scholarly journals Novel Diazenyl Containing Phenyl Styryl Ketone Derivatives As Antimicrobial Agents

2018 ◽  
Vol 17 (1) ◽  
pp. 28-38
Author(s):  
L. Sivasankerreddy ◽  
B. Nagamani ◽  
T. Rajkumar ◽  
M.S. Babu ◽  
N.Y. Subbaiah ◽  
...  

Background: Antibiotics play an important role in the treatment of infections to the humans and at the same time, irrational, frequent prescription of higher antibiotics, change in gene composition of microorganisms are all the reasons behind the development and introduction of new antibiotics against different microorganisms. Objective: In this project, an attempt has been made to synthesize some derivatives of diazenyl containing phenyl styryl ketones and also their in vitro screening was conducted against Mycobacterium tuberculosis, Escherichia coli, Klebsiella pneumonia, Bacillus subtilis, Staphylococcus aureus, Aspergillus niger and Candida albicans. Methods: Ten molecules were synthesized which are diazenyl containing chalcones. 4- aminoacetophenone was diazotised and piperidine was coupled with the formed diazonium chloride. Further, the acetoxy group underwent Claisen-Schmidt condensation with differently substituted aldehydes to form the final compounds- the chalcones. The proposed chemical structures were confirmed by different spectroscopic techniques like FTIR, 1H NMR and Mass spectroscopy. TLC was used to know that the reactants were exhausted and the formation of the product occurred. Sharp melting point of the compounds concludes the purity. Results: The MIC of the compounds 3CP, 3DP, 3EP and 3GP is 20 times the MIC of the standard fluconazole drug against Aspergillus niger. The compound 3GP is as equipotent as the standard drug Pyrazinamide with MIC of 3.12 µg/ml against Mycobacterium tuberculosis. Conclusion: The results are quite promising which on further studies may lead to drug molecules against different microorganisms. Especially, 3EP can be considered as a broad spectrum agent due to its potent activity against different microorganisms like Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia and Candida albicans.

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.


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.


2020 ◽  
Vol 16 (4) ◽  
pp. 514-520
Author(s):  
Marwa A. Sh. Shehab ◽  
Mohamed El-Naggar ◽  
Rabab A. Ismail ◽  
Hala M. El Kafrawy ◽  
Amira Abood ◽  
...  

Background: Amongst the quinolone core structures, 8-hydroxyquinoline (8-HQ or quinolinol) stands out as the greatest frequently used therapeutic moietiy. This includes the most critical molecules in medicinal chemistry. Quinolinol remains a broad-spectrum ligand capable of chelating to a large number of metal ions. Methods: The synthesized quinolinols Mannich bases were screened for their in vitro antimicrobial activity against Staphylococcus aureus (ATTCC 6538), Escherichia coli (ATTCC 7839), Klebsiella pneumonia (ATCC10131). The antifungal activity of the prepared compounds was assessed against Candida albicans (10231), Aspergillus niger and Penicillium sp. The antioxidant activity of the established compounds was assessed by means of α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method. Results: The antimicrobial outcomes indicated that all the synthesized compounds excluding 5 and 9b displayed reasonable antibacterial activity against Staphylococcus aureus (ATTCC 6538) and Escherichia coli (ATTCC 7839) with an inhibition zones ranging from 13 to 23 mm. However, in the case of Klebsiella pneumonia (ATCC10131) only compound 6 did not show any activity. The results also indicated that compounds 2b and 3 were the most potent antibacterial compounds against the verified strains with minimum inhibitory concentration (MIC) values ranging from 0.05 to 0.5mg/ml. In the antifungal assay, all compounds showed good activity against Candida albicans (10231) except compounds 5 and 9b. However, in the case of Aspergillus niger and Penicillium sp. only compounds 2b and 3 showed good activity. In the antifungal assay, MIC values for compounds 2b and 3 ranged from 0.25 to 2.5 mg/ml against the specified fungal strains. The antioxidant activity was assessed using the DPPH scavenging activity method. The results indicated that 2b was the most active among all tested compounds, with almost double the antioxidant activity as compared with that of trolox (positive control). Conclusion: In this work, we describe the synthesis of new Mannich bases comprising 8-HQ (1) and its derivative (8). The resulted Mannich bases of type 2 were used in transamination reactions with hydrazine and hydrazine derivatives. The structures of the newly synthesized Mannich bases were confirmed based on the NMR spectroscopic data and elemental analysis. Antimicrobial and antioxidant activities were also assessed.


2021 ◽  
Vol 6 (2) ◽  
pp. 102-106
Author(s):  
Gopal Senthilkumar ◽  
Chinnusamy Umarani ◽  
Dhurairaj Satheesh

A new organic compound, N-[4-(1,3-benzothiazol-2-ylcarbamoyl)-phenyl]pyrazine-2-carboxamide was synthesized through the reaction between 4-amino-N-(benzo[d]thiazol-2-yl)benzamide and pyrazine-2-carboxylic acid. The synthesized compound has been characterized by spectroscopic techniques such as 1H NMR, 13C NMR, FT-IR and mass spectroscopy. The synthesized compound was screened to antibacterial (Staphylococcus aureus, Klebsiella pneumonia and Escherichia coli), antifungal (Candida albicans and Aspergillus niger) activities. The anticancer activity of the title compound was also evaluated against MDA-MB-231 breast cancer cells.


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.


Author(s):  
O. G. Palmer ◽  
A. K. Onifade

Nosocomial infection is a rising problem in developing countries. Microorganisms Isolated from three private and public hospital environmental surfaces in Akure Metropolis, Ondo State, Nigeria were investigated in this study. Bacterial and fungal organisms were isolated and compared among the three hospitals. The study revealed that bacteria were the most predominant microorganisms found in the hospital environmental surfaces than fungi. Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Bacillus cereus were the bacterial isolates while fungi include Aspergillus fumigatus, Aspergillus niger and Candida albicans.  Staphylococcus aureus was found to be predominant bacteria but Aspergillus funmigatus was the predominant fungi. The result showed that the microbial loads of the public hospitals were higher than that of the private hospitals. The bacteria load of the male ward was found to be higher than that of the female ward while the fungal loads of each of the hospital environmental surfaces of female were higher than that of the male. The study revealed that bacteria were the most predominant microorganisms found in the hospital environment than fungi. Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Bacillus cereus were the bacterial isolates while fungi include Aspergillus fumigatus, Aspergillus niger and Candida albicans.  Staphylococcus aureus was found to be predominant bacteria. All the hospital environmental surfaces were contaminated with one or more microorganisms in the course of the research.


2004 ◽  
Vol 3 (1) ◽  
pp. 73-77 ◽  
Author(s):  
Slavica Ilic ◽  
Sandra Konstantinovic ◽  
Zoran Todorovic

Different extracts containing bioactive components and etheric oil of the flowers of Linum capitation kit. (Linacea) of Serbian origin were tested for an Antimicrobial activity against four bacteria (Staphylococcus aureus Escherichia coli, Bacillus subtilus, Pseudomonas aeruginosa), one mold (Aspergillus niger) and one yeast (Candida albicans). The isolated Flavonoids were also tested against Staphylococcus aureus, Escherichia coli Bacillus anhtracis, Pseudomonas aeruginosa, Aspergillus niger, Candida albicans and Herpes simplex virus type.


Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3220 ◽  
Author(s):  
Tahmina Monowar ◽  
Md. Rahman ◽  
Subhash Bhore ◽  
Gunasunderi Raju ◽  
Kathiresan Sathasivam

Antibiotic resistance is one of the most important global problems currently confronting the world. Different biomedical applications of silver nanoparticles (AgNPs) have indicated them to be promising antimicrobial agents. In the present study, extracellular extract of an endophytic bacterium, Pantoea ananatis, was used for synthesis of AgNPs. The synthesized AgNPs were characterized by UV–Vis spectroscopy, FTIR, transmission electron microscopy (TEM), scanning electron microscopy-energy dispersive X-ray spectroscopy (SEM-EDX), and Zeta potential. The antimicrobial potential of the AgNPs against pathogenic Staphylococcus aureus subsp. aureus (ATCC 11632), Bacillus cereus (ATCC 10876), Escherichia coli (ATCC 10536), Pseudomonas aeruginosa (ATCC 10145) and Candida albicans (ATCC 10231), and multidrug resistant (MDR) Streptococcus pneumoniae (ATCC 700677), Enterococcus faecium (ATCC 700221) Staphylococcus aureus (ATCC 33592) Escherichia coli (NCTC 13351) was investigated. The synthesized spherical-shaped AgNPs with a size range of 8.06 nm to 91.32 nm exhibited significant antimicrobial activity at 6 μg/disc concentration against Bacillus cereus (ATCC 10876) and Candida albicans (ATCC 10231) which were found to be resistant to conventional antibiotics. The synthesized AgNPs showed promising antibacterial efficiency at 10 µg/disc concentration against the MDR strains. The present study suggests that AgNPs synthesized by using the endophytic bacterium P. ananatis are promising antimicrobial agent.


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%.


Antibiotics ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 1158
Author(s):  
Abdelsamed I. Elshamy ◽  
Tarik A. Mohamed ◽  
Eman M. Elkady ◽  
Ibrahim A. Saleh ◽  
Ahmed A. El-Beih ◽  
...  

The organic extracts of the Red Sea soft coral Paralemnalia thyrsoides has led to the identification of two neolemnane-type sesquiterpenoids: paralemnolins X and Y (1, 2). In addition to these newly characterized compounds, ten known metabolites (3–12) were isolated. Previously reported compounds were elucidated by literature comparison of spectroscopic data (1D and 2D NMR as well as MS data). In vitro antimicrobial activity was investigated for compounds (1–12) against Staphylococcus aureus, Escherichia coli, Candida albicans and Aspergillus niger. Compound 5 showed antimicrobial activity against all assayed microorganisms.


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