scholarly journals Synthesis, Characterization of Some New 1,3,5-Trisubstituted Pyrazole Derivatives for Their Antifungal Potential

2021 ◽  
pp. 211-223
Author(s):  
Anupam Sharma ◽  
Alok Pal Jain ◽  
Mayank Gangwar
Keyword(s):  
Saccharomyces Cerevisiae ◽  
Antifungal Activity ◽  
Diffusion Method ◽  
Moderate Activity ◽  
Activity Data ◽  
Mass Spectral ◽  
Fungal Strains ◽  
The Third ◽  
Antifungal Action

The aim of the study was to develop, synthesis, and characterise a novel 1,3,5-trisubstituted-2-pyrazolines derivative, as well as to evaluate its antifungal activity. The reaction of chalcone derivatives with succinic hydrazide in the presence of pyridine yielded the 1,3,5-tri-substituted-2-pyrazolines derivatives. Total 20 compounds has been synthesized and characterized by the IR, 1HNMR and mass spectral analysis. Antifungal activity of the compounds carried out onfour fungal strains i.e. Saccharomyces cerevisiae, A. Niger, C. Albicans and R. Oryzae in two different concentration i.e. 50 and 100 µg/ml by Agar-diffusion method using Cup-plate method. The usual antifungal medicine was ketoconazole. All of the synthesized 1,3,5-trisubstituted pyrazole compounds (ME1-ME8, CL1-CL8, BR1-BR4) showed medium to best action against examined organisms, according to antifungal activity data. The antifungal activity of compounds against fungal strains (Saccharomyces cerevisiae, A. Niger, Candida albicans, and R. Oryzae) revealed the following order of action: CL-4 > BR-4 > CL-3 > CL-2 > ME-3> ME-2> CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8>ME-8 >CL-1 >ME-1 > CL-5 > CL-6 > ME-4 > ME-5 > ME-6 > ME-7 > CL-7 > CL-8>ME-8 >CL-1 >ME-1. Electronegative groups (Br, Cl, F, and NO2) must be present at the third and fifth positions of the 1,3,5-pyrazoline ring for significant antifungal action. The presence of an electronegative group at the third and fifth positions may be required for the best action against bacterial and fungal strains, however the addition of F, NO2 has demonstrated moderate activity, while the substitution of methyl and methoxy  groups may reduce the activity. The synthesized compounds in the BR-1 through BR-4 class are the most active.

Synthesis and Biological Activity of 3-(substitutedphenyl)-6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine: Part II

2020 ◽  
Vol 18 ◽  
Author(s):  
Niranjan Kaushik ◽  
Nitin Kumar ◽  
Anoop Kumar ◽  
Vikas Sharma
Keyword(s):  
Antifungal Activity ◽  
Opportunistic Infections ◽  
Fungal Infections ◽  
Mass Spectral Data ◽  
Triazole Derivatives ◽  
Mass Spectral ◽  
Fungal Strains ◽  
Antifungal Properties ◽  
Antifungal Potential ◽  
Spectral Data Analysis

Background: Fungal infections are opportunistic infections that become a serious problem to human health. Objective: Considering the antifungal potential of triazole nucleus, the study was carried out with the objective to synthesize some novel triazole derivatives with antifungal potential. Method: 1,2,4-triazole derivatives were synthesized via a two step reaction (reported earlier). The first step involves reaction of substituted benzoic acid with thiocarbohydrazide to form 4-amino-3-(substituted phenyl)-5-mercapto-1, 2, 4-triazole derivatives (1a-1k) while in second step, synthesized compounds (1a-1k) were then subsequently treated with substituted acetophenone to yield substituted (4-methoxyphenyl-7H-[1, 2, 4] triazolo [3, 4-b][1,3,4] thiadiazine derivatives (2a-2k). All synthesized compounds were characterized by IR, 1H NMR, and Mass spectral data analysis and were screened for their antifungal properties against different fungal strains i.e. Candida tropicalis (ATCC-13803, ATCC-20913), Candida albicans (ATCC-60193), Candida inconspicua (ATCC-16783) and Candida glabrata (ATCC-90030, ATCC-2001). Results: Compound 2d displayed better percentage inhibition (26.29%, 24.81%) than fluconazole (24.44%, 22.96%) against ATCC-16783, ATCC-2001 fungal strains respectively at 100µg/ml. Compound 2f also displayed better percentage inhibition (28.51%) against ATCC-90030 as compared to fluconazone (27.4%) at 200 µg/ml. Similarly, compounds 2e and 2j also exhibited better antifungal properties than fluconazole at 200µg/ml. Compound 2e was found most potent against ATCC13803 (30.37%) and ATCC-90030 (30.37%) fungal strains as compared to fluconazole (28.14%, 27.4%) at 200 µg/ml respectively whereas compound 2j exhibited better antifungal activity (28.51%) against ATCC-60193 than fluconazole (27.7%) at 200 µg/ml. Conclusion: The results were in accordance with our assertions for triazole derivatives, as all compounds displayed moderate to good antifungal activity.

scholarly journals Synthesis, Spectral Characterization, and Antibacterial and Antifungal Studies of PANI/V2O5Nanocomposites

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Chakradhar Sridhar ◽  
Nagesh Gunvanthrao Yernale ◽  
M. V. N. Ambika Prasad
Keyword(s):  
Antifungal Activity ◽  
Sol Gel ◽  
Chemical Oxidation ◽  
Diffusion Method ◽  
Antibacterial And Antifungal Activity ◽  
X Ray Diffraction ◽  
Xrd Techniques ◽  
Antibacterial And Antifungal

The present study deals with the synthesis and characterization of nanocrystalline vanadium pentoxide (V2O5) nanoparticles and their antibacterial and antifungal activity onStaphylococcus aureus and Aspergillus niger, respectively, by agar diffusion method. The metal oxide has been synthesized by employing the sol-gel method, polyaniline (PANI) has been synthesized by chemical oxidation, and PANI/V2O5composites have been synthesized byin situpolymerization method with different ratios (10, 20, 30, 40, and 50 weight%) of V2O5in PANI. The newly prepared composites were characterized by FTIR and powder X-ray diffraction (P-XRD) techniques and are found to be formed of PANI/V2O5nanocomposites, and also the compounds showed moderate antibacterial and antifungal activity.

scholarly journals Antimicrobial Activity and Characterization of Pomegranate Peel-Based Carbon Dots

2021 ◽  
Vol 2021 ◽  
pp. 1-6
Author(s):  
Waseem Akhtar Qureshi ◽  
B. Vivekanandan ◽  
J. Altrin Jayaprasath ◽  
Daoud Ali ◽  
Saud Alarifi ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Carbon Dots ◽  
Diffusion Method ◽  
Moderate Activity ◽  
E Coli ◽  
Analytical Instruments ◽  
Antimicrobial Efficiency ◽  
Microbial Efficiency ◽  
Ft Ir

This investigation reports the use of agrowaste pomegranate peels as an economical source for the production of fluorescent carbon dots (C-dots) and their potential application as an antimicrobial agent. The carbon dots were prepared through low-temperature carbonization at 200°C for 120 min. The obtained C-dots were found to be small in size and exhibited blue luminescence at 350 nm. Further, the synthesized C-dots were characterized with the help of analytical instruments such as DLS, UV-visible, FT-IR, TEM, and fluorescence spectrophotometer. Antimicrobial activity of the C-dot PP was estimated by the agar diffusion method and MIC. S. aureus and K. pneumoniae are showing susceptibility towards C-dot PP when compared to the standard and showing a moderate activity against P. aeruginosa and resistance towards E. coli. The obtained C dot PPs were found to be around 5-9 nm in size confirmed from DLS analysis and supported by TEM. The synthesized C-dots were investigated to understand their microbial efficiency against pathogens and found to have antimicrobial efficiency. These results suggest that pomegranate peels are a potential source of carbon dots with antimicrobial efficiency.

scholarly journals ANTIFUNGAL ACTIVITY OF PANCHAWALKALA KWATHA AND PANCHAWALKALA SHATADAUTA GHRITA

2021 ◽  
pp. 40-45
Author(s):  
Wadimuna Mudiyanselage Dharmasenage Ruvinika Wirajani Wadimuna ◽  
Gunarathnage Upul Anuruddha Kumara ◽  
W. L. A. Rajini Saroja Pushpakumari
Keyword(s):  
Antifungal Activity ◽  
Agar Plate ◽  
Diffusion Method ◽  
Distilled Water ◽  
Standard Drug ◽  
Antifungal Effect ◽  
Antifungal Action ◽  
Therapeutic Properties ◽  
In Vitro Antifungal Activity

Panchawalkala is one of the ideal herbal combinations in Ayurveda and it has therapeutic properties such as Vranaropana, Shothahara, Graahi and Visarpahara. And also researchers have been proven anthelmintic, antimicrobial, wound healing and anti-inflammatory activities of these plants in combination and individual too. Ghrita (Ghee) is one of the oil preparation made by cow’s milk and it has Balavardhaka, Ojovardhaka, Vayasthapaka, Dhatuposhaka properties and is supreme in Snehana Dravyas. Panchawalkala is widely used in Kwatha and Powder form. Shatadauta Ghrita is the most famous form of the Ghee. The advantages of different innovative preparations are; increased shelf life, ready to use, better acceptability and ease of application. This study was planned to evaluate in-vitro antifungal activity of traditional Panchawalkala Kwatha and innovative Panchawalkala Shatadauta Ghrita (the Ghrita, hundreds times purified by Panchawalkala Kwatha). It was assessed by adopting agar diffusion method. Each agar plate was divided into four equal parts and was cultivated the Candida albicans. Replicator device was used to inoculate multiple specimens on to two parts of three series of plates with respective drugs. Further, responses of organism to the trial drugs were measured and compared with standard drug of Fluconazole (+ve control) and distilled water (-ve control) by using other two parts of the agar plates. All the plates were incubated at 37°C for 24 hours. According to the findings, Panchawalkala Shatadauta Ghrita has an antifungal effect than Panchawalkala Kwatha. Fluconazole is the best antifungal drug among these and distilled water does not have any antifungal action. Hence, it can be concluded that, Panchawalkala Shatadauta Ghrita has antifungal activity rather than Panchawalkala Kwatha but not effective than Fluconazole.    

Design, Synthesis, Docking and Computational Pharmacokinetic Profiling of New Pyrazolinyl Thiazolinone Biheterocycles as Potent Antimicrobial Agents

2020 ◽  
Vol 17 (11) ◽  
pp. 1342-1354
Author(s):  
Vinutha Vittala Salian ◽  
Badiadka Narayana ◽  
Balladka Kunhanna Sarojini ◽  
Sharath Chandra Kodandoor ◽  
Anupam Glorious Lobo
Keyword(s):  
Antifungal Activity ◽  
Active Sites ◽  
Antimicrobial Agents ◽  
Building Blocks ◽  
Diffusion Method ◽  
Dilution Method ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Reference Drug ◽  
Fungal Strains

Background: Development of potential antimicrobial agents is the main aim in the drug discovery process to overcome the problem of drug resistance. Pyrazolines and thiazolinones are extensively used as building blocks for the synthesis of diverse and medicinally important compounds. Methods: In this present work, a new series of functionalized pyrazolinyl-thiazolinone biheterocycles is designed and synthesized from N-pyrazolinecarbothioamide. Antimicrobial screening is carried out in order to discover their potential towards six bacterial and four fungal strains. The zone of inhibition (ZI in mm) was determined by the disc diffusion method and minimum inhibitory concentration (MIC in μg/mL) by macro dilution method. The druggability of these new entities is done through in silico pharmacokinetic profiling using Maestro 2017-1 interface of Schrӧdinger software. Results and Disscusion: Compounds 4c and 4e with chloro and iodo substituents on Nphenylacetamide ring displayed good inhibitory antibacterial activity against the tested bacterial strains with minimum MIC values when compared to the reference drug tetracycline. Compound 3 with an acetic acid derivative showed high antifungal activity among all the tested derivatives. Compound 3 not only showed antifungal activity but also qualified druggability test with no violation of Lipinski rule of five. Conclusion: The capability of the synthesized pyrazolinyl-thiazolinone derivatives was performed to efficiently inhibit the growth of microorganisms against selected bacterial and fungal strains. Further, these compounds are found to be effectively bound to the active sites of attractive target Escherichia coli FabH.

scholarly journals Identification of the Chemical Constituents of the Selected Fraction of the Dichloromethane Extract of Syzygium samarangense Stem Bark Using LC-ESI-MS and Evaluation Its Potential as Antifungal Agent

2021 ◽  
Vol 21 (2) ◽  
pp. 340
Author(s):  
Tukiran Tukiran ◽  
Suyatno Suyatno ◽  
Frisca Nadya Safitri
Keyword(s):  
Antifungal Activity ◽  
Skin Diseases ◽  
Chemical Constituents ◽  
Stem Bark ◽  
Chemical Constituent ◽  
Negative Control ◽  
Diffusion Method ◽  
Moderate Activity ◽  
Disk Diffusion Method ◽  
Esi Ms

Several extracts of Syzygium species have been shown to inhibit the growth of some fungal microorganisms implicated in skin diseases, such as Candida albicans included S. samarangense. However, an antifungal test of C. Albicans on this plant's stem bark had not been reported. This study aimed to identify chemical constituents of the selected fraction from dichloromethane extracts of the stem bark of S. samarangense and determine the antifungal activity of the selected fraction at various concentrations on C. Albicans. The identification of the chemical constituent of the selected fraction has been performed by the LC-ESI-MS technique. An antifungal test of the selected fraction was carried out using the disk diffusion method. The samples used included the selected fraction with 5 variations of concentration (2.5; 2.0; 1.5; 1.0; and 0.5%), positive control (ketoconazole 1%), and negative control (DMSO). The results showed that the selected fraction has antifungal activity on C. Albicans. The results showed that the selected fraction contains four flavonoids: pinocembrin, uvangoletin, stercurensin, and aurentiacin. Due to antifungal activity on C. Albicans, it has moderate activity at a concentration of 2.5%, while concentrations of 2.0, 1.5, 1.0, and 0.5% have weak activity.

scholarly journals Evaluation of Antifungal Activity of Various Plant Latex against Selected Fungal Strains

2021 ◽  
Vol 9 (10) ◽  
pp. 875-883
Author(s):  
Mubashira Begum
Keyword(s):  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Aspergillus Flavus ◽  
Trichoderma Viride ◽  
Aloe Vera ◽  
Diffusion Method ◽  
Calotropis Procera ◽  
Calotropis Gigantea ◽  
Fungal Strains ◽  
Plumeria Rubra

Abstract: Latex is a natural plant polymer and milky white fluid distributed throughout the plant body like leaves, stems, roots and fruits of all flowering plants and consists of proteins, alkaloids, starches, sugars, oils, tannins, resins and gums that coagulate on-air exposure. It is secreted by specialized plant cells called Laticifers. Plants exude latex in response to physical damage. The present study was carried out to assess the potential antifungal activity of latex of five different plants namely Plumeria rubra, Plumeria alba, Aloe vera, Calotropis procera and Calotropis gigantea against three different pathogenic strains of fungi. All five latexes were found to show good to moderated activity against all the three fungal strains, namely Trichoderma viride, Aspergillus flavus and Aspergillus niger. The latex of each plant was tested in two volumes (i.e. 10µl & 20µl), and it was found that the antifungal activity was volume-dependent, and a significant difference was also observed in the case of different fungal strains. The antifungal activity of plant latexes was evaluated by Agar well diffusion method; results revealed that among all the five latexes, the fresh latex of Plumeria rubra (Vol: 10µl &20µl) showed excellent antifungal activity against Aspergillus niger and Aspergillus flavus, whereas fresh latex of Aloe vera (Vol: 10µl & 20µl) showed excellent antifungal activity against Trichoderma viride. The results of the current research imply that the antifungal activity of latex varies with the species of plants and the fungal strains used. The results therefore demonstrated that, the used five latexes effectively inhibited the growth of three tested fungi. Hence, these plant latexes are natural, ecofriendly and can be used as good candidates for the treatment of various fungal diseases. In further words, they can be used for therapy of antifungal-resistant fungi. Keywords: Antifungal activity, Proteins, Alkaloids, Tannins, Resins, Laticifers, Plumeria rubra, Plumeria alba, Aloe vera, Calotropis procera, Calotropis gigantea, Aspergillus flavus, Aspergillus niger, Trichoderma viride, Latex, Agar well diffusion.

Highly Regioselective Ring-Opening of Epoxides: Synthesis and Biological Evaluation as Potent Antimicrobial Agents

2021 ◽  
Vol 6 (3) ◽  
pp. 228-234
Author(s):  
Nilam H. Lalavani ◽  
Krishna A. Bhensdadia ◽  
Shipra H. Baluja
Keyword(s):  
Ring Opening ◽  
Antimicrobial Agents ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Mass Spectral ◽  
Fungal Strains ◽  
Ring Opening Of Epoxides

In present work, a convenient method for the nucleophilic ring-opening of epoxides with secondary amine in presence of ethyl acetate as a polar aprotic solvent using catalytic amount of base is described. Present method is highly regioselective and furnishes the products in short time of period with excellent yield. The regioselectivity of this ring opening was confirmed using FT-IR, 1H NMR, 13C NMR, elemental analysis and mass spectral data. The antimicrobial screening of all these synthesized compounds was done against some bacterial and fungal strains in two polar solvents, DMSO and DMF using agar well diffusion method. These compounds showed good inhibition of bacterial strains and potent against fungal strains than standard drug.

Sign in / Sign up

Export Citation Format

Share Document