scholarly journals SYNTHESIS OF ARYL (5-SUBSTITUTED BENZOFURAN-2-YL) CARBAMATE DERIVATIVES AS ANTIMICROBIAL AGENTS

Author(s):  
Shankar N. Budhwani ◽  
Shailendra Sharma ◽  
Navanath Kalyane

ABSTRACTObjectives: Benzofurans are very interesting heterocycles, which are available in nature and show a wide range of pharmacological activities, viz.,antifungal, antibacterial, antitumor, antimalarial and antioxidant activity.Methods: A convenient method for the preparation of aryl (5-substituted benzofuran-2-yl) carbamate derivatives 6a-6j has been developed. Thetarget compounds 1-(5-nitrobenzofuran-2-yl)-3-arylurea (6a-6e) and 1-(5-bromobenzofuran-2-yl)-3arylurea (6f-6j) have been prepared by reacting5-nitrobenzofuran-2-carbonyl azide 5a or 5-bromobenzofuran-2-carbonyl azide 5b with substituted phenols in reasonable overall yields. Allthe synthesized compounds were characterized using Fourier transform infrared (FTIR), 1H NMR and mass spectrometry and were subjected toantimicrobial screening against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), two Gram-negative bacteria (Escherichiacoli and Pseudomonas aeruginosa), and two fungi (Candida albicans and Aspergillus niger) using two-fold dilution method.Results and Discussion: All the values of FTIR, 1H NMR and mass spectra were found to be prominent. The results indicate that synthesized compound6i showed potent antimicrobial activity comparable to standard.Conclusion: The detailed synthesis, spectroscopic data, and antimicrobial activities of synthesized compounds were reported.Keywords: Benzofuran, Antibacterial activity, Antifungal activity.

Author(s):  
Ali Arkan Majhool ◽  
Hamidah Idris ◽  
Wan Mohd Nuzul Hakimi ◽  
Muhd Danish Daniel Abdullah

The existing study examined three actinomycetes isolated from Beach Ridges Interspersed with Swales (BRIS) soil where the morphological properties were examined and chemical compounds of their metabolite extracts were ana; ysed. Based on phylogenetic analysis of 16S rRNA gene sequences, the strains were identified as Streptomyces sp. AA13, Amycolatopsis sp. AA12 and Micromonosporasp. AA141. Antimicrobial activities of the extracts were tested against a panel of microorganisms that consist of Escherichia coli DSM 30083, Bacillus subtilis DSM 10, Pseudomonas fluorescens DSM 50090, Klebsiella pneumoniae DSM 30104, Micrococcus luteus DSM 20030, and Saccharomyces cerevisiae. Results revealed a wide range of antimicrobial activities produced by the isolates at different concentration of each extracts. The extracts were found to show stronger antimicrobial activities against gram-negative bacteria compared to gram-positive bacteria, while no activities were shown when tested against fungi. Thirty-nine compounds were detected both from Streptomycessp. AA13 and Amycolatopsissp. AA12, while thirty-eight compounds from Micromonosporasp. AA141 using GC-MS. This Study Demonstrate the ability of actinomycetes in producing variety type of compounds with antimicrobial activities that may be the potential candidates as drug leads.


2014 ◽  
Vol 71 (1) ◽  
Author(s):  
Shajarahtunnur Jamil ◽  
Siti Mariam Abdul Lathiff ◽  
Siti Awanis Abdullah ◽  
Noraini Jemaon ◽  
Hasnah Mohd Sirat

Antimicrobial activities of flavonoids isolated from the leaves and heartwoods of Artocarpus anisophyllus Miq. and Artocarpus lowii King were evaluated. Gram positive bacteria (Staphylococcus aureus and Bacillus cereus), Gram negative bacteria (Escherichia coli and Pseudomonas putida) and fungi (Candida albicans and Candida glabrata) were used in this study. Disc diffusion method was used as the qualitative assay while minimum inhibitory concentration and minimum microbicidal concentration methods were used as the quantitative assays. Artocarpin (8) showed strong antimicrobial activity towards all bacteria with inhibition zone diameter more than 11 mm and minimum microbicidal concentration value of 0.45 mg/mL. Isobavachalcone (3) exhibited strong antibacterial activity towards Gram positive bacteria with minimum microbicidal concentration value of 0.45 mg/mL. The findings of this study revealed that the isolated flavonoids from A. anisophyllus and A. lowii have potential to be developed as antimicrobial agents.


2000 ◽  
Vol 44 (4) ◽  
pp. 848-852 ◽  
Author(s):  
C. M. Kunin ◽  
W. Y. Ellis

ABSTRACT Mefloquine was found to have bactericidal activity against methicillin- and fluoroquinolone-susceptible and -resistant strains ofStaphylococcus aureus and Staphylococcus epidermidis and gentamicin- and vancomycin-resistant strains ofEnterococcus faecalis and Enterococcus faecium. The MICs were 16 μg/ml, and the minimal bactericidal concentrations (MBCs) were 16 to 32 μg/ml. These concentrations cannot be achieved in serum. Mefloquine was active at a more achievable concentration against penicillin-susceptible and -resistant Streptococcus pneumoniae, with MICs of 0.2 to 1.5 μg/ml. Mefloquine was not active against gram-negative bacteria and yeasts. In an attempt to find more active derivatives, 400 mefloquine-related compounds were selected from the chemical inventory of The Walter Reed Army Institute of Research. We identified a series of compounds containing a piperidine methanol group attached to pyridine, quinoline, and benzylquinoline ring systems. These had activities similar to that of mefloquine against S. pneumoniae but were far more active against other gram-positive bacteria (MICs for staphylococci, 0.8 to 6.3 μg/ml). They had activities similar to that of amphotericin B againstCandida spp. and Cryptococcus neoformans. Combinations of the compounds with gentamicin and vancomycin were additive against staphylococci and pneumococci. The MIC and MBC of gentamicin were decreased by four- to eightfold when this drug was combined with limiting dilutions of the compounds. There was no antagonism with other antimicrobial drugs. The compounds were rapidly bactericidal. They appear to act by disrupting cell membranes. Combinations of the compounds with aminoglycoside antibiotics may have potential for therapeutic use.


2013 ◽  
Vol 79 (21) ◽  
pp. 6737-6746 ◽  
Author(s):  
Hilda Tiricz ◽  
Attila Szűcs ◽  
Attila Farkas ◽  
Bernadett Pap ◽  
Rui M. Lima ◽  
...  

ABSTRACTLeguminous plants establish symbiosis with nitrogen-fixing alpha- and betaproteobacteria, collectively called rhizobia, which provide combined nitrogen to support plant growth. Members of the inverted repeat-lacking clade of legumes impose terminal differentiation on their endosymbiotic bacterium partners with the help of the nodule-specific cysteine-rich (NCR) peptide family composed of close to 600 members. Among the few tested NCR peptides, cationic ones had antirhizobial activity measured by reduction or elimination of the CFU and uptake of the membrane-impermeable dye propidium iodide. Here, the antimicrobial spectrum of two of these peptides, NCR247 and NCR335, was investigated, and their effect on the transcriptome of the natural targetSinorhizobium melilotiwas characterized. Both peptides were able to kill quickly a wide range of Gram-negative and Gram-positive bacteria; however, their spectra were only partially overlapping, and differences were found also in their efficacy on given strains, indicating that the actions of NCR247 and NCR335 might be similar though not identical. Treatment ofS. meliloticultures with either peptide resulted in a quick downregulation of genes involved in basic cellular functions, such as transcription-translation and energy production, as well as upregulation of genes involved in stress and oxidative stress responses and membrane transport. Similar changes provoked mainly in Gram-positive bacteria by antimicrobial agents were coupled with the destruction of membrane potential, indicating that it might also be a common step in the bactericidal actions of NCR247 and NCR335.


2017 ◽  
Vol 22 (3) ◽  
pp. 147
Author(s):  
Masteria Yunovilsa Putra ◽  
Tri Aryono Hadi

GC-MS analysis of the crude extracts of three different species of Indonesian marine sponges has been carried out for identification of bioactive compounds. The GC-MS analysis from Haliclona (Gellius) sp., Lamellodysidea herbacea, and Spheciospongia inconstans revealed the presence of 23, 21, 19 various compounds, respectively and mainly sterols and fatty acids. All the sponge species has been evaluated for antimicrobial activities, cytotoxicity using brine shrimp lethality bioassay and heme polymerization inhibitory activity assay for antiplasmodial activity. In this study, all the sponge species showed antimicrobial activities against at leastone of the test strains. Among them, the extract of sponge Lamellodysidea herbacea displayed activity against two Gram-positive bacteria (S. aureus and B. subtilis) and the Gram-negative bacteria V. cholerae, with inhibition zones of 10.3, 9.2 and 9.5 mm, respectively. The sponge Haliclona (Gellius) sp., showed significant activity against fungal pathogen C. albicans. The sponge Haliclona (Gellius) sp., displayed the ability to inhibit heme polymerization indicating an anti-Plasmodium function and also showed potent cytotoxic activity against the brine shrimp Artemia sp. Keywords: GC-MS analysis, antimicrobial, sponges,bioactive


Antibiotics ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 1044
Author(s):  
Bahman Khameneh ◽  
N. A. Michael Eskin ◽  
Milad Iranshahy ◽  
Bibi Sedigheh Fazly Bazzaz

The extensive usage of antibiotics and the rapid emergence of antimicrobial-resistant microbes (AMR) are becoming important global public health issues. Many solutions to these problems have been proposed, including developing alternative compounds with antimicrobial activities, managing existing antimicrobials, and rapidly detecting AMR pathogens. Among all of them, employing alternative compounds such as phytochemicals alone or in combination with other antibacterial agents appears to be both an effective and safe strategy for battling against these pathogens. The present review summarizes the scientific evidence on the biochemical, pharmacological, and clinical aspects of phytochemicals used to treat microbial pathogenesis. A wide range of commercial products are currently available on the market. Their well-documented clinical efficacy suggests that phytomedicines are valuable sources of new types of antimicrobial agents for future use. Innovative approaches and methodologies for identifying plant-derived products effective against AMR are also proposed in this review.


1962 ◽  
Vol 8 (5) ◽  
pp. 621-628 ◽  
Author(s):  
W. A. Taber ◽  
B. B. Wiley

The antimicrobial activities of a branched, monoalkyl benzene sulphonate complex (ABS), the active component of a commercial liquid household detergent, and of the detergent have been investigated. Cultures of dermatophytes, Candida albicans, saprophytic phycomycetes, ascomycetes, fungi imperfecti, Gram-positive and Gram-negative bacteria were tested. Only the Fusarium species and the Gram-negative bacteria were not inhibited by a concentration of 0.1 ml of the detergent/50 ml medium. Microgram quantities of ABS inhibited the Gram-positive bacteria and the fungi except Fusarium spp. ABS was lethal in microgram quantities, the effect being detectable within 30 minutes. Inhibition of exogenous respiration of glucose by C. albicans began upon contact and was complete within 50 minutes. A linear and biodegradable ABS was more active than the branched form against C. albicans.


2020 ◽  
Vol 12 (10) ◽  
pp. 949-959
Author(s):  
Ranju Bansal ◽  
Ranjit Singh

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.


2014 ◽  
Vol 9 (12) ◽  
pp. 1934578X1400901 ◽  
Author(s):  
Wan Mohd Nuzul Hakimi Wan Salleh ◽  
Farediah Ahmad ◽  
Khong Heng Yen

The study was designed to examine the chemical composition and antimicrobial activities of essential oils extracted from the aerial parts of three Piper species: Piper abbreviatum, P. erecticaule and P. lanatum, all from Malaysia. GC and GC/MS analysis showed qualitative and quantitative differences between these oils. GC and GC-MS analysis of P. abbreviatum, P. erecticaule and P. lanatum oils resulted in the identification of 33, 35 and 39 components, representing 70.5%, 63.4% and 78.2% of the components, respectively. The major components of P. abbreviatum oil were spathulenol (11.2%), ( E)-nerolidol (8.5%) and β-caryophyllene (7.8%), whereas P. erecticaule oil mainly contained β-caryophyllene (5.7%) and spathulenol (5.1%). Borneol (7.5%), β-caryophyllene (6.6%) and α-amorphene (5.6%) were the most abundant components in P. lanatum oil. Antimicrobial activity was carried out using disc diffusion and broth micro-dilution method against nine microorganisms. All of the essential oils displayed weak activity towards Gram-positive bacteria with MIC values in the range 250–500 μg/mL. P. erecticaule oil showed the best activity on Aspergillus niger (MIC 31.3 μg/mL), followed by P. lanatum oil (MIC 62.5 μg/mL). This study demonstrated that the essential oils have potential as antimicrobial agents and may be useful in the pharmaceutical and cosmetics industries.


Foods ◽  
2019 ◽  
Vol 8 (1) ◽  
pp. 31 ◽  
Author(s):  
Yushuang Lu ◽  
Xiaojian Zhao ◽  
Sheng Fang

The effect of hydrogen peroxide (H2O2) oxidation on the physicochemical, gelation and antimicrobial properties of gellan gum was studied. The oxidized gellan gum (OGG) was characterized by measuring the carboxyl/carbonyl group contents, Fourier transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The H2O2 oxidation resulted in a large increase in the carboxyl groups in gellan gum. The OGG lost gelation ability by oxidation even in the presence of metal ions. The antimicrobial activities of the OGG against Gram-positive bacteria (Staphylococcus aureus), Gram-negative bacteria (Escherichia coli), and fungal (Aspergillus niger) were tested. The OGG could inhibit the growth of both bacteria and fungal, and the activity was improved with an increase in the oxidation level. Finally, the application of the OGG as an active coatings material to extend the storage of apples was tested.


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