scholarly journals Synthesis and antimicrobial activities of novel n-substituted 8-(1-alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5-chloroquinolines

2011 ◽  
Vol 76 (9) ◽  
pp. 1199-1206 ◽  
Author(s):  
Raju Chaudhari ◽  
Sahebrao Rindhe

Herein the synthesis of a series of novel 8-(1- alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5- chloroquinoline derivatives is reported. These derivatives were prepared by the condensation of o-phenylenediamine with [(5-chloroquinolin-8- yl)oxy]acetic acid, followed by substitution at nitrogen with different electrophilic reagents in presence of an appropriate base to give a series of nitrogen heterocycles containing the benzimidazole and quinoline nuclei. The structures of the compounds were confirmed based on 1H-NMR, 13CNMR, IR and mass spectral data. Almost all the compounds exhibited promising antibacterial activity against Salmonella typhimurium and Staphylococcus aureus. Some of the compounds showed good antifungal activities against Aspergillus niger but the antifungal activities against Candida albicans were disappointing.

10.3823/819 ◽  
2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Fatima El Malki ◽  
Kamal Eddaraji ◽  
Rajae Alloudane ◽  
Hassane Greche ◽  
Haiat Essalmani ◽  
...  

Introduction: Medicinal plants are plentiful of bioactive molecules effective against multi-resistance bacteria. The aims of this study were to assess the in vitro antimicrobial activities of essential oils extracted from three Moroccan aromatic plants. Methodology: Analysis of essential oils of Origanum compactum, Rosmarinus officinalis and Pelargonium asperum, collected from different localities in Morocco, were performed using a GC-MS spectrophotometry. Antibacterial activity was evaluated in vitro for five clinical multi-resistant isolates. Results: Origanum showed strong antibacterial activity against tested strains except Pseudomonas aeruginosa while Rosmarinum showed a bactericidal effect against Acinetobacter baumanii, Escherichia coli and Staphylococcus aureus. Pelargonium presented only slight growth inhibition of Staphylococcus aureus on solid medium, but provided bactericidal effect against Acinetobacter baumanii and Staphylococcus aureus. Interestingly, fractions F7 and F8 of Pelargonium which represented only 0.3% and 0.1% of the total mass were found bactericidal respectively against Klebsiella pneumoniae and Pseudomonas aeruginosa. Conclusions: Ours results showed that the antimicrobial activities were variables depending on the chemical composition of essential oils, the fraction used and the microorganism tested.Essential oils fractionation allows detection of bioactive substances, especially those owning antimicrobial activity, present in small quantities.


2019 ◽  
Vol 35 (2) ◽  
pp. 557-562
Author(s):  
D. Kasimbi ◽  
K.Hussain Reddy ◽  
N. Devanna

New hydrazones have been synthesized by condensing 2-acetylthiophene with acetic hydrazide and benzhydrazide. The synthesized hydrazones viz. 2-acetylthiophene acetoylhydrazone (ATAH), 2-acetylthiophene benzoylhydrazone (ATBH) are characterized in the light of physicochemical and analytical data. Structures of ATAH and ATBH are confirmed by FT-IR, 1H-NMR and Mass spectral data. The hydrazones are screened for their anti-bacterial activities against E Coli, Bacillus cereus, Staphylococcus aureus and Pseudomonas aureoginos. Acetoyl hydrazones are found to show more antibacterial activity than the corresponding benzoyl hydrazones.


Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 313
Author(s):  
Xiuli Xu ◽  
Jiangpeng Li ◽  
Kai Zhang ◽  
Shangzhu Wei ◽  
Rui Lin ◽  
...  

Nine new secondary metabolites, including six isocoumarin analogues, 7-hydroxyoospolactone (1), 7-methoxyoospolactone (2), 7-methoxy-9-hydroxyoospolactone (3), 10-acetoxy-9-hydroxyoospolactone (4), 6-dehydroxysescandelin (5), parapholactone (6), and three compounds with a rare skeleton of isocoumarin coupled with phenylethylamine, namely paraphamide A (12), paraphamide B (13), and paraphamide C (14), together with five known compounds, oospolactone (7), 8-O-methyloospolactone (8), 10-hydroxyoospolactone (9), 9,10-dihydroxyoospolactone (10), and oospoglycol (11), were isolated and identified from the marine-derived fungus Paraphoma sp. CUGBMF180003. Their chemical structures were determined using spectroscopic data, including HRESIMS and 1D and 2D NMR techniques. Furthermore, the stereogenic carbons in 5 and 14 were determined by comparing the experimental and calculated electronic circular dichroism (ECD) spectra. The carbon skeleton of 12–14 was identified as the first example of isocoumarin coupled with phenylethylamine derivatives. All of these compounds were examined for antimicrobial activities against Candida albicans and Staphylococcus aureus. Both 1 and 6 showed antibacterial activity against S. aureus with MIC values of 12.5 μg/mL.


2021 ◽  
Vol 4 (2) ◽  
pp. e183
Author(s):  
David Mutisya Musyimi ◽  
Tracy Ann Ashioya ◽  
George Opande ◽  
William Omuketi Emitaro

Human pathogenic microorganisms have developed resistance in response to indiscriminative use of commercial drugs. Plants produce many secondary metabolites with microbiocidal activity hence their use in traditional medicine. Herbalists in Kenya use medicinal plants including Solanum incanum in treating microbial infections. Though S. incanum has been used to treat different diseases in humans and animals, there is little information on antimicrobial activities of its extracts against Escherichia coli and Staphylococcus aureus. In this study, phytochemical analysis and antibacterial activity of solanum incanum leaves, roots and seeds extracts were determined. Ethanolic and aqueous extracts of leaf, root and seed of concentrations 25, 50, 75 and 100, and amoxicillin 25 mg/ml (control) with three replications were used for antibacterial analysis by the agar-well diffusion method. The results were subjected to analysis of variance at P < 0.05. Phytochemical screening revealed the presence of alkaloids, flavonoids, glycosides, saponins, steroids and tannins. Solanum incanum exhibited significant antibacterial effect against the two test bacteria. Ethanol extracts were more active than extracts against the bacteria. Ethanol extracts at 100% inhibited growth of Staphylococcus aureus more than the Escherichia coli. The zones of inhibition for Staphylococcus aureus were 35.0±0.6 mm, 30.94±0.3 mm and 30.14±0.64mm for seed, root and leaves respectively.On the other hand, the zones of inhibition for Escherichia coliat 100% ethanol were 27.20±0.06, 23.14±0.12 and 21.0±0.4 seed, root and leaves respectively.The results validate the use of these plants in ethnomedicine and potential of this plant in treating infections caused by the two bacteria.


2020 ◽  
Vol 8 (2) ◽  
pp. 40
Author(s):  
Ade Kurniawan Arie ◽  
Rosita A J Lintang ◽  
Remy E P Mangindaan ◽  
Agung B Windarto ◽  
Fitje Losung ◽  
...  

Nudibranchs are marine invetebrates belongs to the class of Gastropoda that are able to camouflage and develop a self-defense systems. Marine bacteria contain chemicals compunds that have potentials on marine drugs discovery through the secondary metabolism. The purpose of this study was to isolate the symbiotic bacteria from nudibranches Phylidiella pustulosa and Thuridilla lineolate and to screen the antibacterial activity of these bacterial isolates against Escherichia coli and Staphylococcus aureus. Isolation and culture of the symbiotic bacteria was made on B1 (solid) media. The results of the antibacterial assay showed that the symbiotic bacterial isolates from Phylidiella pustulosa and Thuridilla lineolate were able to inhibit the growth of the Staphylococcus aureus and Escherichia coli test. Keywords: nudibranch, Phyllidiella pustulosa, Thuridilla lineolate, bacteria, antibacterialAbstrakNudibranch adalah avetebrata laut dalam kelas Gastropoda yang mampu melakukan kamuflase dan mengembangkan sistem pertahanan diri. Bakteri laut mengandung senyawa kimia yang berpotensi sebagai bahan obat-obatan yang dihasilkan melalui metabolit sekunder. Tujuan dari penelitian ini yaitu untuk mengisolasi bakteri yang bersimbion dengan nudibranch Phylidiella pustulosa dan Thuridilla lineolate, kemudian mengamati aktivitas antibakteri dari isolat bakteri tersebut terhadap Escherichia coli danStaphylococcus aureus. Isolasi dan kultur bakteri yang bersimbion dibuat pada media B1 (padat). Skrining aktivitas antibakteri menunjukkan isolat bakteri yang bersimbion dengan nudibranch Phylidiella pustulosa dan Thuridilla lineolate mampu menghambat pertumbuhan organisme uji Staphylococcus aureus dan Escherichia coli. Kata kunci: nudibranch, Phyllidiella pustulosa, Thuridilla lineolate, bakteri, antibakteri


1970 ◽  
Vol 18 ◽  
pp. 16-20
Author(s):  
BA Omogbai ◽  
FA Eze

Context: Plant based antimicrobial represent a vast untapped source for medicines and further exploration of plant antimicrobial neeto occur. Evolvulus alsinoides (L) (Convolvulaceae) is a perennial herb is used in traditional medicine in East Asia, India, Africa and Philippines to cure fever, cough, cold, venereal diseases, azoospermia, adenitis and dementia.   Objective: The objective of this research was to evaluate the antimicrobial activity of the extracts of E. alsinoides on some clinical microbial isolates.   Materials and Methods: The ed thanolic and aqueous extracts of the whole plant (leaves and twigs) were analysed for alkanoids, tannins, glycosides, steroids, flavonoids, saponins, volatile oil and resins. The determination of antibacterial activity was done using the agar well diffusion technique. Pure cultures of pathogenic bacteria such as Bacillus cereus, Staphylococcus aureus, Micrococcus leutus, Klebsiella Pneumoniae, Pseudomonas aeruginosa, Escherichia coli and Salmonella typhi were used for antibacterial activity assay, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC).   Results: The ethanolic extract of the plant had MIC values ranging from 16 mg/ml to 512.5 mg/ml. The least MIC was 16mg-ml against Salmonella typhi while Bacillus cereus and Staphylococcus aureus showed the highest MIC of 512.5 mg-ml. In the aqueous extract the MIC ranged between 512.5 to >1025 mg/ml. Salmonella typhi, Micrococcus luteus and Staphylococcus aureus were not inhibited by the water extract. Phytochemical result showed ethanol to be a better solvent for the extraction of the bioactive agents in this plant which include: glycosides, alkaloids, saponins, tannins, flavonoids and volatile oil.   Conclusion: In this study the gram-negative organisms had the lowest MICs and MBCs. This suggests their higher susceptibility to the extract of this plant. On the basis of the result obtained in this investigation it can be concluded that ethanol extract of Evolvulus alsinoides had significant in vitro broad spectrum antimicrobial activity.   Keywords: Evolvulus alsinoides; Phytochemical screening; Antibacterial activity. DOI: http://dx.doi.org/10.3329/jbs.v18i0.8769 JBS 2010; 18(0): 16-20


2019 ◽  
Vol 74 (6) ◽  
pp. 473-478 ◽  
Author(s):  
Abd El-Galil E. Amr ◽  
Ahmed M. Naglah ◽  
Nermien M. Sabry ◽  
Alhussein A. Ibrahim ◽  
Elsayed A. Elsayed ◽  
...  

AbstractInterest in the synthesis of heterocyclic organic molecules with peptide moieties has gained attention due to their potential biological activities. The current work aimed at synthesizing new macrocyclic tripeptide imides and evaluating their possible antimicrobial activities. A series of 11 derivatives were prepared from dimethyl 3,5-pyridinevalinyl ester either by NaOH or NH2NH2 treatment, followed by cyclization and further reaction with NaOH or NH2NH2. The majority of synthesized derivatives showed promising antibacterial and antifungal activities in comparison to standard known antibiotics. Compounds 5a and 7b showed the most potential antibacterial against Staphylococcus aureus and antifungal activities against Candida albicans, respectively.


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