scholarly journals Microwave-assisted Synthesis, Structural Characterization of Amino Pyridines, Pyrrolidine, Piperidine, Morpholine, Acetamides, and Assessment of Their Antibacterial Activity

Author(s):  
Abdulmajeed Alsamarrai ◽  
Saba Abdulghani

A sequence of new acetamide derivatives 9-15 of primary, secondary amine, and para-toluene sulphinate sodium salt have been synthesized under microwave irradiation and assessed in vitro for their antibacterial activity against one Gram-positive and two Gram-negative bacterial species such as S. pyogenes, E. coli, and P.mirabilis using the Mueller-Hinton Agar diffusion (well diffusion) method. The synthesized compounds with significant differences in inhibition diameters and MICs were compared with those of amoxicillin, ampicillin, cephalothin, azithromycin and doxycycline. All of the evaluated acetamide derivatives were used with varying inhibition concentrations of 6.25, 12.5, 37.5, 62.5, 87.5, 112.5 and 125 µg/ml. The results show that the most important antibacterial properties exercised by the synthetic compounds 9 and 11 bearing para-chlorophenyl moiety incorporated into the 2-position moiety of acetamide 2. The molecular structures of the new compounds were determined using FT-IR, 1H-NMR techniques.

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 533
Author(s):  
Abdulmajeed S. H. Alsamarrai ◽  
Saba S. Abdulghani

A series of new acetamide derivatives 22–28 of primary and secondary amines and para-toluene sulphinate sodium salt have been synthesized under microwave irradiation and assessed in vitro for their antibacterial activity against one Gram-positive and two Gram-negative bacterial species such as S. pyogenes, E. coli, and P. mirabilis using the Mueller-Hinton Agar diffusion (well diffusion) method. The synthesized compounds with significant differences in inhibition diameters and MICs were compared with those of amoxicillin, ampicillin, cephalothin, azithromycin and doxycycline. All of the evaluated acetamide derivatives were used with varying inhibition concentrations of 6.25, 12.5, 37.5, 62.5, 87.5, 112.5 and 125 µg/mL. The results show that the most important antibacterial properties were displayed by the synthetic compounds 22 and 24, both of bear a para-chlorophenyl moiety incorporated into the 2-position moiety of acetamide 1. The molecular structures of the new compounds were determined using the FT-IR and 1H-NMR techniques.


2020 ◽  
Vol 5 (2) ◽  
pp. 104
Author(s):  
Destri Khusnul Khotimah ◽  
I Wayan Arya Krishnawan Firdaus ◽  
Maharani Laillyza Apriasari

ABSTRACTBackground: Chronic periodontitis is an infectious disease that causes damage on periodontal ligament and alveolar bone. The severity of periodontitis is caused by several types of bacterial species which one of them is Porphyromonas gingivalis bacteria with a prevalence of 85% in oral cavity. The extract of kelakai leaf contained antibacterial in the form of flavonoid, alkaloid, tannin, and steroid. Flavonoid consists of some chemical compounds which is one of them is quercetin. The level of quercetin in kelakai leaf is 503.56 mgQE/g. From some secondary metabolites, kelakai leaf has inhibitory power toward gram negative bacterial, Porphyromonas gingivalis. Objective: This research was intended to know the activity of inhibitory power of kelakai leaf toward Porphyromonas gingivalis bacteria. Method: This research was an experimental research consisted of 5 experimental groups that were group of kelakai leaf extract on the concentrations of 100 mh/ml, 75 mg/ml, 50mg/ml, and 25 mg/ml and the control group (0.2% chlorhexidine). Each treatment was done in 4 repetitions. The test of inhibitory power used diffusion method by measuring the inhibitory zone around the growth of Porphyromonas gingivalis on Mueller Hinton Agar media. The data were analyzed by using One Way Anova 95% and then continued with LSD. Results: Based on the LSD test, it was known that the extract of Kelakai leaf had inhibitor power activity toward Porphyromonas gingivalis. The highest inhibitory zone was on the concentration of 100 mg/ml with inhibitory zone of 14.61 mm. Conclusion: The extract of kelakai leaf had inhibitory power activity toward Porphyromonas gingivalis bacteria in vitro. Keywords: 0.2% chlorhexidine, Diffusion method, Inhibitory power, Stenochlaena palustris extract, Porphyromonas gingivalis.


2021 ◽  
Vol 74 (9) ◽  
pp. 2109-2111
Author(s):  
Evheniia A. Shtaniuk ◽  
Oleksandra O. Vovk ◽  
Larisa V. Krasnikova ◽  
Yuliia I. Polyvianna ◽  
Tetiana I. Kovalenko

The aim: Study of antibacterial activity of the preparations, containing antiseptic dioxidine and antibiotic levofloxacin in vitro on standard strains of main optional-anaerobic pathogens of purulent-inflammatory processes of surgical wounds S. aureus, E. coli, P. aeruginosa and definition of more effective ones on them. Materials and methods: Solutions of dioxidine 1.2 %, dioxidine 1.2% with decamethaxin, Dioxisole, water soluble ointment with dioxidine 1.2% and levofloxacin 0.1% with decamethaxin were used in experiment. Antibacterial activity was studied on standard strains of S. aureus АТСС 25923, E. coli АТСС 25922, P. aeruginosa АТСС 27853. Distinguishing and identification of pure cultures of bacteria was done according to generally accepted microbiological methods. Determination of purulent-inflammatory processes pathogens sensitivity was done by disco-diffuse method on Mueller-Hinton medium. Antibacterial activity of solutions and ointments was studied with the help of agar diffusion method (“well” method) according to methodic recommendations. Each investigation was repeated 6 times. Method of variation statistics was used for the research results analysis. Results: All antibacterial preparations under study are effective and highly effective on S. aureus АТСС 25923, E. coli АТСС 25922, P. aeruginosa АТСС 27853. Solution with 1.2 % dioxidine with decamethaxin and ointment with 0.1 % levofloxacin and decamethaxin have larger growth retardation zones towards S. aureus and P. aeruginosa. E. coli strains are more sensitive to the solution of Dioxisole and ointment with 1.2 % dioxidine. Conclusions: All strains are sensitive, most of them are highly sensitive, up to 5 antibacterial preparations under study in vitro.


2018 ◽  
Vol 4 (3) ◽  
pp. 27-36 ◽  
Author(s):  
Irina Stepanenko ◽  
Semen Yamashkin ◽  
Yuliya Kostina ◽  
Alyona Batarsheva ◽  
Mikhail Mironov

Introduction. The problem of antibiotic resistance of microorganisms is becoming more urgent in the twenty-first century. Microorganisms possess an evolutionary adaptive capacity. Non-adherence to the basic principles of rational antibiotic therapy leads to menacing consequences. More and more pathogenic microbes are becoming resistant to two or more antibiotics. The search for new compounds with antimicrobial activity is one of the principles for overcoming the antibiotic resistance of microorganisms. Materials and methods. Eighteen test-strains of microorganisms and more than 2000 clinical strains of microorganisms, representating the families Micrococcaceae, Streptococcaceae, Enterobacteriaceae, Moraxellaceae, Pseudomonadaceae, Sphingomonadaceae, Xanthomonadaceae were studied for sensitivity to the compounds derived from 4-, 5-, 6- and 7-aminoindoles. A method of serial dilutions to determine the minimal inhibitory concentration (MIC) of the compounds under study was used in the study, as well as a disc diffusion method. Results and discussion. Sensitivity of the test-strains and of clinical strains of microorganisms to the resulting compounds was studied. The compounds based on substituted 4-, 5-, 6-, 7-aminoindoles showed different activity against the test strains and experimental strains of microorganisms in vitro. It was found that the marked antibacterial activity was exhibited by the compounds containing a trifluoromethyl group. The most significant activity was noted in amides and pyrroloquinolones based on 4-aminoindole, 6-aminoindole and 7-aminoindole.The most effective compounds with laboratory codes 5D, 7D, 39D, S3, HD, 4D showed a pronounced antibacterial activity. Conclusion. Antimicrobial activity of the substituted amides and pyrroloquinolines on the basis of 4-, 5-, 6-, 7-aminoindoles was etermined in our study, as well as the spectra of their action against Gram-positive and Gram-negative microorganisms, which are causative agents of non-specific and certain specific human infectious diseases. Moreover, we evaluated the synthetic potentials of the substituted 4-, 5-, 6-, 7-aminoindoles as the starting compounds for synthesizing a series of indolylamides and pyrroloquinolines. Also, the prospects for targeted synthesis of biologically active compounds based on indole-type aromatic amines were determined.


2021 ◽  
Vol 10 (1) ◽  
pp. 16
Author(s):  
Saskia Arientika Wahyuningrum ◽  
Meiskha Bahar ◽  
Andri Pramesyanti Pramono

Pneumonia is a lung parenchymal infection caused by Pseudomonas aeruginosa.It is Gram negative bacteria that have developed antibiotic resistance. Actinomycetes are Gram-positive bacteria that produce secondary metabolites which have the ability as antimicrobial. Objectives: To identified the ability of Actinomycetes isolates to inhibit the growth of the bacterium Pseudomonas aeruginosa ATCC 27853. The samples in this experiment were from Kebun Raya Bogor that had been rejuvenated on Starch Casein Agar (SCA). Methods: Six dilution series 10-1; 10-2; 10-3; 10-4; 10-5; 10-6 Actinomycetes isolates were used to observe the inhibition zone of P.aeruginosa growth on Mueller Hinton Agar (MHA) media by diffusion method. Results: The effective incubation time occurred at 24 hours, and then it resulted in the average clear zone diameter of 14.70 mm, 10.57 mm, 8.53 mm, 8.47 mm, 6.97 mm, and 5.30 mm. The results of the One – Way Anova test with p-value = 0.000 (p < 0.005) showed some differences at each concentration to inhibit the growth of P.aeruginosa ATCC 27853 at 24 hours incubation period. Conclusion: The most effective concentration of Actinomycetes isolates that can potentially be antibacterial was the concentration of 10-1 with potential solid inhibitory power.Keywords: Actinomycetes, antibacterial, Pseudomonas aeruginosa


Author(s):  
Preeja K. Sundaresan ◽  
Kala P. Kesavan

Background: Sphaeranthus indicus Linn is a widely used medicinal plant in Indian traditional system of medicine against human pathogens. Alarming bacterial resistance is urging scientist to search for newer anti-microbial substances from the medicinal plants. The objective of the study was to evaluate the antibacterial activity of ethanolic extract of the whole plant Sphaeranthus indicus Linn (Asteraceae).Methods: The antibacterial activity of ethanolic extract of whole plant of Sphaeranthus indicus Linn was done against Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Staphylococcus aureus in Mueller Hinton Agar (MHA) and compared with ciprofloxacin as standard by disc diffusion method.Results: The study revealed that there was no zone of inhibition in doses of 100 mcg, 200 mcg and 300 mcg of ethanolic whole plant extract of Sphaeranthus indicus in MHA plates compared with ciprofloxacin 30 mcg.Conclusions: Ethanolic extract of Sphaeranthus indicus does not have antibacterial activity. Further studies are needed in different extracts and parts of the plant. Simultaneous studies can be done in different places to evaluate environmental factors and regional variations.


2018 ◽  
Vol 17 (2) ◽  
pp. 197-203
Author(s):  
Tina Rostinawati ◽  
Ami Tjitraresmi ◽  
Myra Vania Wisnuputri

Methicillin-resistant Staphylococcus aureus (MRSA) is the most common bacteria causing nosocomial infections with high levels of resistance to available antibiotics. So, it is necessary to search for new compounds to solve this problem. Various studies showed antibacterial activity of rambutan peel but for Rambutan Binjai peel extract that are from Indonesia has never been studied against the MRSA. This study aims to determine the antibacterial activity, the value of minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) using agar diffusion method. The concentration of rambutan peel ethanol extract at as much as 62.5 mg/ml showed the inhibitory diameter i.e 21.3 ± 2.4 mm. MIC and MBC were in the same range, which was between 0.98 (mg/ml) to 1.95 (mg/ml). The activity strength of tetracycline against the extract was at 1:50. This revealed that Rambutan Binjai peel extract had great potency as antibacterial agent to MRSA. Dhaka Univ. J. Pharm. Sci. 17(2): 197-203, 2018 (December)


2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Adel S. Al-Zubairi ◽  
Ahmad Bustamam Abdul ◽  
Siddig Ibrahim Abdelwahab ◽  
Chew Yuan Peng ◽  
Syam Mohan ◽  
...  

The use of evidence-based complementary and alternative medicine is increasing rapidly.Eleucine indica(EI) is traditionally used in ailments associated with liver and kidneys. The therapeutic benefit of the medicinal plants is often attributed to their antioxidant properties. Therefore, the aim of this study was to screen the hexane, dicholoromethane, ethyl acetate (EA) and methanol extracts (MeTH) of EI for their antioxidant, antibacterial and anti-cancer effects using total phenolic contents (TPCs) and DPPH, disc diffusion method and MTT cytotoxicity assays, respectively. The MeTH was showed to have the highest TPC and scavenging activity (77.7%) on DPPH assay, followed by EA (64.5%), hexane (47.19%) and DCM (40.83%) extracts, whereas the MeTH showed no inhibitory effect on all tested bacteria strains. However, the EA extract exhibited a broad spectrum antibacterial activity against all tested bacteria exceptBacillus subtilis, in which this bacterium was found to be resistant to all EI extracts. Meanwhile, hexane extract was demonstrated to have a remarkable antibacterial activity against methicillin resistantStaphylococcus aureus(MRSA) andPseudomonas aeruginosa, while the dicholoromethane extract did not exhibit significant activity againstP. aeruginosa. None of the extracts showed significant cytotoxic activity towards MCF-7, HT-29 and CEM-SS human cancer cell lines after 72 h incubation time (IC50> 30 μg/ml). These results demonstrate that the extract prepared from the EI possesses antioxidant activityin vitroin addition to antibacterial properties. Further investigations are needed to verify the antioxidant effectsin vitroandin vivo.


Author(s):  
Resmi Mustarichie ◽  
Sri Agung Fitri ◽  
Danni Ramdhani

Objective: This study aims to determine the antibacterial activity of ethanol extract of bay (Syzygium polyanthum W.) and suji (Dracaena angustifoliaRoxb.) leaves against Shigella dysenteriae and the amount of potassium to the discovery of anti-dysentery drug candidates.Methods: Testing activities and comparative value activities performed by the agar diffusion method, whereas the determination of minimum bactericidal concentration (MBC) was done with the subculture media incubation test followed with microdilution method on Mueller Hinton Agar medium sterile. Potassium levels of the extract were carried out quantitatively using atomic absorption spectrophotometry.Results: The test results showed that the ethanol extract of both leaves had antibacterial activity against S. dysenteriae with MBC values were in the range of 10-20% w/v. Value comparative effectiveness suji leaf ethanol extract to the bay leaf was 1:0.4. Potassium levels ethanol extract of bay and suji leaves were 1.027% and 3.795%, respectively.Conclusion: It can be concluded that the ethanol extract of bay and suji leaves has antibacterial activity against bacteria S. dysenteriae ATCC 13313. Rated comparative activity of the ethanol extract of the suji leaves with bay leaves ethanol extract was 1:0.4 which means to generating resistor diameter equal to 1 part suji leaf ethanol extract equivalent to 0.4 parts of the ethanol extract of bay leaves. The minimum kill concentration ethanol extract of bay and suji leaves ethanol extract was in the range of 10-20% w/v. Both bay and suji leaves have potential as a supplier of potassium in patients with hypokalemia dysentery.Keywords: Bay leaves, Suji leaves, Shigella dysenteriae, Potassium, Atomic absorption spectrophotometry. 


2016 ◽  
Vol 60 (1) ◽  
pp. 5-18 ◽  
Author(s):  
Lia M. Junie ◽  
Mihaela L. Vică ◽  
Mirel Glevitzky ◽  
Horea V. Matei

AbstractThe first aim of the study was to compare the antibacterial activity of several types of honey of different origins, against some bacterial resistant strains. The strains had been isolated from patients. The second aim was to discover the correlations between the antibacterial character of honey and the physico-chemical properties of the honey. Ten honey samples (polyfloral, linden, acacia, manna, and sunflower) from the centre of Romania were tested to determine their antibacterial properties against the following bacterial species: Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, Salmonella enterica serovar Typhimurium, Bacillus cereus, Bacillus subtilis, and Listeria monocytogenes. Bacterial cultures in nutrient broth and the culture medium Mueller-Hinton agar were used. The susceptibility to antibiotics was performed using the disk diffusion method. All honey samples showed antibacterial activity on the isolated bacterial strains, in particular polyfloral (inhibition zone 13-21 mm in diameter) - because it is the source of several plants, and manna (inhibition zone 13-19.5 mm in diameter), and sunflower (inhibition zone 14-18.5 mm in diameter). Pure honey has a significant antibacterial activity against some bacteria which are resistant to antibiotics. Bacterial strains differed in their sensitivity to honeys. Pseudomonas aeruginosa and Staphylococcus aureus were the most sensitive. The present study revealed that honey antibacterial activity depends on the origin of the honey. We also found that there was a significant correlation between antibacterial activity of honeys and the colour of the honey but not between acidity and pH. The statistical analysis showed that the honey type influences the antibacterial activity (diameter of the bacterial strains inhibition zones).


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