scholarly journals BIOLOGICAL ACTIVITY OF N-{3-[(4-METHYLBENZENE-1- SULFONYL)IMINO]-6-OXOCYCLOHEXA-1,4-DIEN-1-YL}ARYLAMIDES AND THEIR DERIVATIVES

2021 ◽  
Vol 26 (1(77)) ◽  
pp. 37-47
Author(s):  
S. A. Konovalova ◽  
A. P. Avdeenko ◽  
V. I. Lubenets ◽  
O. Z. Komarovska-Porokhnyavets ◽  
I. Yu. Yakymenko ◽  
...  

N-{3-[(4-Methylbenzene-1-sulfonyl)imino]-6-oxocyclohexa-1,4-dien-1-yl}arylamides and their derivatives were synthesized by the reaction of the corresponding N-(4-oxocyclohexa-2,5-dien-1-ylidene)arylsulfonamides with N-chloramides. The biological activity of the synthesized compounds was studied on test cultures of Escherichia coli 67, Staphylococcus aureus 209-p, Mycobacterium luteum VKM B-868 and fungi Candida tenuis VKM Y-70, Aspergillus niger VKM F-1119 by the method of diffusion of substances into agar on a solid nutrient medium. The degree of activity of the test compounds was determined by the diameter of the zones of inhibition of growth of test cultures of microorganisms. The minimum inhibitory, bactericidal and fungicidal concentrations were determined by the method of serial dilutions of the substance in a liquid nutrient medium. At the studied concentration, the method of diffusion of substances into agar on a solid nutrient medium has shown that these compounds have low activity against bacteria Escherichia coli, Staphylococcus aureus, Mycobacterium luteum and fungi Candida tenuis, Aspergillus niger. The diameters of the zones of inhibition of growth of test cultures of microorganisms were less than 15 mm. In research by the method of serial dilutions of the substance in a liquid nutrient medium, they have been found to have bactericidal and fungicidal activity. The minimum inhibitory concentration of N-{2-hydroxy-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide was 31.2 μg/ml against bacteria Mycobacterium luteum. The minimum inhibitory concentration of N-{2-hydroxy-3-methyl-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide against fungi Aspergillus niger was 31.2 μg/ml. The minimum bactericidal concentration of N-{2-hydroxy-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide was 62.5 μg/ml against bacteria Mycobacterium luteum. Minimum fungicidal concentration of N-{3-[(4-methylbenzene-1-sulfonyl)imino]-6-oxocyclohexa-1,4-dien-1-yl}benzamide and N-{2-hydroxy-3-methyl-5-[(4-methylbenzene-1-sulfonyl)amino]phenyl}benzamide was 62.5 μg/ml in action to mold fungi Aspergillus niger.

2019 ◽  
Vol 807 ◽  
pp. 141-150
Author(s):  
Lin Yuan ◽  
Xue Ren Qian

Zeolite powders were first treated with hydrochloric acid, then reacted with sodium chloride, and sodium zeolite (Na-Zeolite) powders were obtained. Further Antibacterial zeolite powders were prepared by loading metal ions such as, Ag+ and Zn2+, Ag+ and Cu2+, Zn2+and Cu2+, Ag+ and Cu2+and Zn2+, through ion exchange. The powders were characterized by minimum Inhibitory concentration (MIC), SEM/EDXA and XRD. Antibacterial paper with antibacterial zeolite powders as filler was fabricated. The results demonstrated that MIC of loading (Ag++Zn2+) zeolite was 125ppm against Staphylococcus aureus and Escherichia coli . MIC of loading (Ag++Cu2++Zn2+) zeolite was 62.5ppm against Candida albicans and Aspergillus Niger. By adding 6% of (Ag++Zn2+), (Ag++Cu2+), and (Ag++Cu2++Zn2+) antibacterial zeolite powders, respectively, antibacterial paper were prepared; and the antibacterial rate of these papers against Staphylococcus aureus, Escherichia coli, Candida albicans and Aspergillus Niger for 4h is close to 100%.


2020 ◽  
Vol 24 (2) ◽  
pp. 249-252
Author(s):  
E.I. Oikeh ◽  
F.E. Oviasogie ◽  
E.S. Omoregie

The antibacterial activities of fresh Citrus sinensis seed oil and non-oil  extract are investigated in this study. Gram positive (Staphylococcus aureus and Enterococcus faecalis) and Gram negative (Pseudomonas aeruginosa, Escherichia coli and Salmonella spp.) bacterial strains are used in this study and antibacterial activity is estimated using the agar well diffusion method. Zones of inhibition were measured and the minimum inhibitory concentration and minimum bacteriostatic concentrations were determined. The results show that the non-oil extract had better antibacterial activities against Staphylococcus aureus, Enterococcus faecalis and Escherichia coli compared to the oil extract (zones of inhibition at 200 μg/ml of 12 mm, 8 mm and 2 mm respectively for the nonoil extract; 4 mm, 6 mm, 0 mm respectively for the seed oil). The seed oil however had better antibacterial activity compared to the non-oil extract in Salmonella spp. (zones of inhibition at 200 μg/ml of 8 mm for the seed oil compared to 4 mm for the non-oil extract). Pseudomonas aeruginosa showed similar susceptibility to both extracts at both concentrations studied (zones of inhibition of 4 mm and 2 mm for both extracts at 200 μg/ml and 100 200 μg/ml respectively). Minimum inhibitory concentrations ranged from 50 – 100 μg/ml while minimum bacteriostatic concentrations ranged from 100 – 200 μg/ml. We conclude from our findings that both extracts hold promise in the development of antimicrobial therapeutics. Keywords: Citrus sinensis, Antibacterial, minimum inhibitory concentration, minimum bacteriostatic concentration


Author(s):  
Rubal C Das ◽  
Rajib Banik ◽  
Robiul Hasan Bhuiyan ◽  
Md Golam Kabir

Macrophomina phaseolina is one of the pathogenic organisms of gummosis disease of orange tree (Citrus reticulata). The pathogen was identified from the observation of their colony size, shape, colour, mycelium, conidiophore, conidia, hyaline, spore, and appressoria in the PDA culture. The crude chloroform extracts from the organism showed antibacterial activity against a number of Gram positive and Gram-negative bacteria. The crude chloroform extract also showed promising antifungal activity against three species of the genus Aspergillus. The minimum inhibitory concentration (MIC) of the crude chloroform extract from M. phaseolina against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, and Shigella sonnie were 128 ?gm, 256 ?gm, 128 ?gm and 64 ?gm/ml respectively. The LD50 (lethal dose) values of the cytotoxicity assay over brine shrimp of the crude chloroform extract from M. phaseolina was found to be 51.79 ?gm/ml. DOI: http://dx.doi.org/10.3329/cujbs.v5i1.13378 The Chittagong Univ. J. B. Sci.,Vol. 5(1 &2):125-133, 2010


2020 ◽  
Vol 15 (6) ◽  
pp. 665-679
Author(s):  
Alok K. Srivastava ◽  
Lokesh K. Pandey

Background: [1, 3, 4]oxadiazolenone core containing chalcones and nucleosides were synthesized by Claisen-Schmidt condensation of a variety of benzaldehyde derivatives, obtained from oxidation of substituted 5-(3/6 substituted-4-Methylphenyl)-1, 3, 4-oxadiazole-2(3H)-one and various substituted acetophenone. The resultant chalcones were coupled with penta-O-acetylglucopyranose followed by deacetylation to get [1, 3, 4] oxadiazolenone core containing chalcones and nucleosides. Various analytical techniques viz IR, NMR, LC-MS and elemental analysis were used to confirm the structure of the synthesised compounds.The compounds were targeted against Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and Aspergillus flavus, Aspergillus niger and Fusarium oxysporum for antifungal activity. Methods: A mixture of Acid hydrazides (3.0 mmol) and N, Nʹ- carbonyl diimidazole (3.3 mmol) in 15 mL of dioxane was refluxed to afford substituted [1, 3, 4]-oxadiazole-2(3H)-one. The resulted [1, 3, 4]- oxadiazole-2(3H)-one (1.42 mmol) was oxidized with Chromyl chloride (1.5 mL) in 20 mL of carbon tetra chloride and condensed with acetophenones (1.42 mmol) to get chalcones 4. The equimolar ratio of obtained chalcones 4 and β -D-1,2,3,4,6- penta-O-acetylglucopyranose in presence of iodine was refluxed to get nucleosides 5. The [1, 3, 4] oxadiazolenone core containing chalcones 4 and nucleosides 5 were tested to determined minimum inhibitory concentration (MIC) value with the experimental procedure of Benson using disc-diffusion method. All compounds were tested at concentration of 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, 0.62 mg/mL, 0.31 mg/mL and 0.15 mg/mL for antifungal activity against three strains of pathogenic fungi Aspergillus flavus (A. flavus), Aspergillus niger (A. niger) and Fusarium oxysporum (F. oxysporum) and for antibacterial activity against Gram-negative bacterium: Escherichia coli (E. coli), and two Gram-positive bacteria: Staphylococcus aureus (S. aureus) and Bacillus subtilis(B. subtilis). Result: The chalcones 4 and nucleosides 5 were screened for antibacterial activity against E. coli, S. aureus and B. subtilis whereas antifungal activity against A. flavus, A. niger and F. oxysporum. Compounds 4a-t showed good antibacterial activity whereas compounds 5a-t containing glucose moiety showed better activity against fungi. The glucose moiety of compounds 5 helps to enter into the cell wall of fungi and control the cell growth. Conclusion: Chalcones 4 and nucleosides 5 incorporating [1, 3, 4] oxadiazolenone core were synthesized and characterized by various spectral techniques and elemental analysis. These compounds were evaluated for their antifungal activity against three fungi; viz. A. flavus, A. niger and F. oxysporum. In addition to this, synthesized compounds were evaluated for their antibacterial activity against gram negative bacteria E. Coli and gram positive bacteria S. aureus, B. subtilis. Compounds 4a-t showed good antibacterial activity whereas 5a-t showed better activity against fungi.


2011 ◽  
Vol 8 (3) ◽  
pp. 1456-1461 ◽  
Author(s):  
Donatus Ebere Okwu ◽  
Fred Uchenna Nnamdi

Phenenthrene alkaloid identified as 1-ethanamino 7 hex-1-yne-5I-one phenanthrene was isolated from the ethanolic extract of the leaves ofBryophyllum pinnatum(syn. B. calcinum kalanchoe pinnata) a versatile Nigeria medicinal plant. The structure was elucidated using NMR, IR, UV and MS spectral data. Antimicrobial studies showed that the isolated compound successfully inhibitedPsuedomonas aeruginosa, Klebsiella pneumonia, Staphylococcus aureus, Escherichia coli, Candida albicansandAspergillus niger. This result authenticates the use ofbryophyllum pinantumin phytomedicine for disease prevention and treatment of infections.


2012 ◽  
Vol 5 (1) ◽  
pp. 135-141
Author(s):  
M. Waziri ◽  
J. S. Suleiman

The evaporated extract of cow dung is traditionally used in Northern Nigeria and Cameroun as food additive and in treatment of infectious diseases. In this study, the cow dung ash extract was prepared and tested for some elemental contents as well as the antimicrobial activity against Cyanobacteria (C.bacteria), Staphylococcus aureus (S.aureus), Bacillus subtilis (B.subtilis) and Escherichia coli (E.coli) using different analytical techniques. The extract was highly basic with pH of 11.7 and the elements vary in the following decreasing order of concentration; K>Na>Mg>Ca>Fe>Al>Zn.  S. aureus was the most sensitive bacteria with minimum inhibitory concentration (MIC) value of 0.082 mg/mL while B. subtilis was the least sensitive with MIC value of 4.3 mg/mL. The result of this study indicate that the extract can supplement the dietary Na and K requirements for the users and supports the folkloric use of the extract in treatment of infections.© 2013 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v5i1.11962        J. Sci. Res. 5 (1), 135-141 (2013)


1983 ◽  
Vol 38 (1-2) ◽  
pp. 151-152 ◽  
Author(s):  
Ferdinand Devínsky ◽  
Ivan Lacko ◽  
Ludovít Krasnec ◽  
Dušan Mlynarčík

Antimicrobial activity of N,N′-bis(decylmethyl)-α,ω-alkanediamine dioxides determined on Staphylococcus aureus, Escherichia coli, and Candida albicans is presented as minimal inhibitory concentration (MIC). The effect of the length of linking alkylene chain on this activity has been followed.


Author(s):  
N. I. Popov ◽  
◽  
A. V. Suvorov ◽  
S. M. Lobanov ◽  
S. A. Michko ◽  
...  

The article describes the results of laboratory tests of the effectiveness of the disinfectant Monochloride (Iodine chloride) 2%. Laboratory studies were carried out on test objects and test surfaces contaminated with test cultures of microorganisms, which included museum cultures of E. coli (E. coli 1257), S. aureus 209-P, mycobacteria (pcs. B5), and spores (B. cereus pieces. 96). Disinfection of test objects was carried out by the method of irrigation at a consumption rate of 0,25...0,3 l/ m2 with disinfection of smooth surfaces and 0,5 l/m2, with disinfection of rough surfaces. The treatment was performed twice with an interval of 60 minutes. Our work established that the Monochloride (Iodine chloride) 2% has a high disinfectant activity against Escherichia coli, Staphylococcus aureus, mycobacteria and spores. On the basis of the laboratory work, this tool can be recommended for production tests at veterinary surveillance facilities.


Author(s):  
Haribhai Rabari ◽  
Hetal Vankar ◽  
Beenkumar Prajapati

The emergence of multidrug microbial resistance is the main challenges that the modern scientists have so far been facing in the recent era. In this respect, new series of drug classes having potential to give antimicrobial effect have been synthesized. A new series of 5- substituted-1,10 b-dihydroimidazole[1,2-c]quinazoline derivatives 8a-e have been synthesized and screened for antibacterial activity and antifungal activity. Synthesized derivatives were characterized by IR, MASS and 1H-NMR spectroscopy. Synthesized compounds show good activity, which was comparable to the standard drug and it can be useful for the further clinical study. Antibacterial activity was evaluated against four different pathogenic bacterial strains like Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Pseudo-monas aeruginosa. Among the screened compounds, 8e show good antibacterial activity against Staphylococcus aureus and Escherichia coli with MIC of 50 and 100 μg/ml respectively. Antifungal activity was evaluated  against two strains of fungi. Among the synthesized derivates, compound 8c was emerged out as the potent antifungal compound against Candida albicans and Aspergillus niger with MIC of 25 μg/ml and 75μg/ml respectively. Compound 8e also shows good antifungal activity with MIC of 50 μg/ml against both Candida albicans and Aspergillus niger. The overall results of this study indicated that  synthesized quinazoline derivatives had the potential to act as an antibacterial and antifungal agent, hence further investigation is warranted.


2010 ◽  
Vol 13 (2) ◽  
pp. 46-50
Author(s):  
Dini Kurnia Wisatya ◽  
Purbowatiningrum Ria Sarjono ◽  
Nies Suci Mulyani

Telah dilakukan penelitian tentang pengaruh pemanasan pada proses pembuatan ekstrak kulit buah manggis (Garcinia mangostana Linn) terhadap aktivitas antimikroba. Metode yang digunakan adalah metode pemanasan pada proses pembuatan ekstrak kulit buah manggis sedangkan metode cakram kertas dan metode berat kering digunakan pada uji antimikroba. Mikroba yang diuji menggunakan, bakteri Escherichia coli, Staphylococcus aureus, khamir Candida albicans, dan jamur Aspergillus niger. Metode cakram kertas untuk mengidentifikasi aktivitas antimikroba pada bakteri Escherichia coli, Staphylococcus aureus, khamir Candida albicans, sedangkan metode berat kering digunakan untuk identifikasi aktivitas antimikroba dari jamur Aspergillus niger. Konsentrasi Hambat Minimum pada metode cakram kertas pada mikroba bakteri Escherichia coli, Staphylococcus aureus, khamir Candida albicans yaitu 5 % (w/v), dengan rata-rata luas zona hambat masing-masing 0,043 cm2, 0,018 cm2, 0,013 cm2. Sedangkan pada jamur Aspergillus niger pada konsentrasi 0,5% (w/v), dengan berat kering 0,06 gram.


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