scholarly journals Synthesis and Antimicrobial Activities of N-(Heteroaryl-substituted)-p-toluenesulphonamides

2014 ◽  
Vol 2014 ◽  
pp. 1-5
Author(s):  
Ozoh Chinwe Francisca ◽  
Okoro Uchechukwu Chris ◽  
Ugwu David Izuchukwu
Keyword(s):  
Biological Activities ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
New Class ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
C Nmr

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

scholarly journals In VitroAntimicrobial Activity of Essential Oil ofThymus schimperi,Matricaria chamomilla,Eucalyptus globulus, andRosmarinus officinalis

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Awol Mekonnen ◽  
Berhanu Yitayew ◽  
Alemnesh Tesema ◽  
Solomon Taddese
Keyword(s):  
Antimicrobial Activity ◽  
Minimum Inhibitory Concentration ◽  
Essential Oil ◽  
Essential Oils ◽  
Inhibitory Concentration ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Drug Preparation ◽  
Bacteria And Fungi

In this study, thein vitroantimicrobial activities of four plant essential oils (T. schimperi,E. globulus,R. officinalis, andM. Chamomilla) were evaluated against bacteria and fungi. The studies were carried out using agar diffusion method for screening the most effective essential oils and agar dilution to determine minimum inhibitory concentration of the essential oils. Results of this study revealed that essential oils ofT. schimperi,E. globulus, andR. officinaliswere active against bacteria and some fungi. The antimicrobial effect ofM. chamomillawas found to be weaker and did not show any antimicrobial activity. The minimum inhibitory concentration values ofT. schimperiwere<15.75 mg/mL for most of the bacteria and fungi used in this study. The minimum inhibitory concentration values of the other essential oils were in the range of 15.75–36.33 mg/mL against tested bacteria. This study highlighted the antimicrobial activity of the essential oil ofE. globulus,M. chamomilla,T. Schimperi, andR. officinalis. The results indicated thatT. schimperihave shown strong antimicrobial activity which could be potential candidates for preparation of antimicrobial drug preparation.

scholarly journals Synthesis and Pharmacological Evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

2020 ◽  
Vol 10 (5) ◽  
pp. 274-292
Author(s):  
Rohit Kumar ◽  
Sushil Kumar ◽  
Mohammad Asif Khan
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Biological Activities ◽  
Diffusion Method ◽  
Gram Positive ◽  
Standard Drug ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Pharmacological Evaluation

Recently a series of Schiff bases of diphenylamine derivatives have been synthesized and evaluated in vitro for their antibacterial activity against pathogenic both Gram-positive bacteria B. subtitles and Gram-negative bacteria E. coli using ciprofloxacin as standard drug at conc. of 50 μg/ml and 100 μg/ml. Literature review revels that chalcones possesses various biological activities like antimicrobial, antiviral, anti-inflammatory, anticancer and sedative etc. Therefore the present study was designed on synthesis and pharmacological evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides. Target compound was synthesized by reaction of chloroacetylchloride with diphenylamine to afford 2-chloro-N, N-diphenylacetamide which further by reaction with substituted Chalcones and characterized following recrystallization and evaluated for anti-microbial potential through cup-diffusion method. In results, the target compounds were tested for activity against B. Subtilis, E.Coli and C. albicans. The chalcones having the lipophilic 4-chloro group (RKCT2) showed the greatest antimicrobial activity (zone of inhibition 20 & 22 mm against. B. subtilis, E. Coli, C. Albicans respectively. It suggests further researchers to go through anti-microbial evaluations against a more varieties of bacteria and fungi. Keywords: Schiff bases of diphenylamine derivatives, antibacterial activity, Gram-positive bacteria, 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

scholarly journals Evaluation Laboratory Produced Biosurfactant by Rhodotorula Species and Its Antifungal Activity

2019 ◽  
Author(s):  
Maral Gharaghani ◽  
Marzieh Halvaeezadeh ◽  
Ali Zarei Mahmoudabadi
Keyword(s):  
Antifungal Activity ◽  
Antimicrobial Activities ◽  
Biosurfactant Production ◽  
Diffusion Method ◽  
Disk Diffusion Method ◽  
Low Toxicity ◽  
Rhodotorula Species ◽  
Bacteria And Fungi ◽  
Different Strains

Background: Biosurfactants are amphiphilic surface active compounds that produced by several microorganisms, including, bacteria and fungi. Biodegradability, low toxicity, applications diversity and functionality under extreme conditions are characterized them from chemically biosurfactants. It is found that, Rhodotorula species, read yeasts, have high potency for biosurfactant producing. Recently, antimicrobial activities of biosurfactants have been subjected for new antibiotic therapy. The aim of the present study was to evaluate biosurfactant production by the different strains of Rhodotorula species in laboratory conditions. In addition, antifungal activity of produced biosurfactant was assessed against several saprophytic fungi. In the present study 54 strains of Rhodotorula including, R. glutinis (48 strains), R. minuta (2 strains), R. mucilaginosa (2 strains) and Rhodotorula species (2 strains) were screened for biosurfactant production. The biosurfactant was produced using the Sabouraud dextrose broth medium and confirmed by specific tests. Antifungal assay was also evaluated by disk diffusion method and the serial dilutions of biosurfactant. In the present study, although all tested strains were capable to produce biosurfactant in vitro, the degree of biosurfactant production was varied among stains. 7.4% strains had the highest (+5) biosurfactant activity followed by 16.7%, 29.5%, 25.8% and 20.4% had +4, +3, +2 and +1, respectively. In the present study, all tested fungi were inhibited at 40 &micro;l of biosurfactant. Rhodotorula species are appropriate organisms for the production of biosurfactants and R. glutinis strains have the greatest ability to producing biosurfactant than another species. Furthermore, our results were demonstrated that the produced biosurfactant by R. glutinis presented a valuable potential for biopharmaceutical applications.

Synthesis and in vitro antimicrobial activity of new 3-(2-morpholinoquinolin-3-yl) substituted acrylonitrile and propanenitrile derivatives

2011 ◽  
Vol 65 (5) ◽  
Author(s):  
Jigar Makawana ◽  
Manish Patel ◽  
Ranjan Patel
Keyword(s):  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Double Bond ◽  
Fungal Pathogen ◽  
Condensation Reaction ◽  
Clostridium Tetani ◽  
Gram Positive Bacteria ◽  
Bacteria And Fungi

AbstractA series of new 3-(2-morpholinoquinolin-3-yl)acrylonitrile derivatives (IVa-IVf) has been synthesised by the base-catalysed condensation reaction of 2-morpholinoqionoline-3-carboxaldehydes (IIa-IIc) and 2-cyanomethylbenzimidazoles (IIIa-IIIb). Subsequent regiospecific reduction of the C—C double bond in acrylonitrile moiety afforded 3-(2-morpholinoquinolin-3-yl)propanenitrile derivatives (Va-Vf). All the compounds synthesised were subjected to in vitro antimicrobial screening against some representatives of bacteria and fungi. The majority of the compounds were found to be active against Gram-positive bacteria Bacillus subtilis and Clostridium tetani as well as against the fungal pathogen Candida albicans.

scholarly journals Solidago graminifolia L. Salisb. (Asteraceae) as a Valuable Source of Bioactive Polyphenols: HPLC Profile, In Vitro Antioxidant and Antimicrobial Potential

Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2666 ◽  
Author(s):  
Anca Toiu ◽  
Laurian Vlase ◽  
Dan Cristian Vodnar ◽  
Ana-Maria Gheldiu ◽  
Ilioara Oniga
Keyword(s):  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Biological Properties ◽  
Total Phenolic ◽  
Antimicrobial Potential ◽  
Aerial Parts ◽  
Hplc Profile ◽  
Antibacterial And Antifungal

Solidago species are often used in traditional medicine as anti-inflammatory, diuretic, wound-healing and antimicrobial agents. Still, the bioactive compounds and biological activities of some species have not been studied. The present work aimed to investigate the polyphenolic profile and the biological properties of Solidago graminifolia L. Salisb., a poorly explored medicinal plant. The hydroalcoholic extracts from aerial parts were evaluated for total phenolic content (TPC), total flavonoid content (TFC) and the polyphenolic compounds were investigated by HPLC-MS. The antioxidant potential in vitro was determined using DPPH and FRAP assays. Antibacterial and antifungal effects were evaluated by dilution assays and MIC, MBC and MFC were calculated. The results showed that Solidago graminifolia aerial parts contain an important amount of total phenolics (192.69 mg GAE/g) and flavonoids (151.41 mg RE/g), with chlorogenic acid and quercitrin as major constituents. The hydroalcoholic extracts showed promising antioxidant and antimicrobial potential, with potent antibacterial activity against Staphylococcus aureus and important antifungal effect against Candida albicans and C. parapsilosis. The obtained results indicated that the aerial parts of Solidago graminifolia could be used as novel resource of phytochemicals in herbal preparations with antioxidant and antimicrobial activities.

scholarly journals Synthesis of disulphide-Schiff base derivatives and investigations of in vitro antimicrobial activities against some human pathogens

2017 ◽  
Vol 1 (3) ◽  
pp. 230-234 ◽  
Author(s):  
Sefa Durmuş ◽  
Aslıhan Dalmaz ◽  
Görkem Dülger ◽  
Duygu Bircan Kadıoğlu
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Control Group ◽  
Human Pathogens ◽  
Antibacterial And Antifungal Activities ◽  
Schiff Base Derivatives ◽  
Antibacterial And Antifungal

Abstract Thio-Schiff bases are becoming increasingly widespread in various branches such as the preparation of certain medicines, cosmetic products, and polymer production. In particular, the presence of antibacterial, antifungal, antiviral, antitumor and antimalarial properties of Schiff bases containing sulfur in the structure has made these compounds attractive in different disciplines. In this study, different derivatives of dimeric disulfide-Schiff bases have been synthesized. The antibacterial and antifungal activities of the synthesized these compounds were investigated in vitro against some human pathogens (Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and Candida albicans, C. tropicalis, C. guilliermondii and C. glabrata). Test microorganisms were isolated from the patients appyling to Medical Faculty Hospital of Duzce University were used. Diffusion method was used to determine the antimicrobial activities of the compounds.standard antibacterial (Cefotaxime, Amoxicillin/clavulanicacid) and antifungal (Posaconazole) antibiotics were used as the control group and the results were compared. The result indicated that antimicrobial activity of Disulphide-Schiff Base Derivatives exhibited less activity against bacteria as compared to AMC30 (Amoxicillin/clavulanicacid), but highly effective against bacteria as compared to CTX30 (Cefotaxime). In addition, the compounds exhibited less activity against yeast.

scholarly journals Synthesis andIn VitroBiological Evaluation of Aminonaphthoquinones and Benzo[b]phenazine-6,11-dione Derivatives as Potential Antibacterial and Antifungal Compounds

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Amaç Fatih Tuyun ◽  
Nilüfer Bayrak ◽  
Hatice Yıldırım ◽  
Nihal Onul ◽  
Emel Mataraci Kara ◽  
...  
Keyword(s):  
Spectral Properties ◽  
Antifungal Compounds ◽  
New Members ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Aryl Amines ◽  
Antibacterial And Antifungal ◽  
C Nmr

A series of 2-arylamino-3-chloro-1,4-naphthoquinone derivatives (3a–h) by the reaction of 2,3-dichloro-1,4-naphthoquinone with aryl amines (2a–h) and benzo[b]phenazine-6,11-dione derivatives (4a–c) by the treatment of 2-arylamino-3-chloro-1,4-naphthoquinone derivatives (3a–h) with sodium azide were synthesized and tested for theirin vitroantibacterial and antifungal activities. The results suggest that compounds3dand3ghad potent antifungal activity againstCandida albicans(MIC = 78.12 μg/mL). All synthesized compounds (3a–h,4a–c) possessed activity againstE. faecaliswith MIC values of between 312.5 and 1250 μg/mL. Benzo[b]phenazine-6,11-dione derivatives (4a–c) were mostly active against Gram-positive bacteria. The structures of the new members of the series were established on the basis of their spectral properties (IR,1H NMR,13C NMR, and mass spectrometry).

scholarly journals Chemical composition and biological activities of essential oils of endemic Thymus leucostomus Hausskn. et Velen

2020 ◽  
Vol 49 (4) ◽  
pp. 957-965
Author(s):  
Omer Elkiran ◽  
Cumhur Avsar
Keyword(s):  
Antioxidant Activity ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Antimicrobial Activities ◽  
Gram Positive Bacteria ◽  
In Vitro Antioxidant Activity

The chemical composition, antimicrobial and antioxidant properties of the essential oils from the leaves of endemic Thymus leucostomus naturally grown in Turkey were investigated and chemical differences were discussed by means of chemotaxonomy. Twenty-six components were identified representing 98.8% of the oils. The main compounds in the essential oil of T. leucostomus were: o-cymene (30.6%), carvacrol (9.6%), thymol methyl ether (7.2%), limonene (6.8%). Essential oil was screened for their antimicrobial activities against 7 bacteria and 2 yeast species by using disc-diffusion and MIC procedure. The essential oil showed higher effectiveness against all the tested bacteria and yeast. The extract was observed to be much more effective in Gram-positive bacteria (especially, S. aureus ATCC 6538). In vitro antioxidant activity based on the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical was evaluated for the essential oil, and it was found that the essential oil had good antioxidant activity in the range of the IC50= 5.42 ±0.8 μg/ml.

New Insights Towards 1,4-Benzodiazepines from Curcumin. Design, Synthesis and Antimicrobial Activities

2020 ◽  
Vol 16 (8) ◽  
pp. 1112-1123
Author(s):  
Othman Hamed ◽  
Oswa Fares ◽  
Shaima Taleeb ◽  
Ghaleb Adwan ◽  
Haythem Saadeh ◽  
...  
Keyword(s):  
Biological Activities ◽  
Antimicrobial Activities ◽  
High Potency ◽  
Step Method ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria

Background: Curcumin is a safe, versatile natural product with unlimited number of biological activities and a precursor for various heterocyclic compounds. Objective: The present study was aimed to the development of a curcumin based antimicrobial reagent with high potency against gram-positive and gram-negative bacteria. Methods: Herein we report a simple and convenient one step method for synthesizing a series of 1,4-benzodiazepines via condensation cyclization reaction between curcumin and various 1,2- phenylenediamine in refluxed ethanol. Results: A series of new 1,4-benzodiazepins were synthesized and their structures were supported by FT-IR, 1H NMR, 13C NMR, and mass spectral analysis. Synthesized 1,4-benzodiazepins were evaluated for their in vitro antimicrobial activity against gram positive (S. aureus and S. epidermidis) and gram negative (E. coli and P. aeruginosa) bacteria. They exhibited low to high potency against the tested organisms. In particular, dichlorinated 1,4-benzodiazepine 9 exhibited a remarkable potency against the gram-positive bacteria S. aureus (MIC: 3.125 μg mL-1, MBC: 12 μg mL-1). It showed a higher potency than most of the tested reference drugs. Compound 9 showed the medium activity against E. coli. Genotoxic study revealed that, benzodiazepines 9 attacked the DNA of E. coli strains and damaged it. The potency of compound 9, could be attributed to the multiple chlorine atoms present on the aromatic ring. Conclusion: Some of the synthesized curcumin based benzodiazepines showed excellent potency against gram positive bacteria. These benzodiazepines could be a great candidate as a future antimicrobial agent.

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