scholarly journals Synthesis of some novel 1H-indole derivatives with antibacterial activity and antifungal activity

2020 ◽  
Vol 9 (2) ◽  
pp. 961-967 ◽  

The present research works a series of new 1H-Indole derivatives were synthesized. The title compound was obtained by the reaction of indole with chloroacetylchloride in toluene afforded 2-chloro-1-(indoline-1-yl) ethanone which reacts with 1,4 diamine benzene in chloroform afforded 2-((4-aminophenyl)amino)-1-(1H-indol-1-yl)ethan-1-one, on further reaction with various acetophenone in presence of acetic acid in ethanol gave various final derivatives. After synthesis of compounds, the synthesized compounds were characterized by their IR, 1HNMR spectral data and elemental analysis. These derivatives were screened for their antimicrobial activity (Paper-disk-plate technique (disc diffusion method) and Tube-dilution technique (broth microdilution technique), antifungal activity of all synthesized compounds were evaluated against Aspergillus niger and Candida albicans (ATCC 10231) using Fluconazole as the standard drug using the paper plate method and antibacterial activity against both Gram-positive (Bacillus subtilis) and Gram-negative bacteria (Escherichia coli) using Ampicillin as standard medication at a concentration of 50g/ml, 100g/ml. The collected compounds were evaluated for antibacterial activity and antifungal activity. All compounds exhibit significant antimicrobial activity.

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.


Author(s):  
Dhanapal Venkatachalam ◽  
Akhib Rahman ◽  
Basil Sunny ◽  
Jensy Jacob ◽  
Nikhil Kuriyan ◽  
...  

Objective: The present study was designed to check in-vitro efficacy of Antibacterial and antifungal activity of aqueous and hexane extracts of stem of Justicia gendarussa against selected bacterial and fungal strains. Justicia gendarussa, belonging to the family Acanthaceae, commonly known as ‘‘vatham kolli’ was used in treatment of bronchitis, inflammation, eye diseases, ear ache, vaginal discharges, rheumatism, dysentery, eczema and jaundice. Methodology: Hexane and aqueous extracts of Justicia gendarussa was used for antimicrobial screening. Antibacterial activity was tested against pathogenic bacterial strains Eschericha coli and Staphylococcus aureus. Also antifungal activity was tested against one human pathogenic fungal strain i.e. Candida albicans. Antibacterial and antifungal activities of Justicia gendarussa extract was carried out by using disc diffusion method. Results: Aqueous extract of Justicia gendarussa showed the largest zone of inhibition (5mm) against Eschericha coli, at 50µgm/ml and 3mmzone of inhibition against S. aures, at 50µgm/ml. Hexane extract does not   showing activity against to human pathogenic E. coli and S. aures, at 50µgm/ml. Aqueous extract has shown more potent antibacterial activity against Eschericha coli. Aqueous extract was found to be more effective against human pathogenic fungus Candida albicuns than hexane extract and standard drug. The zone of inhibition of Aqueous extract was 11mm and the zone of inhibition of hexane extract was7mm and standard only 2mm.The phytochemical screening demonstrated the presence of different types of compounds like terpenoids, tannins, and flavonoids which may contribute for the anti-microbial action of this plant. Conclusions: These findings provide scientific evidence of traditional use of Justicia gendarussa and also indicate the potential of this plant for the development of antimicrobial agents.


Author(s):  
SIREESHA KALVA ◽  
RAGHUNANDAN N.

Objective: To estimate the antimicrobial activity of methanolic extract of Adenium obesum (family Apocyanaceae) in association with phytochemical analysis. Methods: The methanolic extract of the flowers of Adenium obesum was prepared and investigated for phytochemical constituents using standard methods. Antimicrobial activity of methanolic extract Adenium obesum has been carried out against one gram-positive bacteria Staphylococcus aureus and one gram-negative bacteria Escherichia coli and the antifungal activity of the plant extract was evaluated on Candida albicans species. The testing was done by the disc diffusion method to visualize the zone of inhibition of methanolic extract was compared with that of standard drug i.e., Ciprofloxacin for antibacterial activity and Fluconazole for antifungal activity. The minimum inhibition concentration was determined by micro dilution method (cup-plate method). Results: The present investigation shows the phytochemical analysis confirmed the presence of alkaloids, saponin glycosides, flavonoids, phenols, proteins and amino acids, cardiac glycosides, steroids, tannin, and phenolic compounds. The anti-microbial activity of the methanolic extract of the plant showed significant results against all the three of the test organisms in compare to the standard drugs. Conclusion: The present study concluded that methanolic extract of the flowers of adenium obesum proved the existence of phytochemical constituents. The methanolic extract of the was found to possess promising antimicrobial activity when compared with the standards and it can be useful for the development of antibiotics.


Author(s):  
Bindhu R. Kamath ◽  
Sabeena Kizhedath

Background: Cassia fistula Linn is a plant which is widely grown in India and is used for medicinal purposes. The study was carried out with an objective to demonstrate the antimicrobial activity of leaves of Cassia fistula Linn. The aim of the study is to assess antibacterial and antifungal activity of methanolic leaf extract of Cassia fistula Linn against selected clinical isolates.Methods: The antimicrobial activity of methanolic extract of Cassia fistula was evaluated using agar well diffusion method and to zone of inhibition of extract was determined. Clinical isolates of Staphyloccocus aureus, MRSA, Pseudomonas aeruginosa, E. coli and Proteus were screened.Results: The methanolic extracts exhibited antibacterial activity against Staphylococcus aureus. The extract was not active against E. coli, Proteus, MRSA, Pseudomonas aeruginosa. The extract also failed to demonstrate antifungal activity against Candida albicans and Aspergillus niger.Conclusions: The global emergence of multidrug resistant bacterial strains is increasing, limiting the effectiveness of current drugs and treatment failure of infections. A novel approach to the prevention of antibiotic resistance of pathogenic species is the use of new compounds that are not based on existing synthetic antimicrobial agents.


2017 ◽  
Vol 23 (1) ◽  
Author(s):  
Mohamed Salah K. Youssef ◽  
Ahmed Abdou O. Abeed ◽  
Talaat I. El-Emary

AbstractWith an intention to synergize the antimicrobial activity of 1,3-diphenyl pyrazole and chromene derivatives, 20 hybrid compounds were synthesized and evaluated for their antimicrobial activity. Structures of the newly synthesized compounds were established by elemental analysis and spectral data. All compounds were evaluated for their antimicrobial activity against Gram positive and Gram negative bacteria and antifungal activity by a well diffusion method. Compounds


2015 ◽  
Vol 2015 ◽  
pp. 1-10
Author(s):  
Ravi Bhushan Singh ◽  
Nirupam Das ◽  
Md. Kamaruz Zaman

A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, 1HNMR, 13CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 μgmL−1 against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 μgmL−1) and S. aureus (MIC 6.25 μgmL−1). The studies demonstrated that the para-fluorophenylpiperazine substituted s-triazine (4n) was potent and exhibited broad spectrum antibacterial activity against S. epidermidis, K. pneumoniae, and P. aeruginosa with MIC of 6.25 μgmL−1 and for E. coli, it showed an MIC of 3.125 μgmL−1 equipotent with reference to the standard drug. Among all the compounds under investigation, compound 4g also demonstrated significant antifungal activity (3.125 μgmL−1) against C. albicans.


2018 ◽  
Vol 2018 ◽  
pp. 1-5 ◽  
Author(s):  
Ali Yetgin ◽  
Kerem Canlı ◽  
Ergin Murat Altuner

In this study, antimicrobial activities of two different samples ofAllium sativumL. from Turkey (TR) (Taşköprü, Kastamonu, Turkey) and China (CN) were determined. A broad spectrum of Gram-negative and Gram-positive bacteria (17 bacteria) including species ofBacillus,Enterobacter,Enterococcus,Escherichia,Klebsiella,Listeria,Pseudomonas,Salmonella, andStaphylococcuswere used for testing antibacterial activity. In addition, antifungal activity againstCandida albicanswas also investigated. Antimicrobial activity was tested by using 3 different processes (chopping, freezing, and slicing by the disk diffusion method). The results showed that TR garlic presented more antimicrobial activity than CN garlic. Mechanism of activity of CN garlic could be proposed to be different from that of TR garlic.


Author(s):  
S. Santoshkumar ◽  
N. D. Satyanarayana ◽  
R. Anantacharya ◽  
P. Sameer

Objective: Synthesis of novel 2-(1-benzofuran-2-yl)-N'-[(3Z)-2-oxo-1, 2-dihydro-3H-indol-3-ylidene] quinoline-4-carbohydrazide and its derivatives for antimicrobial and antitubercular activity.Methods: Synthesis was carried out using the general method and the structures were confirmed by IR, 1H-NMR, [13]C-NMR and mass spectral analysis. The antibacterial activity was carried by agar well diffusion method, antifungal activity was performed by poison food technique and antitubercular activity was carried out by Microplate Alamar Blue Assay (MABA) method with the help of H37Rv. In silico absorption, distribution, metabolism, excretion, toxicity (ADMET) study of the drug, likeliness was carried out in ACD/lab-2.Results: The results revealed that at 25 mg/ml concentration, compounds 3a and 5a showed good antibacterial activity at 3.5±0.1, 3.8±0.3, 3.6±0.2 respectively against E. coli, K. pneumonia and S. typhimurium, when compared with drug streptomycin with similar concentration. The percentage of inhibition found at 50 µg/ml concentration, compounds 2b and 6a exhibited good antifungal activity at 53±1.15, 57±1.52 against A. flavus and C. neoformans, compared with standard drug fluconazole. The increase in activity was found to be dose dependent. The analogue 2a showed good antitubercular activity at 12.5±0.5 µg/ml, compounds 2b, 3a, 4a-b, 5a-b and 6a-b exhibited significant activity at 25±0.57 µg/ml and compound 3b showed moderate activity at 50±0.57 µg/ml. The mean value of P<0.05 were considered to be statistically significant. The absorption, distribution, metabolism, excretion and toxicity studies of the entitled molecules were analyzed and found to be in acceptable range.Conclusion: The study reveals that compounds containing benzofuran coupled nitrogen heterocycles are essential for activity as they possess excellent drug-like characteristics, suggesting to be potentially best inhibitor of H37Rv strain. The in silico ADME analysis also revealed that all the compounds were in acceptable range to obey the pharmacokinetic parameters.


Author(s):  
Alphonsus D’souza ◽  
Prashant Nayak ◽  
Prasanna Shama Khandige ◽  
Pankaj Kumar

Aim: Nicotine Substituted  1,3,4 Oxadiazole and pyrazole moieties were integrated by utilizing hydrazide as halfway .Oxadiazole were acquired by two techniques one is by utilizing PoCl3 within the sight of fragrant corrosive ,other is by utilizing carbon disulphide in the presence ofpotassium hydroxide as an impetus .Pyrazoles were likewise gotten by ehtylacetoacetate we acquired unrefined item and again it was recrystallized by utilizing alcohol.All incorporated mixtures were evaluated for Antibacterial activity  and enaminones showed promising action against standard medication ciprofloxacin. Methods: TLC on silica gel G was used to check for homogeneity of the title compound. H NMR, Mass, and IR Spectra were used to characterise these compounds, and their antibacterial activity was tested. Results: All of these compounds, including nicotine substituted ester, hydrazide, 1,3,4 Oxadiazole, and pyrazole, showed antibacterial activity. The maximum activity of enaminones was comparable to that of the standard drug ciprofloxacin (5mcg). Compound1 showed potent antimicrobial activity Conclusion: In the zone of inhibition studies, all six samples at MIC concentrations showed reasonable antimicrobial activity Compound1 showed very good antimicrobial activity


2016 ◽  
Vol 81 (3) ◽  
pp. 233-242 ◽  
Author(s):  
Kumaraswamy Battula ◽  
Sirassu Narsimha ◽  
Vasudevareddy Nagavelli ◽  
Priyanka Bollepelli ◽  
Rao Srinivasa

A convenient synthesis of novel1,4-disubstituted 1,2,3-triazoles (4a-j & 5a-j) is reported via copper (I) - catalyzed one pot [3+2] cycloaddition of various alkyl halides, sodium azide with (prop-2-yn-1-yl)thiomorpholine and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide. All the synthesized compounds were investigated for their antimicrobial activity. Compounds 4a, 4b, 4c, 4g, 5a and 5j against S.epidermidis, 4a, 5a and 5d against P. aeroginosa, 4a, 4b and 4g against K.pneumoniae, 4b, 5a and 5d against S.aureus and 5b, 5e and 5j against B.Subtilis have shown excellent antibacterial activity compared to the standard drugs Penicillin and Streptomycin. Compounds 4c, 4e, 4f, 4j, 5c, 5d, 5g and 5j have registered moderate antifungal activity as compared with standard drug Ampothericin-B.


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