Biological evaluation of 10-(diphenylmethylene)- 4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

2009 ◽  
Vol 4 (3) ◽  
pp. 362-368 ◽  
Author(s):  
Joanna Stefańska ◽  
Anna Bielenica ◽  
Marta Struga ◽  
Stafan Tyski ◽  
Jerzy Kossakowski ◽  
...  

AbstractAntibacterial and antifungal activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives were examined by the disc-diffusion method (growth inhibition zone diameter in agar medium). The MIC’s for the most active agents were determined. Title compounds were also evaluated in vitro against representatives of different virus classes. Most of the tested compounds exhibit activity against CVB-2 virus.

2016 ◽  
Vol 8 (2) ◽  
pp. 209-216
Author(s):  
A. Rahim ◽  
R. Ali ◽  
A. Islam

 2',4',5'- and 2',3',4'-trimethoxy flavanones have been synthesized starting with 2-hydroxyacetophone and substituted aldehyde. Antibacterial activities of the flavanones have been tested along with their corresponding chalcones against two human pathogenic bacteria (Streptococcus-b-haemolyticus and  Klebsiella sp. (G-)). Antifungal activities of the flavanones have also been investigated against  two plants pathogenic mold fungi (Rhizactonia solani Sclerotium rolfsii). The structures of the synthesized compounds have been characterized with the help of  UV, IR and 1H NMR and 13C-NMR spectra. The antibacterial and antifungal screening were performed in vitro by the filter paper disc diffusion method and poisoned food technique. The flavanones showed antibacterial activity while no activity was observed to their corresponding chalcones against the tested bacteria. On the other hand, chalcones and their corresponding flavanones both showed fungicidal activities.


2021 ◽  
Author(s):  
Faisal MB. Al-Sarraj ◽  
Ahmad M. Qumri

Abstract Background: Essential oils (EOs) are volatile, liquid substances that come from natural sources such as plants. As secondary metabolites of most plant species, that are typically found in leaf chloroplasts or from the hydrolysis of certain glycosides, their primary function is to combat attacks from predators as well as attract pollinators. Due to their biological activity, EOs have gained popularity in industries such as food processing, cosmetics, and personal care products as well as the pharmaceutical industry. In this study, the antimicrobial nature and antioxidant activity of Saudi Arabian EOs were compared with the antimicrobial activity of known antibiotics.Methods: The In vitro evaluation of antibacterial activity and antioxidant capacity of EOs collected from Jeddah domestic market for gram-negative and gram-positive pathogenic bacteria was carried out using the disc diffusion method. Disc diffusion method was used for the assessment of bactericidal activity of local EOs. The antioxidant activity was determined using phosphomolybdenum method. Furthermore, RAPD-PCR was used to compare the effects of these EOs on DNA in both untreated and treated pathogenic bacterial strains.Results and Conclusion: Bacterial strains with varying antibiotic resistance potential have been successfully isolated. The inhibition zone measurement revealed that the EOs used had some antibacterial effects on the bacterial strains as well as some selectivity on the bacterial strains that they acted on.


2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Tanveer MahamadAlli Shaikh ◽  
Habtamu Debebe

Indole motifs are one of the most significant scaffolds in the discovery of new drugs. We have described a synthesis of new N-substituted indole derivatives (1-3), and their in vitro antimicrobial activities were investigated. The synthesis of titled compounds has been demonstrated by utilizing commercially available starting materials. The antibacterial and antifungal activities were performed using new strains of bacteria Staphylococcus aureus, Escherichia coli, and Candida albicans using the disc diffusion method. Notably, the compound 4-(1-(2-(1H-indol-1-yl) ethoxy) pentyl)-N,N-dimethyl aniline (1) was found to be most potent than the other analogues (2 and 3), which has shown higher inhibition than the standard drug chloramphenicol.


2006 ◽  
Vol 1 (8) ◽  
pp. 1934578X0600100 ◽  
Author(s):  
Hocine Laouer ◽  
Salah Akkal ◽  
Claire Debarnot ◽  
Bruno Canard ◽  
Uwe J. Meierhenrich ◽  
...  

The chemical composition of the essential oil of Saccocalyx satureioides Coss. et Dur. (Lamiaceae) was analyzed by chiral and achiral GC/MS and 42 components were identified. The main constituents were (+)-α-terpineol (35.9%), thymol (15.6%) and borneol (12.4%). The in vitro antibacterial and antifungal activities of the essential oil were assessed by the disc diffusion method, and were significant on the six microorganisms tested. A moderate inhibitory activity against hepatitis C virus polymerase was also evidenced.


2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600
Author(s):  
Andrés F. Peralta-Bohórquez ◽  
Clara Quijano-Célis ◽  
Mauricio Gaviria ◽  
Consuelo Vanegas-López ◽  
Jorge A. Pino

The chemical composition of the volatile compounds from the leaves of Lantana canescens Kunth (Verbenaceae) and L. lopez-palacii Moldenke grown in Colombia were analyzed by GC and GC/MS. One hundred and thirty-nine volatile compounds were identified in L. canescens, of which the major ones were β-caryophyllene (13.5%), germacrene D (10.3%) and 1-octen-3-ol (8.4%). In the oil obtained from L. lopez-palacii, eighty-three compounds were identified, of which the most prominent were 1-octen-3-ol (24.4%) and β-caryophyllene (15.2%). The in vitro antibacterial activity of the L. lopez-palacii essential oil was studied against three bacterial strains using the disc diffusion method. No antimicrobial activity was found against Escherichia coli, Enterobacter sakazakii and Listeria monocytogenes.


2003 ◽  
Vol 51 (1) ◽  
pp. 53-59 ◽  
Author(s):  
I. Biksi ◽  
Andrea Major ◽  
L. Fodor ◽  

In vitro antimicrobial sensitivity of 12 Hungarian isolates and the type strain ATCC 33144 of Actinobaculum suis to different antimicrobial compounds was determined both by the agar dilution and by the disc diffusion method. By agar dilution, MIC50 values in the range of 0.05-3.125µg/ml were determined for penicillin, ampicillin, ceftiofur, doxycycline, tylosin, pleuromutilins, chloramphenicol, florfenicol, enrofloxacin and lincomycin. The MIC50 value of oxytetracycline and spectinomycin was 6.25 and 12.5µg/ml, respectively. For ofloxacin, flumequine, neomycin, streptomycin, gentamicin, nalidixic acid, nitrofurantoin and sulphamethoxazole + trimethoprim MIC50 values were in the range of 25-100µg/ml. With the disc diffusion method, all strains were sensitive to penicillin, cephalosporins examined, chloramphenicol and florfenicol, tetracyclines examined, pleuromutilins, lincomycin and tylosin. Variable sensitivity was observed for fluoroquinolones (flumequine, enrofloxacin, ofloxacin), most of the strains were susceptible to marbofloxacin. Almost all strains were resistant to aminoglycosides but most of them were sensitive to spectinomycin. A strong correlation was determined for disc diffusion and MIC results (Spearman's rho 0.789, p<0001). MIC values of the type strain and MIC50 values of other tested strains did not differ significantly. Few strains showed a partially distinct resistance pattern for erythromycin, lincomycin and ampicillin in both methods.


1970 ◽  
Vol 10 (3) ◽  
pp. 148-151
Author(s):  
M Ahmad ◽  
M Rahman ◽  
P Kumar Paul

Aims & Methods: The present study was undertaken to compare the antibacterial activity of a cephradine derivative with that of the parent antibiotic cephradine. Cephradine was converted to its benzoyl derivative by Schotten-Baumann method for the first time. Disc diffusion method was employed to find out the antibacterial activity against EPEC, ETEC, E. Agg, Salmonella typhi, Salmonella group B, Shigella boydii, Shigella dysenteriae 1, Shigella dysenteriae 2, Shigella flexinariae and Shigella sonnei. Melting point, TLC, HPLC, UV, FTIR and <sup>1</sup>H NMR studies were carried out to check the purity and confirm that the derivative was cephradine benzoate. Results: The benzoyl derivative showed promising activity against tested bacteria. The results obtained from the study demonstrate that the benzoyl derivative could be a potential antibacterial agent. Key words: Cephradine benzoate, antibacterial activity, disc diffusion method.   DOI: http://dx.doi.org/ 10.3329/bjms.v10i3.8356 BJMS 2011; 10(3): 148-151


2021 ◽  
Vol 3 (1) ◽  
pp. 14-18
Author(s):  
Qyana Al Farisi ◽  
Yuke Andriane ◽  
Miranti Kania Dewi

Kematian akibat infeksi Shigella, terutama Shigella dysenteriae dapat mencapai lebih dari 10% terutama pada anak dan lanjut usia pada kondisi tanpa pemberian terapi yang efektif. Siprofloksasin merupakan lini pertama untuk pengobatan infeksi Shigella, akan tetapi obat ini memiliki beberapa kekurangan di antaranya harga yang mahal dan resistensi. Daun mengkudu merupakan tanaman tradisional yang diduga memiliki efek antimikro dan diharapkan dapat menjadi alternatif terapi antibiotik bagi Shigella dysenteriae yang saat ini sudah banyak mengalami resistensi. Tujuan penelitian ini adalah mengetahui efek antimikro ekstrak air daun mengkudu (Morinda citrifolia L.) terhadap bakteri Shigella dysenteriae. Penelitian ini bersifat eksperimental laboratorium murni. Zona hambat ditentukan melalui metode difusi cakram. Objek penelitian yang digunakan adalah Shigella dysenteriae ATCC nomor 13313. Sampel uji berupa ekstrak air daun mengkudu konsentrasi 100%, kontrol positif (siprofloksasin) dan kontrol negatif (aquadest) dengan 9 kali pengulangan. Hasil uji antimikro dengan metode difusi cakram menunjukkan tidak terbentuk zona hambat pada ekstrak air daun mengkudu konsentrasi 100%. Hal tersebut menunjukkan ekstrak air daun mengkudu konsentrasi 100% tidak memiliki efek antimikro terhadap bakteri Shigella dysenteriae. Kadar flavonoid, tanin, dan alkaloid yang terdapat dalam ekstrak air daun mengkudu konsentrasi 100% pada penelitian ini kemungkinan belum cukup untuk menghasilkan efek yang diharapkan. Antimicrobial Effect of Water Extract of Noni (Morinda citrifolia L.) Leaves against Shigella dysenteriae In VitroDeath due to infection with Shigella, especially Shigella dysenteriae, can reach more than 10%, especially in children and the elderly in conditions without effective therapy. Ciprofloxacin is the first line for the treatment of Shigella infection, however this drug has several disadvantages including high price and resistance. Noni leaf is a traditional plant that is thought to have antimicrobial effects and is expected to be an alternative antibiotic therapy for Shigella dysenteriae which is currently experiencing a lot of resistance. The purpose of this study was to determine the antimicrobial effect of the water extract of noni leaves (Morinda citrifolia L.) on Shigella dysenteriae bacteria. This research is a pure laboratory experimental study. The zone of inhibition is determined by the disc diffusion method. The research object used was Shigella dysenteriae ATCC number 13313. The test sample was a water extract of noni leaves with a concentration of 100%, positive control (ciprofloxacin) and negative control (aquadest) with 9 repetitions. The results of the antimicrobial test using the disc diffusion method showed no inhibition zone was formed in the water extract of noni leaves with a concentration of 100%. This shows that a water extract of noni leaves with a concentration of 100% did not have an antimicrobial effect against the Shigella dysenteriae bacteria. The levels of flavonoids, tannins, and alkaloids contained in the water extract of noni leaves with a concentration of 100%  in this study may not be sufficient to produce the expected effect.


Author(s):  
Daniel A. Ondeko ◽  
Bernard F. Juma ◽  
Lilechi D. Baraza ◽  
Peter K. Nyongesa

Aims: To determine chemical constituents of the Leaf extracts of Centella asiatica using the LC-MS and GC-MS and their antimicrobial activities. Study Design: Structural determination of compounds from the leaf extracts was done using GC-MS and LC-MS analysis. The antimicrobial properties of the extracts were done using disc diffusion method. Place and Duration of Study:  Pure and Applied Chemistry Department, Masinde Muliro University of Science and Technology, Kenya: Between 2016-2019. Methodology: Plant materials of C. asiatica were sequentially extracted separately based on the polarity viz., hexane, ethyl acetate and methanol. Determination of chemical constituents was done using LC-MS and GC-MS analysis and phytochemical screening. The extracts were assayed against Staphylococcus aureus, Klebsiella pneumonia, Escherichia coli and Candida albicans. Standard antimicrobials viz. ampicillin and Nystatin were used as the control. Disc diffusion method was used and zones of inhibition, after respective incubation periods, were used to quantify antibacterial and antifungal activity. Results: Phytochemical screening of the hexane, ethyl acetate and methanolic extracts showed that terpenoids, flavonoids, saponins, alkaloids, steroids, amino acids and proteins, reducing sugars and carbohydrates were present. LC-MS and GC-MS analyses of the methanolic extracts identified 22 and 33 compounds, respectively, by use of the national institute of standards and technology (NIST) library. The extracts showed appreciable activity against common microbes tested. Conclusion: This study forms the basis for the biological characterization and significance of the compounds identified in the leaf and stem extracts of C. asiatica. These compounds are known to possess antibacterial and antifungal activities that could be established as potential candidates for future drug development. However, these extracts, need to be subjected to further chromatographic procedures to isolate the identified compounds and their bioactivities determined.


2021 ◽  
Vol 12 (6) ◽  
pp. 87-90
Author(s):  
Virendra Vaishnav ◽  
Debasish Sahoo ◽  
Tanushree Chatterjee

Medicinal Plants are the good source of natural antimicrobial agents. The main aim of present study was to evaluate the antibacterial activity of stem and root of Rauwolfia serpentina against six microorganism, Powdered stem and root of plant were extracted with acetone, chloroform and methanol and streptomycin used as positive control. The antibacterial activity of Rauwolfia serpentine was detected by using disc diffusion method and agar well diffusion method on the following bacteria- Bacillus cereus, Staphylococcus aureus, Bacillus fusiformis, Escherichia coli, Pseudomonas aeruginosa and P. luminescens. The experiment reported that R. serpentina Root methanol extract shown 14.86 ± 1.11 highest antibacterial activity against Pseudomonas aeruginosa through well diffusion method. Whereas root chloroform recorded 13.46 ± 1.28 highest antibacterial activity against E. coli through disc diffusion method, maximum zone of inhibition 22.66±0.52 mm was found for the positive control, streptomycin through well diffusion method. Further studies should be undertaken to reveal the correct mechanism of action of antimicrobial effect to identify the active ingredients which can be used in drug development program.


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