scholarly journals In vitro Antimicrobial Activity of Some Synthetic Isoindolinone and Isoquinolinone Derivatives

1970 ◽  
Vol 5 (1) ◽  
pp. 15-19 ◽  
Author(s):  
AFG Masud Reza ◽  
Md. Wahab Khan ◽  
Mohammad S Rahman ◽  
Chowdhury M Hasan ◽  
Mohammad A Rashid

A total of six N-substituted benzamides, eight isoindolinone derivatives and six isoquinolinone analogs have been screened against five Gram positive and twelve Gram negative bacteria as well as four human fungal pathogens. From the antimicrobial screening, it is evident that 2-iodo-N-subustituted tetrahydro-1-oxo isoquinoline-3-carboxylic acids showed very prominent activity at a concentration 200 µg/disc, while the N-subtituted-3-alkyl isoindolin-1-one acetates showed weak to moderate activity. At the same time, 2-iodo-N-subustituted benzamides revealed very poor activity. Key words: 2-iodo-N-substituted benzamide, Isoindolinone, Isoquinolinone, Antimicrobial assay, Disc diffusion. Dhaka Univ. J. Pharm. Sci. Vol.5(1-2) 2006 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

eLife ◽  
2019 ◽  
Vol 8 ◽  
Author(s):  
Mark Austin Hanson ◽  
Anna Dostálová ◽  
Camilla Ceroni ◽  
Mickael Poidevin ◽  
Shu Kondo ◽  
...  

Antimicrobial peptides (AMPs) are host-encoded antibiotics that combat invading microorganisms. These short, cationic peptides have been implicated in many biological processes, primarily involving innate immunity. In vitro studies have shown AMPs kill bacteria and fungi at physiological concentrations, but little validation has been done in vivo. We utilized CRISPR gene editing to delete most known immune-inducible AMPs of Drosophila, namely: 4 Attacins, 2 Diptericins, Drosocin, Drosomycin, Metchnikowin and Defensin. Using individual and multiple knockouts, including flies lacking these ten AMP genes, we characterize the in vivo function of individual and groups of AMPs against diverse bacterial and fungal pathogens. We found that Drosophila AMPs act primarily against Gram-negative bacteria and fungi, contributing either additively or synergistically. We also describe remarkable specificity wherein certain AMPs contribute the bulk of microbicidal activity against specific pathogens, providing functional demonstrations of highly specific AMP-pathogen interactions in an in vivo setting.


2018 ◽  
Author(s):  
Mark Austin Hanson ◽  
Anna Dostalova ◽  
Camilla Ceroni ◽  
Mickael Poidevin ◽  
Shu Kondo ◽  
...  

Antimicrobial peptides (AMPs) are host-encoded antibiotics that combat invading microorganisms. These short, cationic peptides have been implicated in many biological processes, primarily involving innate immunity. In vitro studies have shown AMPs kill bacteria and fungi at physiological concentrations, but little validation has been done in vivo. We utilised CRISPR gene editing to delete all known immune inducible AMPs of Drosophila, namely: 4 Attacins, 4 Cecropins, 2 Diptericins, Drosocin, Drosomycin, Metchnikowin and Defensin. Using individual and multiple knockouts, including flies lacking all 14 AMP genes, we characterize the in vivo function of individual and groups of AMPs against diverse bacterial and fungal pathogens. We found that Drosophila AMPs act primarily against Gram-negative bacteria and fungi, acting either additively or synergistically. We also describe remarkable specificity wherein certain AMPs contribute the bulk of microbicidal activity against specific pathogens, providing functional demonstrations of highly specific AMP-pathogen interactions in an in vivo setting.


Author(s):  
Ahmed T. Sulaiman ◽  
Susan W. Sarsam

A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity against some of the examined Gram-positive and Gram-negative bacteria. While no activity was exhibited by any of the examined compounds against the Gram-positive S. aureus.


2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Mansour Znati ◽  
Aymen Jabrane ◽  
Hafedh Hajlaoui ◽  
Fethia Harzallah-Skhiri ◽  
Jalloul Bouajila ◽  
...  

The present work describes the chemical composition and evaluates the antimicrobial and the anti-acetylcholinesterase properties of the flower oil from the Tunisian Ferula lutea obtained by hydrodistillation and analyzed by combination of GC/FID and GC/MS. The chemical composition of the flower oil of this species is reported for the first time. Seventeen compounds were identified accounting for 94.3% of the total oil. The chemical composition of this essential oil was characterized by a high proportion of monoterpene hydrocarbons (80.4%) among which δ-3-carene (31.2%) and α-pinene (25.8%) were the predominant compounds. The oxygenated monoterpenes represent the second major fraction (12.0%), 2,3,6-trimethylbenzaldehyde (10.9%) being the predominant one. Furthermore, the isolated oil was tested for its antimicrobial activity using the disc-diffusion and the microdilution assays against six Gram-positive and five Gram-negative bacteria as well as towards eight Candida species. It was found that flower oil of F. lutea exhibited interesting antibacterial and anticandidal activity (MIC = 39 μg/mL against Escherichia coli, Staphylococcus aureus and S. epidermidis and MIC = 156 μg/mL against Candida albicans). The anti-acetylcholinesterase effect of this oil was also evaluated in this work. Results showed that this oil exhibits significant activity (IC50 =70.25±5.41 μg/mL).


2021 ◽  
Vol 29 (2) ◽  
pp. 183-190
Author(s):  
I.V. Shipitsyna ◽  
◽  
E.V. Osipova ◽  
A.A. Natalskiy ◽  
A.V. Pavlov ◽  
...  

Objective. To determine the species composition of the associations isolated from osteomyelitis foci and to study the character of associate relationships based on the biofilm-forming ability data. Methods. The microbiological study included clinical isolates (n=184) obtained from associations (n=88) during primary inoculations from wounds and fistulas of patients (n= 88) with chronic osteomyelitis of long tubular bones. In order to obtain an associative biofilm in vitro, the cultures of competing bacterial strains were daily mixed in 1:1 ratio. The biofilms were grown on the surface of polystyrene plates with subsequent determination of the level of biofilm formation in 24 and 48 hours. Thecoefficient of relationship (CR) was calculated to evaluate the synergistic, neutral and antagonistic relationships between bacteria in the biofilms. Results. The associations of staphylococcus with gram-negative bacteria were most frequently recovered from osteomyelitis foci. On the 1st day of the experiment, 38,6 % of associations had a moderate biofilm-forming ability, and besides, associations of gram-positive + gram-negative bacteria were observed in 36,4%; 42,1% of associations had a low biofilm-forming ability; 19,3% - had a high biofilm-forming ability. After 48 hours the percentage of mild adhesive strains remained at the same level - 38,6%, as for the low adhesive ones it decreased to 36,4%, high adhesive - increased up to 25%. Most bacterial associations manifested antagonistic relationships. Synergism in biofilm-formingby the association of S. aureus + P. aeruginosa was observed in 2 cases,while the level of film-forming was high as on the first and the second day of the study. In several associations it transformed from antagonistic to synergistic or neutral relationships. Conclusion. It has ben established that among the identified associations, the largest specific weight falls on the associations of gram-positive + gram-negative bacteria , while S. aureus is one of the most common components. These associations were noted to have high and mild activity of biofilm -forming on the surface of polystyrene plates. Relationships between the microorganisms isolated from osteomyelitis foci in associations, as a rule, are antagonistic. What this paper adds For the first time, the nature of the relationship between microorganisms in the composition of associations isolated from the osteomyelitis focus has been studied on the basis of biofilm-forming ability data. It has been established that in microbiocenosis of the osteomyelitis foci, the greatest specific weight falls on the associations of S. aureus with gram-negative bacteria. These associations have a high and moderate activity of biofilm formation on the surface of polystyrene plates. The relationships between microorganisms isolated from the osteomyelitis focus as part of associations are usually antagonistic.


2015 ◽  
Vol 69 (8) ◽  
Author(s):  
Martin Krátký ◽  
Jana Mandíková ◽  
František Trejtnar ◽  
Vladimír Buchta ◽  
Jiřina Stolaříková ◽  
...  

AbstractProgression of drug resistance among bacterial and fungal pathogens justifies the development of novel antimicrobial agents. Thus, a series of novel sulphamethoxazole-based ureas and imidazolidine- 2,4,5-triones have been designed and synthesised. The urea derivatives were obtained by the reaction of sulphamethoxazole and isocyanates, and their cyclisation to imidazolidine-2,4,5-triones was performed via oxalyl chloride. All synthesised derivatives were evaluated in vitro to determine their activity against gram-positive and gram-negative bacteria, fungi, Mycobacterium tuberculosis, and atypical mycobacteria and their cytotoxicity. The growth of mycobacteria was inhibited within the range of 4-1000 μM and M. tuberculosis was the least-susceptible strain. 4-(3-Heptylureido)- N-(5-methylisoxazol-3-yl)benzenesulphonamide was identified as the most promising compound because it exhibited the highest activity against atypical mycobacteria at minimum inhibitory concentrations, from 4 μM, and with acceptable toxicity (selectivity indices for M. avium and M. kansasii higher than 16 and 62.5, respectively). Gram-positive bacteria, including methicillinresistant Staphylococcus aureus, were inhibited at concentrations starting from 125 μM, whereas the investigated derivatives exhibited almost no antifungal potency and activity against gram-negative species.


2019 ◽  
Vol 16 (4) ◽  
pp. 401-407
Author(s):  
Fauzia Anjum Chattha ◽  
Samina Kousar ◽  
Mehr-un-Nisa ◽  
Munawar Ali Munawar

Background: Indazoleacetic acids and their pharmaceutically acceptable salts have been claimed to be useful as anti-inflammatory, analgesic and antipyretic agents. They are active in the treatment of respiratory diseases such as asthma, bronchitis, allergies and obstructive pulmonary diseases. </P><P> Objectives: We report herein a feasible study concerned about the design, synthesis, structure and in vitro antimicrobial activity of 3-arylindazole-1-acetic acids derivatives. Series of compounds were synthesized by alkylation of 3-arylindazoles. Method: Synthesized compounds were subjected to study the effect on microbial growth in vitro. All synthesized compounds were found to exhibit antibacterial activities against a range of grampositive (Bacillus subtilis, Staphylococcus aureus) and gram-negative bacteria (Shigella sonnei, Escherichia coli) by broth dilution method. Results: The synthesized compounds exhibited antibacterial activities comparable to fluoroquinolones and some compounds exhibited better activity. These findings suggest a great potential of 3-arylindazole-1-acetic acids as antibacterial compounds. Conclusion: 3-Arylindazole-1-acetic acids are potent antimicrobial agent better than their respective 3-arylindazoles that revealed moderate activity against both gram positive and gram negative bacteria.


2016 ◽  
Vol 3 (1) ◽  
pp. 17-24 ◽  
Author(s):  
Poonam Gupta ◽  
Jitendra K. Gupta

A series of 4-chloro-3-methyl-N-(substituted phenyl)-5-oxo-4,5-dihydro-1H-pyrazole-1- carbothioamide were synthesized using earmark reaction of thiosemicarbazides and ethyl-2-chloroacetoacetate in DMF. All structures of the synthesized compounds were distinguished on the basis of IR,1H-NMR,13C-NMR and also elemental analysis. Synthesized Compounds were examined their potent antifungal activity using disc diffusion technique against three fungal pathogens vizAspergillus niger, Candida albicansandCurvularia. Fluconazole were used as standard drug respectively. All compounds exhibited good to moderate activity.


Author(s):  
Sushma Vashisht ◽  
Manish Pal Singh ◽  
Viney Chawla

The methanolic extract of the resin of Shorea robusta was subjected to investigate its antioxidant and antibacterial properties its utility in free radical mediated diseases including diabetic, cardiovascular, cancer etc. The methanol extract of the resin was tested for antioxidant activity using scavenging activity of DPPH (1,1-diphenyl-2-picrylhydrazil) radical method, reducing power by FeCl3 and antibacterial activity against gram positive and gram negative bacteria using disc diffusion method. The phytochemical screening considered the presence of triterpenoids, tannins and flavoniods. Overall, the plant extract is a source of natural antioxidants which might be helpful in preventing the progress of various oxidative stress mediated diseases including aging. The half inhibition concentration (IC50) of resin extract of Shorea robusta and ascorbic acid were 35.60 µg/ml and 31.91 µg/ml respectively. The resin extract exhibit a significant dose dependent inhibition of DPPH activity. Antibacterial activity was observed against gram positive and gram negative bacteria in dose dependent manner.Key Words: Shorea robusta, antioxidant, antibacterial, Disc-diffusion, DPPH.


2020 ◽  
Vol 20 (3) ◽  
pp. 192-208 ◽  
Author(s):  
Talita Odriane Custodio Leite ◽  
Juliana Silva Novais ◽  
Beatriz Lima Cosenza de Carvalho ◽  
Vitor Francisco Ferreira ◽  
Leonardo Alves Miceli ◽  
...  

Background: According to the World Health Organization, antimicrobial resistance is one of the most important public health threats of the 21st century. Therefore, there is an urgent need for the development of antimicrobial agents with new mechanism of action, especially those capable of evading known resistance mechanisms. Objective: We described the synthesis, in vitro antimicrobial evaluation, and in silico analysis of a series of 1H-indole-4,7-dione derivatives. Methods: The new series of 1H-indole-4,7-diones was prepared with good yield by using a copper(II)- mediated reaction between bromoquinone and β-enamino ketones bearing alkyl or phenyl groups attached to the nitrogen atom. The antimicrobial potential of indole derivatives was assessed. Molecular docking studies were also performed using AutoDock 4.2 for Windows. Characterization of all compounds was confirmed by one- and two-dimensional NMR techniques 1H and 13C NMR spectra [1H, 13C – APT, 1H x 1H – COSY, HSQC and HMBC], IR and mass spectrometry analysis. Results: Several indolequinone compounds showed effective antimicrobial profile against Grampositive (MIC = 16 µg.mL-1) and Gram-negative bacteria (MIC = 8 µg.mL-1) similar to antimicrobials current on the market. The 3-acetyl-1-(2,5-dimethylphenyl)-1H-indole-4,7-dione derivative exhibited an important effect against different biofilm stages formed by a serious hospital life-threatening resistant strain of Methicillin-Resistant Staphylococcus aureus (MRSA). A hemocompatibility profile analysis based on in vitro hemolysis assays revealed the low toxicity effects of this new series. Indeed, in silico studies showed a good pharmacokinetics and toxicological profiles for all indolequinone derivatives, reinforcing their feasibility to display a promising oral bioavailability. An elucidation of the promising indolequinone derivatives binding mode was achieved, showing interactions with important sites to biological activity of S. aureus DNA gyrase. These results highlighted 3-acetyl-1-(2-hydroxyethyl)-1Hindole- 4,7-dione derivative as broad-spectrum antimicrobial prototype to be further explored for treating bacterial infections. Conclusion: The highly substituted indolequinones were obtained in moderate to good yields. The pharmacological study indicated that these compounds should be exploited in the search for a leading substance in a project aimed at obtaining new antimicrobials effective against Gram-negative bacteria.


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