SYNTHESIS AND ANTIMICROBIAL EVALUATION OF SOME NEW OXAZINE DERIVATIVES DERIVED FROM COUMARINYL CHALCONES

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (10) ◽  
pp. 19-24
Author(s):  
Katte I. Bhat ◽  
Abhishek Kumar ◽  
Alafiya A. Matcheswala ◽  
Pankaj Kumar ◽  

A series of novel substituted 3-(2-amino-6-phenyl-6H-1,3-oxazin-4-yl)-2H-chromen-2-ones(AO1-AO10) was synthesized upon refluxing ethanolic solution of substituted 3-cinnamoyl-2H chromen-2-one with urea in presence of 20 % NaOH. The intermediate chalcones, substituted 3-cinnamoyl-2H-chromen2-ones, were synthesized by condensing 3-acetyl coumarin with various substituted benzaldehydes in presence of 20 % NaOH. The structures of the final synthesized compounds were characterized by UV, IR, 1 H NMR and mass spectra. The antibacterial activity of the synthesized compounds was estimated by tube dilution method. The turbidity was observed for the synthesized compounds. Few compounds showed promising minimum inhibitory concentration by tube dilution method.

Author(s):  
Na Li ◽  
Jiang-Kun Dai ◽  
Dan Liu ◽  
Jin-Yi Wang ◽  
Jun-Ru Wang

Natural products are an important source of antibacterial agents. Canthin-6-one alkaloids have displayed potential antibacterial activity based on our previous work. In order to improve the activity, twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by double dilution method. Four compounds (6f, 6i, 6p and 6t) displayed 2-fold superiority (minimum inhibitory concentration (MIC) = 3.91 µg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae than agrochemical propineb. Moreover, the structure–activity relationships (SARs) were also carefully summarized in order to guide the development of antibacterial canthin-6-one agents.


Author(s):  
Hidayatullah Hidayatullah ◽  
Syariful Anam ◽  
Muhamad Rinaldhi Tandah

Bamban (Donax canniformis (G. Forst.) K. Schum.) is one of the family Marantaceae plant that has many uses such as traditional medicine. Methanol extract of bamban leaves contains phenolic, tannins and saponins compounds. The purpose of this research is to determine the class of compounds that has antibacterial activity against Staphylococcus aureus and determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) methanol extract of bamban leaves. This extract was prepared using maceration method with methanol solvent. Determination the class of compounds was initiated by bioautografi test in order to determine spots which has have antibacterial activity. Subsequently, the spot were identified the class of compound using reagent spray FeCl3 and H2SO4 10%. The determination of MIC and MBC using dilution method. Research showed there are three compounds that had antibacterial activity. These compounds were predicted as spot I and spot II which were phenolic compounds and spot III as a saponin compound. MIC and MBC value of the methanol extract of leaves bamban leaves 8% and 13%, respectively.


PHARMACON ◽  
2020 ◽  
Vol 9 (2) ◽  
pp. 226
Author(s):  
Garry Clements ◽  
Paulina V. Y. Yamlean ◽  
Widya Astuty Lolo

ABSTRACTCelery herbs (Apium graveolens L.) have content flavonoid, saponin and tannin. Flavonoids have anti-inflammatory properties, antioxidants and antibacterials. This study aims to determine whether the ethanol extract of celery herbs can be formulated into cream preparations, test the quality of preparations at concentrations of 5%, 10% and 15%. These methods of research are experimental laboratories by making the supply of self-sustaining herbal celery ethanol extract cream and testing the quality of the cream preparation,  as well as testing of antibacterial activity was carried out using the liquid dilution method and measuring value of  Minimum Inhibitory Concentration  and Minimum Bactericidal Concentration using a UV-Vis Spectrophotometer. This research shows that celery herbs ethanol extract can be formulated into cream preparations, fulfilling quality test of organoleptic, scatter power, adhesion and cycling test, but that doesn’t meet the requirements for homogeneity tests and pH tests and has antibacterial activity which not only inhibits but kills bacteria in preparations of 5% and 15%Keywords: Cream Celery herb extract, Antibacterial, Staphylococcus aureus, UV-Vis spectrophotometer ABSTRAK Herba Seledri (Apium graveolens L.) memiliki kandungan flavonoid, saponin dan tannin. Flavonoid memiliki khasiat sebagai antiinflamasi, antioksidan dan antibakteri. Penelitian ini bertujuan untuk mengetahui apakah ekstrak etanol herba Seledri dapat diformulasikan menjadi sediaan krim, menguji mutu sediaan pada konsentrasi 5%, 10% dan 15%. Metode penelitian ini experimental laboratorium dengan membuat Sediaan Krim Ekstrak Etanol Herba Seledri dan menguji mutu sediaan krim, serta   menguji aktivitas antibakteri menggunakan metode dilusi cair dan mengukur nilai KBM dan KHM menggunakan Spektrofotometer UV-Vis. Hasil penelitian menujukkan bahwa ekstrak etanol herba Seledri dapat diformulasikan menjadi sediaan krim, memenuhi uji mutu sediaan organoleptik, daya, sebar, daya hambat dan stabilitas  namun tidak memenuhi persyaratan untuk uji homogenitas dan uji pH serta mempunyai aktivitas antibakteri yang membunuh bakteri pada sediaan berkonsentrasi 5% dan 15%.Kata Kunci : Krim Ekstrak herba Seledri, Antibakteri, Staphylococcus aureus, Spektrofotometer UV-Vis


Author(s):  
Zahra Shahidi ◽  
Shiva Tavakol Davani ◽  
Faranak Noori ◽  
Masoumeh Hasani Tabatabaei ◽  
Fatemeh Sodeif ◽  
...  

Objectives: Toothpastes and mouthwashes contain chemicals that may be harmful to oral tissues. This study assessed the cytotoxicity and antibacterial activity of toothpastes and compare the Iranian and foreign toothpastes and mouthwashes available in the Iranian market in this respect. Materials and Methods: Twenty samples (13 toothpastes and 4 mouthwashes) were selected. The cytotoxicity of 1, 10, and 50 mg/mL of toothpastes and 0.05, 2 and 10 µL of mouthwashes was measured after 1, 15 and 30 min of exposure to human gingival fibroblasts, each in triplicate. The methyl thiazolyl tetrazolium (MTT) assay was used for cytotoxicity testing. The serial dilution method was utilized to determine the minimum inhibitory concentration (MIC) of each sample against Lactobacillus acidophilus (L. acidophilus) and Streptococcus mutans (S. mutans). Two-way ANOVA and Tukey’s test were used for data analysis. Results: A significant difference in cytotoxicity was noted among different products (P=0.00). The difference in cytotoxicity of each sample was not significant at 1, 15 and 30 min (P=0.08). The obtained MIC for all toothpastes and mouthwashes was between 0.0039 mg/mL and 0.0156 mg/mL, except for Sensodyne toothpaste and Oral B mouthwash. Conclusion: Some brands of toothpastes have higher cytotoxicity due to their composition, and their cytotoxicity should not be overlooked. The antibacterial activity of the samples was almost equal when they were in contact with L. acidophilus and S. mutans except for the Irsha mouthwash, Sehat, Darugar and Bath toothpastes. The antibacterial effect of toothpastes and mouthwashes increased with an increase in exposure time.


2016 ◽  
Vol 6 (2) ◽  
pp. 99
Author(s):  
Tri Desiana KH ◽  
Achmad Sudirman ◽  
Devi Eka Juniarti

Background. Enterococcus faecalis is an anaerobic facultative gram-positive bacteria which contribute to the failure of root canal treatment with the number of prevalence 24% to 77%. At the preparation stage, a material for irrigation which has antibacterial activity to Enterococcus faecalis is needed. Phyllantus niruri linn is one of herbal medicament which is potential as antibacterial agent as it contains active antibacterial chemical-compound. Purpose. The purpose of the study is to identify Minimum Inhibitory Concentration and Minimum Bactericidal Concentrationof Phyllantus niruri linn against Enterococcus faecalis.Method. The research method used is laboratory experimental. Enterococcus faecalis ATCC 29212 was suspended into several concentration of Phyllantus niruri linn extract from dilution method on BHIB medium. Each tube was incubated for 24 hours. Then, each tube was subcultured to Nutrient agar medium using spreader in a petridish. Each petridish was incubated for 24 hours and the growth of the colony was manually calculated using CFU/ml unit. Result. At the concentration of 6.25%, Phyllanthus niruri linn was able to inhibit the growth of Enterococcus faecalis as 90% and there was no bacteria at the concentration of 12.5%. Conclusion. 6.25% concentration of Phyllanthus niruri linn extract was Minimum Inhibitory Concentration and 12.5% concentration was Minimum Bactericidal Concentration to Enterococcus faecalis.


2015 ◽  
Vol 73 (3) ◽  
pp. 759-762
Author(s):  
Wan-Qing Cheng ◽  
Zhen-Jian Zhang ◽  
Chuan-Bin Cao ◽  
Xiao-Wen Ye ◽  
Wang-Ping Pan ◽  
...  

Abstract A research on Jinyulian Oral Solution was conducted and the objectives were to discover its possible acute toxicity and antibacterial effects when used in vitro and in vivo. Regarding the acute toxicity test, Kunming mice were fed a maximum amount of the solution as their stomachs could hold, i.e., 40 mL kg−1. To ascertain the minimum inhibitory concentration (MIC) of the solution, two types of germs, i.e., Staphylococcus aureus and Escherichia coli, were selected and tube dilution method was adopted. An antibacterial experimental model relying on animals’ body was developed for the researchers to observe the solution’s antibacterial effects. Test results showed that no abnormalities were discovered within 14 days after the initial date of testing and the mice grew as normal when fed with an amount of the solution 250 times of a normal clinical doze (In this case a man was assumed to weigh 60 kg.) and that the solution demonstrated obvious antibacterial effects on the two types of selected germs. The respective measured MIC50 and MIC90 values of the two germs were 3.2, 12.8, 6.4, and 25.6 mg L−1. Therefore, it is reasonable to conclude that Jinyulian Oral Solution possesses no acute toxicity but obvious antibacterial effects on the two before-mentioned germs.


2020 ◽  
Vol 7 (2) ◽  
pp. 75
Author(s):  
Amalia Khairunnisa ◽  
Nashrul Wathan ◽  
Mia Fitriana ◽  
Fadlilaturrahmah Fadlilaturrahmah ◽  
Nisriyati Fiddina

Nymphaea pubescens Willd telah diketahui mempunyai efek antibakteri, terutama pada biji dan daunnya. Tetapi sampai saat ini bagian bunga dari tanaman tersebut belum dilakukan pengujian aktivitas antibakteri. Tujuan dari penelitian ini untuk melakukan skrining fitokimia, uji aktivitas antibakteri dan penentuan konsentrasi hambat minimum (KHM) dari ekstrak metanol bunga N. pubescens terhadap S. aureus dan E. coli. Proses ekstraksi bunga N. pubescens dimaserasi menggunakan pelarut metanol dengan perbandingan 1: 4 b/v. Metode pengujian yang digunakan ada dua yaitu metode difusi untuk pengujian aktivitas antibakteri dan metode dilusi untuk pengukuran konsentrasi hambat minimum (KHM). Hasil skrining fitokimia didapatkan bahwa ekstrak metanol bunga N. pubescens mengandung senyawa golongan fenolik, saponin dan flavonoid. Hasil pengujian aktivitas antibakteri menunjukkan bahwa ekstrak metanol bunga N.pubescens mampu menghambat S. aureus (diameter hambat 10 ± 0,29 mm) dan E.coli (diameter hambat 10,2 ± 0,50 mm). Konsentrasi hambat minimum dari ekstrak metanol bunga N. pubescens terhadap S.aureus sebesar 12,5% dan terhadap E.coli sebesar 25%. Dapat disimpulkan bahwa ekstrak metanol bunga N. pubescens memiliki aktivitas sebagai antibakteri. Nymphaea pubescens Willd has known to have antibacterial effects, especially on the seeds and leaves. However, until now the flower of the plant has not been tested for antibacterial activity. The purpose of this study was to perform phytochemical screening, antibacterial activity test and determine the minimum inhibitory concentration (MIC) of the methanol extract of N. pubescens flowers against S. aureus and E. coli. The process of extracting N. pubescens flowers is macerated using methanol as a solvent with a ratio of 1: 4 w / v. There are two test methods used, namely the diffusion method for testing antibacterial activity and the dilution method for measuring the minimum inhibitory concentration (MIC). The results of phytochemical screening showed that the methanol extract of N. pubescens flowers contained phenolic compounds, saponins, and flavonoids. The results of the antibacterial activity test showed that the methanol extract of N.pubescens flowers was able to inhibit S. aureus (inhibition diameter 10 ± 0.29 mm) and E. coli (inhibitory diameter 10.2 ± 0.50 mm). The minimum inhibitory concentration of the methanol extract of N. pubescens flowers against S.aureus was 12.5% and against E. coli was 25%. It can be concluded that the methanol extract of N. pubescens flowers has antibacterial activityKeywords: Nymphaea pubescens, lotus flower, methanol extract, antibacterial


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Milind J. Umekar ◽  
Radheshyam T. Lohiya ◽  
Krishna R. Gupta ◽  
Nandkishore R. Kotagale ◽  
Neha S. Raut

Abstract Background The metal ion complexes of meropenem and cefixime with cadmium, silver, palladium, zinc, nickel, cobalt and copper were synthesized and characterized by UV, FTIR and H1-NMR spectrophotometry. The antibacterial effects of the complexes were studied using cup and plate method against S. aureus, B. subtilis, E. coli, P. aeruginosa and K. pneumoniae for normal and resistant strains of bacteria. The minimum inhibitory concentration of the metal ion complexes was determined by broth dilution method. Results UV spectroscopic studies suggested that meropenem ligand form complex with different metal ions and FTIR spectrum confirmed the proposed structure. Similarly, UV spectrum of cefixime metal ion complexes at λmax 202–295 nm and meropenem metal ion complexes at λmax 249–304 nm was observed in all the complexes. FTIR peaks for a proposed structure were observed in all the meropenem and cefixime metal ion, indicating the formation of complexes, and retained the functional groups of drugs. Meropenem as well as cefixime metal ion complexes exhibited more antibacterial activity against all the selected bacterial strains. Specifically, the lowest minimum inhibitory concentration against P. aeruginosa and K. pneumoniae was observed to be 100 and 150 μg/ml, respectively. Conclusion The present study concluded that the meropenem and cefixime metal complexes can exhibit the better treatment than individual drug on normal as well as resistant bacteria.


Author(s):  
Alphonsus D’souza ◽  
Pankaj Kumar ◽  
Abhishek Kumar ◽  
Soundarya M. Rai ◽  
Prashant Nayak

A series of substituted dihydro-1, 2-oxazole benzopyran-2-one (SR1-SR6) were synthesized through the intermediate substituted benzopyran-2-one chalcones and were characterized using spectral analysis.   Compounds were docked with receptor DNA Gyrase B (PDB code: 5L3J) to know its interaction and binding energy; ranges -3.38 to -2.15 kcal/mol. Further these compounds were tested for antibacterial activity using tube dilution method and MIC values were observed; ranges 3.12 to 25 µg/ml. Compound 3-(5-(m-tolyl)-4,5-dihydroisoxazol-3-yl)-2H-chromen-2-one (SR3) showed the best interaction with binding energy -3.38 kcal/mol and antimicrobial activity having MIC 3.12 µg/ml. GRAPHICAL ABSTRACT


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