scholarly journals Syntheses and In Vitro Biological Activity of Some Derivatives of C-9154 Antibiotic

2012 ◽  
Vol 2012 ◽  
pp. 1-6
Author(s):  
Isaac Asusheyi Bello ◽  
George Iloegbulam Ndukwe ◽  
Joseph Olorunju Amupitan ◽  
Rachael Gbekele Ayo ◽  
Francis Oluwole Shode
Keyword(s):  
Biological Activity ◽  
Minimum Inhibitory Concentration ◽  
Functional Group ◽  
Inhibitory Concentration ◽  
2D Nmr ◽  
Esterification Reaction ◽  
New Antibiotics ◽  
Derivatives Of ◽  
Better Than

In our continued attempts at designing new antibiotics based on the structure of the C-9154 antibiotic, to simultaneously improve activity and lower toxicity, an analogue to the C-9154 antibiotic and six derivatives of this analogue were synthesized. The approach was to significantly reduce the polarity of the synthesized analogue in the derivatives to achieve increased permeability across cell membranes by conversion of the highly polar carboxylic group to an ester functional group. The compounds were synthesized using a two-step reaction which involved an additional reaction between benzyl amine and maleic anhydride and then conversion of the terminal carboxylic acid functional group to an ester functional group using a thionyl chloride mediated esterification reaction. The compounds were fully characterized using Infrared, GC-MS, and 1D and 2D NMR experiments. The in vitro biological activity of the compounds showed that the derivatives were more active than the analogues as was anticipated with minimum inhibitory concentration in the range 0.625–5 μg/mL. The analogue had minimum inhibitory concentration in the range 2.5–10 μg/mL. These values are significantly better than that obtained for the original C-9154 antibiotic which had activity in the range 10–>100 μg/mL.

scholarly journals Syntheses and Biological Activity of Some Derivatives of C-9154 Antibiotic

2012 ◽  
Vol 2012 ◽  
pp. 1-7
Author(s):  
Isaac Asusheyi Bello ◽  
George Iloegbulam Ndukwe ◽  
Joseph Olorunju Amupitan ◽  
Rachael Gbekele Ayo ◽  
Francis Oluwole Shode
Keyword(s):  
Biological Activity ◽  
Functional Group ◽  
Marked Effect ◽  
2D Nmr ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
New Antibiotics ◽  
Agricultural Use ◽  
Derivatives Of

This research was undertaken to design several new antibiotics, by structurally modifying the C-9154 antibiotic, simultaneously improving its activity and lowering toxicity. This was achieved by synthesizing an analogue to the C-9154 antibiotic and seven derivatives of this analogue. The approach was to significantly reduce the polarity of the synthesized analogue in the derivatives to achieve increased permeability across cell membranes by conversion of the highly polar carboxylic group to an ester functional group. The compounds were fully characterized using infrared, GC-MS, and 1D and 2D NMR experiments. The in vitro biological activity of the compounds showed that the derivatives were more active than the analogue as was anticipated and both were more active than the standard drugs used for comparison. Work is ongoing to establish applications for the compounds as antiplasmodials, antivirals, anticancers/tumours, antitrypanosomiasis, anthelminthic, and as general antibiotics for human, veterinary, and even agricultural use as they had marked effect on both Gram-positive and Gram-negative bacteria and some fungi.

Antibiotic potential of some synthesized derivatives of C-9154 antibiotic

2020 ◽  
Vol 15 (2) ◽  
pp. 52-58
Author(s):  
Isaac Asusheyi Bello ◽  
Isaac Asusheyi Bello ◽  
George Iloegbulam Ndukwe ◽  
Joseph Olorunju Amupitan ◽  
Rachael Gbekele Ayo ◽  
...  
Keyword(s):  
Structural Modification ◽  
Functional Group ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Derivatives Of ◽  
Acid Functional Group ◽  
Better Than

Structural modification of the C-9154 antibiotic in an attempt to simultaneously improve its activity and lower its toxicity led to the synthesis of an analogue of the C-9154 antibiotic and six derivatives of this analogue. The significant reduction of the polarity of the synthesized analogue in the derivatives to increase permeability across cell membranes was achieved by conversion of the highly polar carboxylic group to the nonpolar ester functional groups. The compounds were synthesized by condensation of 4-nitroaniline with maleic anhydride and then conversion of the terminal carboxylic acid functional group to an ester functional group using a thionyl chloride-mediated esterification. The in vitro biological activity using gram positive bacteria (MRSA, S. pyogenes, B. subtilis, and C. ulcerans), gram negative bacteria (E. coli, P. mirabilis, P. aeruginosa, S. typhii, S. dysenteriae, and K. pneumonia and some fungi (C. albicans, A. nigre and T. rubrum), showed that the derivatives were more active than their respective analogue and significantly better than the standard antibiotics (Sparfloxacin and Fluconazole) used for comparison, establishing their potential or use as antibiotics. The derivatives exhibited activity at concentrations as low as 0.625μg/mL while the analogue was active at 2.5μg/mL. These values were higher than results obtained for the standard drugs which showed activity at concentrations of 5 μg/mL. The derivatives however did not show activity against A. nigre whereas the analogue was active against it. Keywords: C-9154 Antibiotic, Bioactivity, Fumaramidmycin, antibacterial, antifungal

scholarly journals Synthesis and biological activity of some triazole-bearing benzimidazole derivatives

2011 ◽  
Vol 76 (3) ◽  
pp. 341-352 ◽  
Author(s):  
K.F. Ansari ◽  
C. Lal ◽  
R.K. Khitoliya
Keyword(s):  
Biological Activity ◽  
Minimum Inhibitory Concentration ◽  
Spectral Data ◽  
Inhibitory Concentration ◽  
Benzimidazole Derivatives ◽  
Disc Diffusion ◽  
Standard Drug ◽  
Elemental Analyses ◽  
Bacteria And Fungi

A number of N'-[(aryl)methylidene]-2-(2-methyl-1H-benzimidazol- 1-yl)acetohydrazide and 4-(aryl)-5-[(2-methyl-1H-benzimidazol- 1-yl)methyl]-4H-1,2,4-triazole-3-thiol derivatives were synthesized by incorporating various aromatic and heterocyclic substituents on 2-methyl-1H-benzimidazole. The structures of all the synthesized compounds were elucidated based on their elemental analyses and spectral data. The in vitro activities of these compounds against bacteria and fungi were evaluated by the disc diffusion and the minimum inhibitory concentration (MIC) methods. Some of the synthesized derivatives were found to be as active as kanamycin (standard drug).

Synthesis and biological activity of aldehyde derivatives of isopimaric acid

2021 ◽  
Vol 18 ◽  
Author(s):  
Yanju Lu ◽  
Zhendong Zhao ◽  
Yuxiang Chen ◽  
Jing Wang
Keyword(s):  
Inhibitory Concentration ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Klebsiella Pneumonia ◽  
Hep G2 ◽  
Isopimaric Acid ◽  
Streptococcus Pneumonia ◽  
Derivatives Of ◽  
Better Than

: Four series of acylhydrazone derivatives, including halogenated aryl modified acylhydrazone, thiophene, pyrrole and quinoline, were synthesized and characterized. The minimum inhibitory concentrations of the compounds against five bacteria were determined and most of the compounds displayed some degree of antibacterial activity. Isopimaric acid (pyrrole-3-carboxaldehyde) acylhydrazone (3j) exhibited the most potent activity against Streptococcus pneumonia and Klebsiella Pneumonia, with the minimum inhibitory concentration being 3.91 μg/mL. The antimicrobial activity against S. pneumoniae was improved when the pyrrole structure was introduced into isopimaric acid. All heterocyclic acylhydrazone derivatives of isopimaric acid exhibited a good in vitro antitumorial activity at 100 μM. It is concluded that the inhibitory effect of isopimaric acid (2-fluoro-6-methoxybenzaldehyde) acylhydrazone (3d) on Hep G2 and isopimaric acid (3-bromothiophene-2-carbaldehyde) acylhydrazone (3g) on Hep G2 and MDAMB 231 is better than that of the positive control 5-fluorouracil (5-FU) (76.51%), which is a widely used clinical anticancer agent, at 100 μM.

In Vitro Antibacterial activity of ethanolic extract of Myrsine africana against laboratory Strains of Pathogenic Organisms

2016 ◽  
Vol 5 (04) ◽  
pp. 4512
Author(s):  
Jackie K. Obey ◽  
Anthoney Swamy T* ◽  
Lasiti Timothy ◽  
Makani Rachel
Keyword(s):  
Antibacterial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
E Coli ◽  
Zones Of Inhibition ◽  
In Vitro Antibacterial Activity ◽  
Myrsine Africana

The determination of the antibacterial activity (zone of inhibition) and minimum inhibitory concentration of medicinal plants a crucial step in drug development. In this study, the antibacterial activity and minimum inhibitory concentration of the ethanol extract of Myrsine africana were determined for Escherichia coli, Bacillus cereus, Staphylococcus epidermidis and Streptococcus pneumoniae. The zones of inhibition (mm±S.E) of 500mg/ml of M. africana ethanol extract were 22.00± 0.00 for E. coli,20.33 ±0.33 for B. cereus,25.00± 0.00 for S. epidermidis and 18. 17±0.17 for S. pneumoniae. The minimum inhibitory concentration(MIC) is the minimum dose required to inhibit growth a microorganism. Upon further double dilution of the 500mg/ml of M. africana extract, MIC was obtained for each organism. The MIC for E. coli, B. cereus, S. epidermidis and S. pneumoniae were 7.81mg/ml, 7.81mg/ml, 15.63mg/ml and 15.63mg/ml respectively. Crude extracts are considered active when they inhibit microorganisms with zones of inhibition of 8mm and above. Therefore, this study has shown that the ethanol extract of M. africana can control the growth of the four organisms tested.

scholarly journals THE EFFECT OF PROPOLIS EXTRACT AND PROPOLIS CANDIES ON THE GROWTH OF AGGREGATIBACTER ACTINOMYCETEMCOMITANS ATCC 43718

2017 ◽  
Vol 10 (17) ◽  
pp. 26
Author(s):  
Khodijah Khodijah ◽  
Ratna Farida ◽  
Nurtami Soedarsono
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Aggregatibacter Actinomycetemcomitans ◽  
Spectrophotometric Analysis ◽  
Propolis Extract ◽  
Post Exposure ◽  
Colony Forming Units

Objective: This experiment aimed to analyze the effect of propolis extract and propolis containing candies on the growth of Aggregatibacter actinomycetemcomitans using spectrophotometric analysis and colony-forming units (CFU) counts.Methods: After A. actinomycetemcomitans were exposed to propolis extract and candies, the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined with spectrophotometry and post-exposure colony counting.Results: The MIC of propolis extract against A. actinomycetemcomitans was determined to be 10%, and the MBC was 20%. A decrease in the total CFU count of A. actinomycetemcomitans was observed after propolis extract and candy exposure.Conclusions: Propolis extract and propolis candies were effective in inhibiting the growth of A. actinomycetemcomitans ATCC 43718 in vitro.

scholarly journals New Antimalarial and Antimicrobial Tryptamine Derivatives from the Marine Sponge Fascaplysinopsis reticulata

Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 167 ◽  
Author(s):  
Pierre-Eric Campos ◽  
Emmanuel Pichon ◽  
Céline Moriou ◽  
Patricia Clerc ◽  
Rozenn Trépos ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Minimum Inhibitory Concentration ◽  
Marine Sponge ◽  
Nmr Spectra ◽  
Inhibitory Concentration ◽  
Chemical Study ◽  
2D Nmr ◽  
Antimicrobial Activities ◽  
2D Nmr Spectra ◽  
Ic50 Values

Chemical study of the CH2Cl2-MeOH (1:1) extract of the sponge Fascaplysinopsis reticulata collected in Mayotte highlighted three new tryptophan derived alkaloids, 6,6′-bis-(debromo)-gelliusine F (1), 6-bromo-8,1′-dihydro-isoplysin A (2) and 5,6-dibromo-8,1′-dihydro-isoplysin A (3), along with the synthetically known 8-oxo-tryptamine (4) and the three known molecules from the same family, tryptamine (5), (E)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (6) and (Z)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (7). Their structures were elucidated by 1D and 2D NMR spectra and HRESIMS data. All compounds were evaluated for their antimicrobial and their antiplasmodial activities. Regarding antimicrobial activities, the best compounds are (2) and (3), with minimum inhibitory concentration (MIC) of 0.01 and 1 µg/mL, respectively, towards Vibrio natrigens, and (5), with MIC values of 1 µg/mL towards Vibrio carchariae. In addition the known 8-oxo-tryptamine (4) and the mixture of the (E)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (6) and (Z)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (7) showed moderate antiplasmodial activity against Plasmodium falciparum with IC50 values of 8.8 and 8.0 µg/mL, respectively.

scholarly journals DIFFERENCE BETWEEN ANTIMICROBIAL EFFECTS OF PAPACARIE AND PAPAIN ON STREPTOCOCCUS MUTANS IN VITRO

2019 ◽  
pp. 79-83
Author(s):  
TITTY SULIANTI ◽  
NILAKESUMA DJAUHARI ◽  
BAMBANG NURSASONGKO
Keyword(s):  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Zone Of Inhibition ◽  
Antimicrobial Effects ◽  
Treatment Groups ◽  
Group Control ◽  
Caries Removal ◽  
And Diffusion ◽  
Better Than

Objective: The aim is to compare the antimicrobial effects of papain and Papacarie with dilution and diffusion tests.Methods: There were two treatment groups and one Group control. The treatment group received papain and Papacarie, and the control groupreceived chlorhexidine, in five liquids with different concentrations of 0.5%, 0.25%, 0.125%, 0.0625%, and 0.03%. The dilution and diffusion testswere used to determine the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and zone of inhibition for eachtreatment material.Results: MICs of papain and Papacarie were 12.5%, indicating that at a concentration of 12.5%, the material can inhibit the growth of Streptococcusmutans. Papain does not have an MBC value but the Papacarie has an MBC at 25%, which indicating that at a concentration of 25%, Papacarie hasbactericidal effects on S. mutans. The zone of inhibition of papain was lower than Papacarie.Conclusion: Based on chemomechanical caries removal materials, the antimicrobial effects of Papacarie were better than those of papain.

scholarly journals In VitroActivity of Omadacycline againstChlamydia pneumoniae

2018 ◽  
Vol 63 (2) ◽  
pp. e01907-18 ◽  
Author(s):  
Stephan A. Kohlhoff ◽  
Natalia Huerta ◽  
Margaret R. Hammerschlag
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Chlamydia Pneumoniae ◽  
Inhibitory Concentration ◽  
Content Type

ABSTRACTThein vitroactivities of omadacycline, azithromycin, doxycycline, moxifloxacin, and levofloxacin were tested against 15 isolates ofChlamydia pneumoniae. The minimum inhibitory concentration at which 90% of the isolates ofC. pneumoniaewere inhibited by omadacycline was 0.25 μg/ml (range, 0.03 to 0.5 μg/ml).

Activity of myxin against Ceratocystis ulmi

1969 ◽  
Vol 15 (1) ◽  
pp. 133-135 ◽  
Author(s):  
E. A. Peterson
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Liquid Culture ◽  
Inhibitory Concentration ◽  
In Vitro Tests ◽  
Strong Inhibition ◽  
Solid Media ◽  
Highly Sensitive ◽  
Paper Disc ◽  
Disc Assay

Eight strains of Ceratocystis ulmi originating from different locations and host species were found to be highly sensitive to the antibiotic myxin in in vitro tests. By paper disc assay, amounts as low as 0.5–1.0 μg caused strong inhibition of the fungus on solid media. The minimum inhibitory concentration in liquid culture was 0.2 μg/ml and levels of antibiotic above this concentration proved to be fungicidal.

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