Rapid and efficient synthesis of newer heterocyclic 2-azetidinone and 5-benzylidine-4-oxo-thiazolidine compounds and their pharmacological studies

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Inhibitory Effect ◽  
Diffusion Method ◽  
Spectroscopic Techniques ◽  
Antimicrobial Compounds ◽  
Efficient Synthesis ◽  
Proteus Vulgaris ◽  
Bacterial Strains ◽  
Pharmacological Studies ◽  
In Vitro Antibacterial Activity

A straightforward rapid and efficient protocol for the synthesis of 2-azetidinone (D1-10) and 5-benzylidine-4-oxo-thiazolidine (F1-10) has been designed and synthesized in order to find newer antimicrobial compounds. The structure of entitle compounds have been evaluated on the basis of various spectroscopic techniques FTIR, 1H-NMR, 13C-NMR as well as elemental microanalysis. The title compounds were screened for their preliminary in vitro antibacterial activity against a panel of selected pathogenic bacterial strains, Staphylococcus aureus (MTCC 96), Escherichia coli (MTCC 443), Proteus vulgaris (MTCC 426) and Pseudomonas aeruginosa (MTCC 424) using cup-plate agar diffusion method at 40 μg/ml concentration. Out of synthesized compounds, compound nos. D4, D5, D7, D8, D9 and D10 have shown outstanding inhibitory effect against all pathogens and consider as the best bioactive desired antibacterial analogue of the series as compare to standard drugs ampicilline and chloramphenicol.

Preliminary in Vitro Investigations on The Inhibitory Activity of The Original Dietary Supplement Oxidal® on Pathogenic Bacterial Strains

2020 ◽  
Vol 11 ◽  
pp. 37-43
Author(s):  
Prof. Teodora P. Popova ◽  
Toshka Petrova ◽  
Ignat Ignatov ◽  
Stoil Karadzhov
Keyword(s):  
Dietary Supplement ◽  
Broad Spectrum ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Clinical Effectiveness ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Microbial Strains

The antimicrobial action of the dietary supplement Oxidal® was tested using the classic Bauer and Kirby agar-gel diffusion method. Clinical and reference strains of Staphylococcus aureus and Escherichia coli were used in the studies. The tested dietary supplement showed a well-pronounced inhibitory effect against the microbial strains commensurable with that of the broad-spectrum chemotherapeutic agent Enrofloxacin and showed even higher activity than the broad spectrum antibiotic Thiamphenicol. The proven inhibitory effect of the tested dietary supplement against the examined pathogenic bacteria is in accordance with the established clinical effectiveness standards for antimicrobial agents.

scholarly journals Essential Oil from Leaves of Lantana canescens and L. lopez-palacii Grown in Colombia

2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600
Author(s):  
Andrés F. Peralta-Bohórquez ◽  
Clara Quijano-Célis ◽  
Mauricio Gaviria ◽  
Consuelo Vanegas-López ◽  
Jorge A. Pino
Keyword(s):  
Essential Oil ◽  
Volatile Compounds ◽  
Diffusion Method ◽  
Disc Diffusion ◽  
Enterobacter Sakazakii ◽  
Bacterial Strains ◽  
Disc Diffusion Method ◽  
Germacrene D ◽  
In Vitro Antibacterial Activity

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.

scholarly journals In vitro antibacterial activity of Terminalia chebula leaf gall extracts against some human pathogenic strains

2012 ◽  
Vol 1 (8) ◽  
pp. 217-220 ◽  
Author(s):  
BE Ravi Shankara ◽  
YL Ramachandra ◽  
S Sundara Rajan ◽  
J Preetham ◽  
PS Sujan Ganapathy
Keyword(s):  
Antibacterial Activity ◽  
Aqueous Extract ◽  
Ethanol Extract ◽  
Pharmaceutical Journal ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Terminalia Chebula ◽  
Bacterial Strains ◽  
South Indian

The leaf galls of Terminalia chebula is used widely as Karkatasringi in south Indian markets. Karkatashringi is an important crude drug employed in various indigenous systems of medicine against several diseases and the drug has diverse medicinal properties. The present study was carried out to understand the antimicrobial activity of various extracts. The antibacterial activity of T. chebula (leaf gall) was evaluated against ten bacterial strains including Gram-positive and Gram-negative bacteria using the agar-well diffusion method. Among the two extracts tested, the ethanol extract presented the best results against all the bacteria while aqueous extract showed moderate inhibition of the microbial growth. Each extract is unique against different microorganisms; Staphylococcus aureus was more susceptible to both extract among the tested organisms, whereas Serratia marcescens and Proteus mirabilis were less susceptible for ethanol and aqueous extract respectively. The inhibitory effect of the extracts was compared with standard antibiotic Ciprofloxacin.DOI: http://dx.doi.org/10.3329/icpj.v1i8.11254 International Current Pharmaceutical Journal 2012, 1(8): 217-220 

scholarly journals The influence of plant essential oils on in vitro growth of Pectobacterium and Dickeya spp. bacteria

2021 ◽  
Vol 20 (6) ◽  
pp. 19-29
Author(s):  
Małgorzata Schollenberger ◽  
Agnieszka Gadomska-Gajadhur ◽  
Ewa Mirzwa-Mróz ◽  
Damian Kret ◽  
Ewa Skutnik ◽  
...  
Keyword(s):  
Essential Oils ◽  
Soft Rot ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Juniperus Virginiana ◽  
Bacterial Strains ◽  
Disk Diffusion Method ◽  
First Report ◽  
Plant Essential Oils

 The activity of essential oils from Eucalyptus globulus, Pinus silvestris, Lavandula angustifolia, Juniperus virginiana, Rosmarinus officinalis and Citrus paradise against the soft-rot pathogens Pectobacterium carotovorum subsp. carotovorum, Pectobacterium atrosepticum, Pectobacterium parmentieri and Dickeya solani was determined in vitro. The antibacterial activity of the essential oils will be evaluated using the disk-diffusion method by Kirby-Bauer [Bauer et al. 1966]. It was found that all the presented essential oils varied in antimicrobial activity against the four bacterial strains. No differences in the influence of streptomycin on inhibition of growth of the four bacterial strains were observed. Among six tested plants, essential oils from P. sylvestris had the strongest inhibitory effect on the growth of soft rot bacteria from Pectobacterium genus. This paper constitute the first report on the activity of the essential oils obtained from J. virginiana against soft rot bacteria. They are also the first report on the activity of the essential oils obtained from E. globulus, P. silvestris, L. angustifolia and C. paradisi against P. atrosepticum, P. parmentieri and D. solani as well as on the activity of the R. officinalis essential oils against P. atrosepticum and P. parmentieri.

Evaluation of Antibacterial Activity of Acer syriacum by Bioautography Method

1970 ◽  
Vol 9 (2) ◽  
pp. 3215-3219
Author(s):  
B. Al Asfour ◽  
R. Al-kayali ◽  
A. Kitaz
Keyword(s):  
Antibacterial Activity ◽  
Methanolic Extract ◽  
Ethyl Acetate Extract ◽  
Diffusion Method ◽  
Klebsiella Pneumonia ◽  
Bacterial Strains ◽  
In Vitro Antibacterial Activity ◽  
Inhibition Zones ◽  
Layer Chromatography

antibacterial activity of leaves, fruits and bark of acer syriacum was evaluated against both negative and positive gram bacterial strains. The powder of above parts were sequentially extracted with aqueous methanol 80%, acetone and petroleumether by maceration. The in vitro antibacterial activity of A. syriacum extracts (in concentration of 200 mg/mL) was performed by agar well diffusion method. Among the tested extracts, leaves methanolic extract has shown the highest growth inhibition. Further, the extract was fractionated, separated by thin layer chromatography (TLC) and submitted to bioautography. the results indicate that the ethyl acetate extract had  the most efficient antibacterial  compounds that displayed inhibition zones (25 mm) against Staphylococcus aureus ATCC25923 and (28mm) against Klebsiella pneumonia ATCC700603. the clear zones were located at RF= 0.15.

scholarly journals Chemical Composition and Antibacterial Activity of the Essential Oil of Retrohpyllum rospigliosii Fruits from Colombia

2010 ◽  
Vol 5 (7) ◽  
pp. 1934578X1000500
Author(s):  
Clara E. Quijano-Celis ◽  
Mauricio Gaviria ◽  
Consuelo Vanegas-López ◽  
Ina Ontiveros ◽  
Leonardo Echeverri ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Diffusion Method ◽  
Disc Diffusion ◽  
Bacterial Strains ◽  
Positive Bacterium ◽  
Disc Diffusion Method ◽  
In Vitro Antibacterial Activity ◽  
Bacterium Bacillus

The essential oil from fruits of Retrophyllum rospigliosii (Pilger) C.N. Page grown in Colombia was analyzed by GC and GC/MS. Ninety-one compounds were identified, of which the most prominent were limonene (37.7%) and α-pinene (16.3%). The in vitro antibacterial activity of the essential oil was studied against seven bacterial strains using the disc diffusion method. The strongest activity of the oil was against the Gram-positive bacterium Bacillus cereus.

scholarly journals Phytochemical Studies Antibacterial and Antioxidant Activities of Aerial Parts of Ferula lutea (Poir.) Maire.

2019 ◽  
Vol 6 (1) ◽  
pp. 17-25
Author(s):  
Ibtissem Boulacel ◽  
Brahim Harkati ◽  
Radia Ayad ◽  
Ibrahim Demirtas ◽  
Hocine Laouer ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Dry Weight ◽  
Antibacterial Activities ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Spectroscopic Techniques ◽  
Aerial Parts ◽  
New Compounds

Abstract The focus of this paper was to assess the phytochemical composition, the antioxidant and antibacterial activities of the crude extracts of the aerial parts of Ferula lutea. Four new compounds were isolated from this genus, and their structures were primarily established by extensive spectroscopic analysis including 1D and 2D spectroscopic techniques. Total phenolics and flavonoids containing in ethyl acetate (AcOEt) and n-butanol (n-BuOH) extracts were quantified [199.1-184.02 mg gallic acid equivalent / g of dry weight], flavonoids [70.24-65.95 mg quercetin / g dry weight]. DDPH scavenging and phosphomolybdenum methods were used to evaluate in vitro antioxidant activity. The obtained results showed a significant antioxidant activity of the two aerial parts. Correlation analysis between the DPPH values and those for TAC indicates the possibility of the two models for evaluating antioxidants power from medicinal plants. Dichloromethane (CH2Cl2), AcOEt and n-BuOH extracts were screened against two gram-negative [Escherichia coli (E.coli) and Pseudo aeruginosa (P.aer)] and two gram-positive [Staphylococcus aureus (S.aur) and Bacillus (Bacil.)] bacteria using disc diffusion method. The results indicate a good inhibition of CH2Cl2 and EtAct extracts on the growth of (Bacil. and E.coli). Furthermore n-but extract showed a significant inhibitory effect only against E.coli.

scholarly journals In Vitro Antibacterial Activity of Black Soldier Fly (Hermetia Illucens) Larva Extracts Against Gram-Negative Bacteria

2019 ◽  
Vol 43 (2) ◽  
Author(s):  
Harlystiarini Harlystiarini ◽  
Rita Mutia ◽  
I Wayan Teguh Wibawan ◽  
Dewi Apri Astuti
Keyword(s):  
Antibacterial Activity ◽  
Inhibition Zone ◽  
Test Method ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Black Soldier Fly ◽  
E Coli ◽  
In Vitro Antibacterial Activity ◽  
Zone Growth

The aim of this study was to evaluate the in vitro antibacterial activity of Black soldier fly (BSF) larva extract. The BSF larva was extracted using methanol and then tested for antibacterial activity using agar diffusion method (zone growth inhibition). The antibacterial activity was conducted against Salmonella sp. and Escherichia coli, two important bacterial strains in poultry, using six dilution levels (10 mg/ml, 20 mg/ml, 40 mg/ml, 80 mg/ml, 160 mg/ml and 320 mg/ml). All the results were subjected analyze using t-test method. Based on the diameter of the inhibition zone, the BSF larva extract has a strong (P<0.05) antibacterial activity against Salmonella sp. and E. coli when the concentration used 320 mg/ml. In addition, BSF larva extract also contain high amount of lauric acid (49.18%), a saturated fatty acid that has been proven to proposes as antibacterial agent. Therefore, it could be concluded that the BSF larva extract could be used as a candidate for antibacterial substances. 

Mechanism of the Antiplatelet Action of Dipyridamole in Whole Blood: Modulation of Adenosine Concentration and Activity

1986 ◽  
Vol 55 (01) ◽  
pp. 012-018 ◽  
Author(s):  
Paolo Gresele ◽  
Jef Arnout ◽  
Hans Deckmyn ◽  
Jos Vermylen
Keyword(s):  
Platelet Aggregation ◽  
Adenosine Receptor ◽  
Whole Blood ◽  
Blood Cells ◽  
Inhibitory Action ◽  
Phosphodiesterase Inhibitor ◽  
Inhibitory Effect ◽  
Adenosine Concentration ◽  
Pharmacological Studies

SummaryDipyridamole inhibits platelet aggregation in whole blood at lower concentrations than in plasma. The blood cells responsible for increased effectiveness in blood are the erythrocytes. Using the impedance aggregometer we have carried out a series of pharmacological studies in vitro to elucidate the mechanism of action of dipyridamole in whole blood. Adenosine deaminase, an enzyme breaking down adenosine, reverses the inhibitory action of dipyridamole. Two different adenosine receptor antagonists, 5’-deoxy-5’-methylthioadenosine and theophylline, also partially neutralize the activity of dipyridamole in blood. Enprofylline, a phosphodiesterase inhibitor with almost no adenosine receptor antagonistic properties, potentiates the inhibition of platelet aggregation by dipyridamole. An inhibitory effect similar to that of dipyridamole can be obtained combining a pure adenosine uptake inhibitor (RE 102 BS) with a pure phosphodiesterase inhibitor (MX-MB 82 or enprofylline). Mixing the blood during preincubation with dipyridamole increases the degree of inhibition. Lowering the haematocrit slightly reduces the effectiveness.Although we did not carry out direct measurements of adenosine levels, the results of our pharmacological studies clearly show that dipyridamole inhibits platelet aggregation in whole blood by blocking the reuptake of adenosine formed from precursors released by red blood cells following microtrauma. Its slight phosphodiesterase inhibitory action potentiates the effects of adenosine on platelets.

Total Synthesis and Antibacterial Screening of (±)-6,8-Dihydroxy-3- undecyl-3,4-dihydroisochromen-1-one: A Structural Analogue of Metabolites from Ononis natrix

2019 ◽  
Vol 16 (3) ◽  
pp. 245-248
Author(s):  
Hummera Rafique ◽  
Aamer Saeed ◽  
Ehsan Ullah Mughal ◽  
Muhammad Naveed Zafar ◽  
Amara Mumtaz ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Structural Analog ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Antibacterial Screening ◽  
Maximum Inhibition ◽  
Bacillus Subtilus ◽  
Hydrolysis Of ◽  
Direct Condensation

Background: (±)-6,8-Dihydroxy-3-undecyl-3,4-dihydroisochromen-1-one is one of the structural analog of several substituted undecylisocoumarins isolated from Ononis natrix (Fabaceae), has been successfully synthesized by direct condensation of homopthalic acid (1) with undecanoyl chloride yields isochromen-1-one (2). Methods: Alkaline hydrolysis of (2) gave the corresponding keto-acid (3), which is then reduced to hydroxy acid (4) then its cyclodehydration was carried out with acetic anhydride to afford 3,4- dihydroisochromen-1-one (5). Followed by demethylation step, the synthesis of target 6,8- dihydroxy-7-methyl-3-undecyl-3,4-dihydroisocoumarin (6) was achieved. Results: In vitro antibacterial screening of all the synthesized compounds were carried out against ten bacterial strains by agar well diffusion method. Conclusion: Newly synthesized molecules exhibited moderate antibacterial activity and maximum inhibition was observed against Bacillus subtilus and Salmonella paratyphi.

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