SYNTHESIS, CHARACTERISATION AND USEFUL THERAPEUTIC ACTIVITY OF NOVEL 2- QUINOLONE DERIVATIVES

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 41-46
Author(s):  
B.S Jayashree ◽  
◽  
N Sharma ◽  
S. Nigam

A series of novel 2-oxo-1,2,3,4-tetrahydroquinolin-7-yl benzoate derivatives were synthesised and obtained in moderate yields (55-85%) by the reaction of parent 7-hydroxy-1,2,3,4-tetrahydroquinolin- 2-one (7-hydroxy-3,4-dihydroquinolin-2(1H)-one) with substituted benzoyl chlorides. The synthesised test compounds were characterised by spectral analysis. Partition coefficient was determined for all test compounds and was found to be in the range of 1.2-2.9. Further, the compounds were screened for their antibacterial and antioxidant activities. They were also randomly screened for their antidiabetic potential by non-enzymatic glycosylation of haemoglobin assay. However, the results revealed that test compounds did not possess antioxidant and antidiabetic potential comparable to that of their respective standards. The results also revealed that most of the compounds exhibited antibacterial action against four bacterial strains namely Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Further, the test compound VIIl (at 500 µg mL-1), showed zone of inhibition comparable to that of the standard ciprofloxacin (at 500 µg mL-1).

Author(s):  
P Danish ◽  
Q Ali ◽  
MM Hafeez ◽  
A Malik

Aloe vera is a well-known medicinal plant used in many therapeutic purposes. Naturally it is composed of many useful compounds that have ability to use for treatment of many diseases. The active compounds reported in this plant are saponins, sugar, enzymes, vitamins, aloesin, aloeemodin, aloin, acemannan aloemannan, aloeride, methylchromones, flavonoids, naftoquinones, sterols, minerals, anthraquinones, amino acids, lignin and salicylic acid and other different compounds including fat-soluble and water-soluble vitamins, enzymes, minerals, simple/complex sugars, organic acid and phenolic compounds. In this study aloe vera is used for antibacterial and antifulgal activity against different strains of bacteria and pathogenic fungal strains. Ethanol extract of Aloe vera leaves and roots is applied on these bacterial and fungal strains in different concentrations (15, 20, 25, 30µl). Bacillus cereus, Bacillus subtitis, Bacillus megaterium, Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumannii, and some other bacterial strains are used for this study. Escherichia coli and Agrobacterium tumefacins shows zone of inhibition around 18mm which consider as good result. Bacillus subtitis and Bacillus megaterium also shows good result around 16mm. Proteus mirabilis and Pseudomonas aeruginosa shows minimum zone of inhibition which is around 11mm. among all used fungal strains (fuserium oxysporum, Candida albicans, Aspergillus fumigatus, Aspergillus niger) fuserium oxysporum and Aspergillus niger shows excellent results around 19mm both against root extract and leaves extract.


2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
S. C. Sati ◽  
Lokendra Singh

Anguillospora longissima, isolated from root as endophytic freshwater hyphomycetes, was evaluated for its bioactivity (antibacterial potential) against five bacterial strains, namely, Gram-positive (Bacillus subtilisMTCC 121) and Gram-negative (Agrobacterium tumefaciensMTCC 609,Escherichia coliMTCC 40,Erwinia chrysanthemum,andXanthomonas pseudomonas). Antimicrobial activity was assessed by measuring the zone of inhibition with preliminary and secondary antimicrobial assays. The applied fungus was found significant for all tested bacterial strains as showen by their zone of inhibition. In preliminary antimicrobial assay, maximum zone of inhibition was recorded against Gram-negative human pathogenic bacterial strainEscherichia coli(23 mm) followed byErwinia chrysanthemi(22 mm),Agrobacterium tumefaciens(21 mm), andXanthomonas phaseoli(21 mm), while minimum zone of inhibition was observed againstBacillus subtilis(20 mm). In secondary antimicrobial assay, the maximum zone of inhibition was recorded againstErwinia chrysanthemi(11 mm) followed byAgrobacterium tumefaciens(10 mm),Xanthomonas phaseoli(10 mm), andBacillus subtilis(9 mm) and minimum inhibition was found againstEscherichia coli(8 mm).


Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-4 ◽  
Author(s):  
Mohammad Firoz Alam ◽  
Mohammed M. Safhi ◽  
Sivakumar Sivagurunathan Moni ◽  
Aamena Jabeen

The objective of this investigation was to predict the antibacterial properties ofsodium seleniteagainst selected human pathogens. A group of six human bacterial pathogens includingStaphylococcus aureus,Streptococcus pyogenes,Bacillus subtilis,Escherichia coli,Pseudomonas aeruginosa, andKlebsiella planticolawere utilized for screening. The spectrum of activity was qualified based on zone of inhibition. Our study demonstrated thatsodium seleniteexhibits a strong spectrum of activity againstBacillus subtilis,Staphylococcus aureus,Escherichia coli, andKlebsiella planticola.The spectrum of activity was compared with standard ciprofloxacin disc (5 μg/disc) and observed to have satisfactory effect.


2021 ◽  
Vol 37 (5) ◽  
pp. 1132-1138
Author(s):  
Sonia Yadav ◽  
Nitin Kumar

Coumarins are well known for their significant biological potential against several onsets. A series of novel 4-hydroxycoumarin substituted derivatives were synthesized and screened for their antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeureginosa bacterial strains. The zone inhibition was observed against 10 µL against different for each compound. The outcomes of the study showed that out of 10 synthesized compounds, compound 4a, 4b, 4h, and 4j showed most significant inhibitory potential against different microbial strains. The zone of inhibition for compound 4a and 4b was found as 6.36 ± 0.162, 5.60 ± 0.049, 3.61 ± 0.176, 5.64 ± 0.021 and 7.29 ± 0.339, 5.53 ± 0.459, 3.35 ± 0.226, 5.55 ± 0.042 mm while compound 4h and 4j exhibited 7.10 ± 0.544, 5.11 ± 0.183, 3.95 ± 0.226, 4.94 ± 0.494 and 6.46 ± 1.725, 4.53 ± 0.261, 3.83 ± 0.791, 5.40 ± 0.049 mm, respectively.


Author(s):  
E. Vijaya Sekhar ◽  
Subhas S. Karki ◽  
Javarappa Rangaswamy ◽  
Mahesh Bhat ◽  
Sujeet Kumar

Abstract Background Sulfonamides (sulfa drugs) and the metals like mercury, copper, and silver bear antimicrobial properties. The discovery of broad-spectrum antibiotics such as penicillins, cephalosporins, and fluoroquinolones has reduced their use. However, in some instances these drugs are the first-line treatment. The metal-based sulfonamide (e.g., silver sulfadiazine) is considered as first choice treatment in post-burn therapy while the use of silver nanoparticle-cephalexin conjugate to cure Escherichia coli infection explains the synergistic effect of sulfa drugs and their metal conjugates. With growing interest in metal-based sulfonamides and the Schiff base chemistry, it was decided to synthesize sulfonamide Schiff base metal complexes as antioxidant and antimicrobial agent. Results The Fe (III), Ru (III), Co (II), Ni (II), Cu (II), Pd (II), Zn (II), Cd (II), and Hg (II) metal complexes of 4-((thiophen-2-ylmethylene)-amino)-benzenesulfonamide (TMABS) were prepared and studied for thermal stability, geometry, and other electronic properties. The ligand TMABS (Schiff base) and its metal complexes were screened in-vitro for 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and antimicrobial properties against Gram-positive (+ve) Bacillus subtilis (MTCC-441), Staphylococcus aureus (MTCC 7443), Gram-negative (-ve) Escherichia coli (MTCC 40), Salmonella typhi (MTCC 3231), and fungal strains Aspergillus niger (MTCC-1344) and Penicillium rubrum by agar well diffusion method. Results summarized in Tables 3, 4, and 5 represent the inhibitory concentration (IC50) in micromole (μM). The zone of inhibition (ZI) in millimeter (mm) represents antimicrobial properties of TMABS and its metal complexes. Conclusions The synthesized sulfanilamide Schiff base (TMABS) behaved as a neutral and bidentate ligand coordinating with metal ions through its azomethine nitrogen and thiophene sulfur to give complexes with coordination number of 4 and 6 (Fig. 3). The nucleophilic addition of sulfanilamide amino group (–NH2) group to carbonyl carbon (>C=O) of benzaldehyde gave sulfanilamide Schiff base (imine) (Fig. 2). All the metal complexes were colored and stable at room temperature. With IC50 of 9.5 ± 0.1 and 10.0 ± 0.7 μM, the Co, Cu, and Pd complexes appeared better antioxidant than the ligand TMABS (155.3±0.1 μM). The zone of inhibition (ZI) of Hg (28 mm) and Ru complexes (20 mm) were similar to the ligand TMABS (20 mm) against Aspergillus niger (MTCC-1344) as in Figs. 4, 5, and 6. None of the synthesized derivatives had shown better antimicrobial properties than the standard streptomycin sulfate and fluconazole.


Foods ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 285
Author(s):  
Da Liu ◽  
Ronald Walcott ◽  
Kevin Mis Solval ◽  
Jinru Chen

Interests in using biological agents for control of human pathogens on vegetable seeds are rising. This study evaluated whether probiotic bacterium Lactobacillus rhamnosus GG, bacterial strains previously used as biocontrol agents in plant science, as well as a selected plant pathogen could compete with foodborne human pathogens, such as Salmonella enterica and enterohemorrhagic Escherichia coli (EHEC), for growth in microbiological media and attachment to vegetable seeds; and to determine whether the metabolites in cell-free supernatants of competitive bacterial spent cultures could inhibit the growth of the two pathogens. The results suggest that the co-presence of competitive bacteria, especially L. rhamnosus GG, significantly (p < 0.05) inhibited the growth of Salmonella and EHEC. Cell-free supernatants of L. rhamnosus GG cultures significantly reduced the pathogen populations in microbiological media. Although not as effective as L. rhamnosus GG in inhibiting the growth of Salmonella and EHEC, the biocontrol agents were more effective in competing for attachment to vegetable seeds. The study observed the inhibition of human bacterial pathogens by competitive bacteria or their metabolites and the competitive attachment to sprout seeds among all bacteria involved. The results will help strategize interventions to produce vegetable seeds and seed sprouts free of foodborne pathogens.


mSystems ◽  
2017 ◽  
Vol 2 (4) ◽  
Author(s):  
Amy Platenkamp ◽  
Jay L. Mellies

ABSTRACT Archetypal pathogenic bacterial strains are often used to elucidate regulatory networks of an entire pathovar, which encompasses multiple lineages and phylogroups. With enteropathogenic Escherichia coli (EPEC) as a model system, Hazen and colleagues (mSystems 6:e00024-17, 2017, https://doi.org/10.1128/mSystems.00024-17 ) used 9 isolates representing 8 lineages and 3 phylogroups to find that isolates with similar genomic sequences exhibit similarities in global transcriptomes under conditions of growth in medium that induces virulence gene expression, and they found variation among individual isolates. Archetypal pathogenic bacterial strains are often used to elucidate regulatory networks of an entire pathovar, which encompasses multiple lineages and phylogroups. With enteropathogenic Escherichia coli (EPEC) as a model system, Hazen and colleagues (mSystems 6:e00024-17, 2017, https://doi.org/10.1128/mSystems.00024-17 ) used 9 isolates representing 8 lineages and 3 phylogroups to find that isolates with similar genomic sequences exhibit similarities in global transcriptomes under conditions of growth in medium that induces virulence gene expression. They also found variation among individual isolates. Their work illustrates the importance of moving beyond observing regulatory phenomena of a limited number of regulons in a few archetypal strains, with the possibility of correlating clinical symptoms to key transcriptional pathways across lineages and phylogroups.


2014 ◽  
Vol 77 (7) ◽  
pp. 1212-1218 ◽  
Author(s):  
BURTON BLAIS ◽  
MYLÈNE DESCHÊNES ◽  
GEORGE HUSZCZYNSKI ◽  
MARTINE GAUTHIER

A simple immunoenzymatic enterohemorrhagic Escherichia coli (EHEC) colony check (ECC) assay was developed for the presumptive identification of priority EHEC colonies isolated on plating media from enrichment broth cultures of foods. With this approach, lipopolysaccharide extracted from a colony is spotted on the grid of a polymyxin-coated polyester cloth strip, and bound E. coli serogroup O26, O45, O103, O111, O121, O145, and O157 antigens are subsequently detected by sequential reactions with a pool of commercially available peroxidase-conjugated goat antibodies and tetramethylbenzidine substrate solution. Each strip can accommodate up to 15 colonies, and test results are available within 30 min. Assay performance was verified using colonies from a total of 73 target EHEC isolates covering the range of designated priority serogroups (all of which were reactive), 41 nontarget E. coli isolates including several nontarget Shiga toxin–producing E. coli serogroups (all unreactive), and 33 non–E. coli strains (all unreactive except two bacterial strains possessing O-antigenic structures in common with those of the priority EHEC). The ECC assay was reactive with target colonies grown on several types of selective and nonselective plating media designed for their cultivation. These results support the use of the ECC assay for high-throughput screening of colonies isolated on plating media for detecting priority EHEC strains in foods.


2020 ◽  
pp. 1-4
Author(s):  
Hatim MY Hamadnalla ◽  
◽  
Mahdi Abd Elmageed Mohammed ◽  

The objective of this study to examine phytochemical analysis of sonchus oleraceus l, (asteraceae) (moliata) extracts which were extracted by four solvents, petroleum ether, chloroform, methanol and distill water and to assess their potential antibacterial against four standard bacteria gram-positive and gramnegative (bacillus subtilis staphylococcus aureu, salmonella typhi, and pscudomona aeruginosa) and antioxidant activities. (moliata) extracts using cold maceration method to extract sonchus oleraceus l, (asteraceae) locally known as (moliata) extracts, where dpph assay and paper disc diffusion assay were employed to evaluate the antioxidant and antibacterial activities respectively. The results showed that tannins, triterpenes, a sterols, flavonoids and cardiac glycosides compounds were present in the sonchus oleraceus l, (asteraceae) lives (moliata) extracts. The methanol extract of leaves showed high antioxidant potential (77± 0.03 % ) and chloroform showed low antioxidant potential activity (4±0.09) compare with propyl gallate as standard (93± 0.010 %) against dpph. Chloroform extract was effective and give moderate zone of inhibition against staphylococcus aureus. Methanol extract was effective and showed moderate zone of inhibition against staphylococcus aureus, bacillus subtilis, salmonella typhi and pseudomonas aeruginosa.


2021 ◽  
Vol 5 (1) ◽  
pp. 1-9
Author(s):  
Antonio Carlos Pereira de Menezes Filho ◽  
Matheus Vinícius Abadia Ventura ◽  
Carlos Frederico de Souza Castro

Tibouchina granulosa is a species that blooms annually in several regions of Brazil. This species is still little explored in terms of phytocompounds in all organs of this plant, especially the floral organ. Flowers of T. granulosa were collected in the municipality of Rio Verde, Goiás, Brazil, in 2021. The hydroethanolic floral extract was prepared by maceration and qualitative phytochemical (colorimetric reactions and salt formation) and antibacterial analyzes performed and the results expressed in millimeters of inhibition at different concentrations in mg mL-1. Several phytochemical classes were observed with positive results, especially for alkaloids, phenolics, oxylates, saponins, carbohydrates and tannins. As for the bacterial assay, potential antibacterial activity was observed for all bacterial strains tested, except for Salmonella serovar Thyphymurium and serovar Enteritidis. Expressive inhibitions were observed for Enterococcus faecalis > Pseudomonas aeruginosa > Staphylococcus aureus and Escherichia coli at the highest concentrations between 100-50 mg mL-1. The floral extract of Tibouchina granulosa showed phytotherapeutic potential with the presence of several phytochemical groups and expressive antibacterial activity.


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