show good activity, which was comparable to the standard drug and it can be useful for the further clinical study. Antibacterial activity was evaluated against four different pathogenic bacterial strains like Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Pseudo-monas aeruginosa. Among the screened compounds, 8e show good antibacterial activity against Staphylococcus aureus and Escherichia coli with MIC of 50 and 100 μg/ml respectively. Antifungal activity was evaluated  against two strains of fungi. Among the synthesized derivates, compound 8c was emerged out as the potent antifungal compound against Candida albicans and Aspergillus niger with MIC of 25 μg/ml and 75μg/ml respectively. Compound 8e also shows good antifungal activity with MIC of 50 μg/ml against both Candida albicans and Aspergillus niger. The overall results of this study indicated that  synthesized quinazoline derivatives had the potential to act as an antibacterial and antifungal agent, hence further investigation is warranted.

scholarly journals Reactive oxygen species (ROS) mediated enhanced anti-candidal activity of ZnS–ZnO nanocomposites with low inhibitory concentrations

RSC Advances ◽  
2015 ◽  
Vol 5 (94) ◽  
pp. 76718-76728 ◽  
Author(s):  
P. Suyana ◽  
S. Nishanth Kumar ◽  
Nimisha Madhavan ◽  
B. S. Dileep Kumar ◽  
Balagopal N. Nair ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Reactive Oxygen Species ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Candida Tropicalis ◽  
Yeast Species ◽  
Reactive Oxygen ◽  
Oxygen Species ◽  
Precipitation Technique

Enhanced antifungal activity against the yeast species Candida albicans, Candida tropicalis and Saccharomyces cerevisiae was displayed by ZnS–ZnO nanocomposites prepared by a simple precipitation technique.

Production of taunit–antibiotic nanocomplexes and study of their antifungal activity relative to Aspergillus niger and Candida albicans

2015 ◽  
Vol 51 (9) ◽  
pp. 887-892 ◽  
Author(s):  
A. V. Timofeeva ◽  
M. V. Ilyina ◽  
E. A. Stepashkina ◽  
L. A. Baratova ◽  
G. S. Katrukha
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger

Dihydropyrimidinones containing boronic acids

2005 ◽  
Vol 83 (12) ◽  
pp. 2052-2059 ◽  
Author(s):  
Johanna M Blacquiere ◽  
Oana Sicora ◽  
Christopher M Vogels ◽  
Miroslava Čuperlović-Culf ◽  
Andreas Decken ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Lewis Acid ◽  
Anticancer Agents ◽  
Breast Cancer Cell Line ◽  
Cancer Cell Line ◽  
Acid Catalyst ◽  
Boronic Acids ◽  
Ability To Act ◽  
Biginelli Compounds ◽  
Lewis Acid Catalyst

The addition of formylphenylboronic acid derivatives to urea and ethyl acetoacetate proceeds in the absence of an additional Lewis acid catalyst to give the corresponding dihydropyrimidinones (Biginelli products) in good yields. Novel boron-containing dihydropyrimidinones have been investigated for their ability to act as anticancer agents against the breast cancer cell line MCF7.Key words: anticancer, Biginelli compounds, boronic acids, breast cancer, dihydropyrimidinones.

scholarly journals UJI AKTIVITAS ANTIJAMUR BEBERAPA SENYAWA MONOKARBONIL ANALOG CURCUMIN HASIL SINTESIS

2018 ◽  
Vol 5 (2) ◽  
pp. 149
Author(s):  
Ismi Rahmawati ◽  
Desi Purwaningsih
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
1H Nmr ◽  
Aldol Condensation ◽  
Fungal Infections ◽  
Trichophyton Mentagrophytes ◽  
Curcumin Analogue ◽  
Pityrosporum Ovale ◽  
Post Hoc

Antifungal Activity of Some Synthesized Mono-Carbonyl Analogue Compounds of CurcuminABSTRACTFungal resistance can pose a threat to future fungal infections, therefore studies to find other compounds that have antifungal activity need to be done. The aim of this study was to examine antifungal activity of synthesized curcumin analogue compounds i.e. 2,6-Bis-(2'-furilidin)-cyclohexanone (26FuH); 2,5-Bis-(2'-furilidine)-cyclopentanone (25FuP) and 1,5-Difuril-1,4-pentadien-3-on (15FuA). The curcumin analogue compound was successfully synthesized with Aldol condensation using KOH 7.5% as the catalyst. The compound was purified and characterized by melting point, thin layer chromatography, gas chromatography with mass spectrometry, FTIR spectrophotometry, spectrophotometry 1H-NMR. The results showed pure compounds and have a structure that corresponds to the target compounds. All compound were assayed as antifungal against Candida albicans, Pityrosporum ovale, Aspergillus niger, and Trichophyton mentagrophytes. The activity of each compound represented by inhibitory diameter was analyzed by one-way ANOVA followed by post hoc Tukey (p<0.05). All three compounds showed antifungal activity against Candida albicans, Pityrosporum ovale, and Aspergillus niger. The best antifungal activity was shown by 26FuH against Pityrosporum ovale.Keywords: antifungal activity, curcumin, monocarbonyl, Pityrosporum ovale, synthesis ABSTRAKResistensi jamur dapat menjadi ancaman pada kasus infeksi jamur di masa mendatang, oleh sebab itu penelitian untuk menemukan senyawa lain yang memiliki aktivitas antijamur perlu dilakukan. Penelitian ini bertujuan untuk menguji aktivitas antijamur senyawa analog curcumin hasil sintesis yaitu senyawa 2,6-Bis-(2’-furilidin)-sikloheksanon (26FuH); 2,5-Bis-(2’-furilidin)-siklopentanon (25FuP) dan 1,5-Difuril-1,4-pentadien-3-on (15FuA). Senyawa analog curcumin sudah berhasil disintesis dengan metode kondensasi Aldol menggunakan katalis KOH 7,5%. Senyawa hasil sintesis dimurnikan dan dikarakterisasi dengan menggunakan pemeriksaan organoleptis, titik lebur, kromatografi lapis tipis, kromatografi gas dengan spektrometri massa, spektrofotometri FTIR, spektrofotometri 1H-NMR. Hasil menunjukkan senyawa murni dan struktur sesuai senyawa target. Hasil sintesis diuji aktivitas antijamur terhadap Candida albicans, Pityrosporum ovale, Aspergillus niger dan Trichophyton mentagrophytes. Hasil diameter daya hambat dianalisis dengan ANOVA satu arah dilanjutkan post hoc Tukey (p<0,05). Ketiga senyawa memiliki aktivitas antijamur terhadap jamur Candida albicans, Pityrosporum ovale, dan Aspergillus niger. Aktivitas antijamur terbaik adalah senyawa 26FuH terhadap jamur Pityrosporum ovale.Kata Kunci: aktivitas antijamur, curcumin, monokarbonil, Pityrosporum ovale, sintesis

scholarly journals Antifungal activity of Bacillussp. Gn-A11-18isolated from decomposing solid green household waste in water and soil against Candida albicans and Aspergillus niger

2020 ◽  
Vol 150 ◽  
pp. 02003 ◽  
Author(s):  
Azeddin El Barnossi ◽  
Fatimazahrae Moussaid ◽  
Abdelilah Iraqi Housseini
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Pathogenic Fungus ◽  
Bioactive Compound ◽  
Household Waste ◽  
Diffusion Method ◽  
Agar Plug ◽  
Opportunistic Pathogenic

Candida albicans an opportunistic pathogenic fungus causes many infections in humans. Whereas Aspergillus niger is a fungus that can produce ochratoxins, a group of extremely dangerous secondary metabolites that are classified as potentially carcinogenic to humans and also causing deterioration in grapes, strawberries, etc. The purpose of the current study is to isolate, purify, identify and characterize new microorganisms associated with solid green household waste for the control of C. albicans and A. niger. The antifungal activity of bacterial isolates was carried out in vitro by the agar plug diffusion method, the disk and well diffusion method. The isolate that showed promising activity has been identified by those macroscopic, microscopic and biochemical characteristics. The results obtained in the course of this study showed the isolation of an isolate named Gn-A11-18, which was shown to have significant inhibitory activity with a 42.66% inhibition percentage against A. niger and a 44.66 mm inhibition diameter against C. albicans compared to the controls. The identification of Gn-A11-18 isolate has shown that this isolate belongs to the genus Bacillus with a similarity to Bacillus subtilis and Bacillus tequilensis. In the light of the results of this study, we can suggest that the bioactive compound of Bacillus sp. Gn-A11-18 could become a biological alternate that could have an important role to fight against C. albicans and A. niger.

Synthesis of New Bis-pyrazolines Endowed with Potent Antifungal Activity against Candida albicans and Aspergillus niger

2020 ◽  
Vol 17 ◽  
Author(s):  
Belgin Sever ◽  
Mehlika Dilek Altıntop ◽  
Ahmet Özdemir
Keyword(s):  
Candida Albicans ◽  
Molecular Docking ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Mtt Assay ◽  
Active Site ◽  
Antifungal Agents ◽  
Docking Studies ◽  
Antifungal Effects ◽  
Nih 3T3

Background: Due to the increasing number of cases of invasive fungal infections (IFIs), there is an urgent need to identify potent antifungal agents capable of combating IFIs. Pyrazolines are one such class of therapeutically active agents that could be considered to fulfil this need. Objective: In this context, this paper aims to identify two new series of bis-pyrazolines endowed with potent antifungal activity against Candida albicans and Aspergillus niger. Methods: Two new series of bis-pyrazolines (4a-i, 5a-e) were synthesized through an efficient and and versatile synthetic procedure. The compounds were screened for their antifungal effects on C. albicans and A. niger using a broth microdilution method. Their cytotoxic effects on NIH/3T3 mouse embryonic fibroblast cell line were determined using MTT assay. Molecular docking studies were performed in the active site of lanosterol 14α-demethylase (CYP51) to shed light on their antifungal effects using Schrödinger’s Maestro molecular modeling package. Results And Discussion: 5,5'-(1,4-Phenylene)bis[1-(2-(5-phenyl-1,3,4-oxadiazol-2-yl)thio)acetyl)-3-(2-thienyl)-4,5- dihydro-1H-pyrazole] (4a) and 5,5'-(1,4-phenylene)bis[1-(2-(4-(2-hydroxyethyl)-1-piperazinylthiocarbamoyl)thio)acetyl)-3- (2-thienyl)-4,5-dihydro-1H-pyrazole] (5a) were found as the most promising antifungal agents in this series. Compounds 4a and 5a showed pronounced antifungal activity against C. albicans (MIC= 0.016 mg/mL) and A. niger (MIC= 0.008 mg/mL). Based on MTT assay, their antifungal effects were selective (IC50 > 0.500 mg/mL for NIH/3T3 cell line). Molecular docking studies suggested that compounds 5a-e might show their anticandidal effects via CYP51 inhibition in regard to their stronger interactions in the active site of CYP51. Conclusion: Compounds 4a and 5a stand out as potential antifungal agents for the management of IFIs caused by C. albicans and A. niger.

Anti-Fungal Activity of Cressa cretica, Leptadenia pyrotechnica and Pulicaria crispa, indigenous plants of Cholistan desert, Pakistan

2020 ◽  
Vol 18 ◽  
Author(s):  
Faheem Hadi ◽  
Tahir Maqbool ◽  
Sameera Khurshid ◽  
Aisha Nawaz ◽  
Saira Aftab ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Aspergillus Flavus ◽  
Fungal Infections ◽  
Fungal Species ◽  
Fungal Activity ◽  
Aspergillus Ustus ◽  
Mother Tincture ◽  
Anti Fungal

Background: Fungal infections have always remain a problem and they are getting worse with passage of each year due to their resistance against available antibiotics. Natural ways of treatment with homoeopathic medicines made of mother tinctures of plants have no reported side effects and have been proved effective against many bacterial and fungal infections. Materials & Methods: Preparation of mother tinctures of plants Cressa cretica, Leptadenia pyrotechnica and Pulicaria crispa was done and used to evaluate the anti-fungal potential of these plants against potentially pathogenic fungal species like Aspergillus niger, Aspergillus flavus, Aspergillus ustus and Candida albicans by agar disc diffusion method. Each tincture was evaluated at 0.25 ml, 0.5 ml and 1 ml volume per disc and zone of inhibition was measured in millimetres and compared with commercial drug Fluconazole (2 mg/ml) which was used as standard. Results: The results showed that satisfactory anti-fungal activity of these plants in comparison to standard drug Fluconazole. The ratio of antifungal activity of Cressa cretica measured as the zone of growth inhibition of these cultures against Aspergillus niger, Aspergillus flavus, Aspergillus ustus and Candida albicans was 24 mm / 27 mm, 30mm / 28 mm, 23 mm/ 30 mm and 32 mm/ 30 mm respectively. In the case of Leptadenia pyrotechnica, the mother tincture’s antifungal activity was 32 mm / 27 mm, 30 mm / 28 mm, 17 mm/ 30 mm and 24 mm/ 30 mm. In case of our third plant Pulicaria crispa, antifungal activity came out to be 23 mm/ 27 mm, 26 mm/ 28 mm, 26 mm / 30 mm and 24 mm/ 30 mm. Conclusion: Our study proved that mother tincture of these plants can be a potential new therapy to treat fungal infections and has the potential to rule out fungal problems. Further research using mother tincture of these plants against other fungal species has the potential to prove them a safer and widespread anti-fungal homoeopathic medicine.

Antifungal study of substituted 4-pyridylmethylene-4′-aniline Schiff bases

RSC Advances ◽  
2016 ◽  
Vol 6 (106) ◽  
pp. 104575-104581 ◽  
Author(s):  
P.-L. Lam ◽  
K. K.-H. Lee ◽  
S. H.-L. Kok ◽  
R. Gambari ◽  
K.-H. Lam ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Schiff Bases ◽  
Drug Candidates

Two substituted 4-pyridylmethylene-4′-aniline Schiff bases showed antifungal activity against.Aspergillus nigerandCandida albicans. They may be useful for the development of safe drug candidates forA. nigerandC. albicanscases of otomycosis.

scholarly journals Novel Antifungal Dimers from the Roots of Taiwania cryptomerioides

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 437
Author(s):  
Ming-Jen Cheng ◽  
Ming-Der Wu ◽  
Chao-Lin Chang ◽  
Hsun-Shuo Chang ◽  
Chiou-Fung Chyu ◽  
...  
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Spectroscopic Analysis ◽  
Methanol Extract ◽  
Penicillium Italicum ◽  
Antifungal Activities ◽  
Nmr Data ◽  
Taiwania Cryptomerioides

Five new dimer compounds, namely Taiwaniacryptodimers A‒E (1–5), were isolated from the methanol extract of the roots of Taiwania cryptomerioides. Their structures were established by mean of spectroscopic analysis and comparison of NMR data with those of known analogues. Their antifungal activities were also evaluated. Our results indicated that metabolites 1, 2, 4, and 5 displayed moderate antifungal activities against Aspergillus niger, Penicillium italicum, Candida albicans, and Saccharomyces cerevisiae.

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