scholarly journals An Efficient Green Procedure for Synthesis of Some Fluorinated Curcumin Analogues Catalyzed by Calcium Oxide under Microwave Irradiation and Its Antibacterial Evaluation

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
S. Elavarasan ◽  
D. Bhakiaraj ◽  
T. Elavarasan ◽  
M. Gopalakrishnan

A series of fluorine substituted curcumin analogues have been synthesized in a cheaper and greener method using calcium oxide as catalyst under microwave irradiation. All the synthesized compounds have been characterized by FT-IR, MS, elemental analysis, and1H and13C NMR spectroscopic techniques and screened for antibacterial activities againstStaphylococcus aureus,β-Heamolytic streptococcus,Shigella flexneri,Vibrio cholerae,Pseudomonas aeruginosa, andKlebsiella pneumonia. All the synthesized compounds are showing good zone of inhibition against the tested bacterial strains.

Author(s):  
Marwah W. Khalid ◽  
Leaqaa Abd ◽  
Ahmed N. Abood

  Secnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 144-fold increase in aqueous solubility compared to ciprofloxacin. Taste evaluation by panel method showed palatable taste in prodrugs compared to the parent drugs. The synthesized compounds were screened for their antimicrobial activity against different bacterial strains which are, Staphylococcus aureus, Pseudomonas aeruginosa, E. coli and Klebsiella pneumonia. The prodrugs have revealed excellent antibacterial activities compared with the parent compounds. Chemical hydrolysis study at pH (1.2 and 7.4) has indicated that these compounds may pass unhydrolyzed through the stomach and produce enough stability to be absorbed from the intestine as indicated by t1/2 values.


2020 ◽  
Vol 82 (11) ◽  
pp. 2344-2352
Author(s):  
C. Joseph Kirubaharan ◽  
Zhen Fang ◽  
Chong Sha ◽  
Yang-Chun Yong

Abstract Silver (Ag) and palladium (Pd) nanoparticles were synthesized via a green synthesis route, which was mediated with the extract of Daucus carota leaves. The morphological, crystalline and structural nature of the synthesized nanoparticles was characterized by UV-Vis spectrophotometer, and TEM, XRD and FT-IR analyses. High antibacterial activities of the prepared Ag and Pd nanoparticles were observed towards different water-borne pathogens of Klebsiella pneumonia, Vibrio cholera and Escherichia coli. The catalytic efficiency of the prepared nanoparticles for the removal of rhodamine 6G (Rh-6G) dye was also evaluated. Nearly 98% of the Rh-6G dye was decolorized by the synthesized Pd nanoparticles within 2 min, and the synthesized Ag nanoparticles took 30 min for 89.4% decolorization. This work provided greener nanocatalysts for pollutant treatment and demonstrated the power of green biosynthesis for metallic nanoparticles.


2020 ◽  
Vol 17 (7) ◽  
pp. 631-638
Author(s):  
Dele ABDISSA ◽  
Gezahegn FAYE ◽  
Melkamu FAYERA ◽  
Shiferaw DEMISSIE

Kniphofia pumila has been traditionally used for the treatment of different diseases in Oromiya regional state, western part of Ethiopia. Thus, the main objective of this study was to extract bioactive natural products from the roots of K. pumila and perform in vitro antibacterial activity tests against selected pathogens. Extraction of compound from the roots of K. pumila was carried out by maceration method at room temperature and its antibacterial activity was done using agar disc diffusion method. The crude extracts alone and along with ZnCl2 were tested against pathogenic bacteria Escherichia coli (ATCC 25722), Klebsiella pneumoniae subsp. pneumoniae (DSM 19613), Staphylococcus aureus (ATCC 25925) and Salmonella Typhimurium (ATCC 13311). Following its promising activity, the acetone crude extract that have shown better antibacterial activity was subjected to column chromatography for isolation of pure compound. Hence, one pure compound (GZ-1) was obtained from acetone crude extract. Meanwhile, the antibacterial activities of the isolated compound alone and in combination with ZnCl2 were also performed against all aforementioned bacterial strains. Then, isolated compound was characterized by using NMR spectroscopic techniques such as 1H-NMR, 13C-NMR and, 2D NMR, so as to establish its structure as 3’-acetyl-2’,6’-dihydroxy-4-methoxyphenyl-1,8-dihydroxy-3-methylanthraquinone, trivial name knipholone. Finally, GZ-1 was isolated from the roots of K. pumila and it was noted that the antibacterial activities of ZnCl2 in combination with crude extract as well as with isolated compound against E. coli (ATCC 25722), S. aureus (ATCC 25925) and S. Typhimurium (ATCC 13311) bacterial strains showed remarkable results which were greater than the antibacterial activity of the positive standard drug (gentamycin). To sum up, from the chromatographic isolation of roots acetone extract of K. pumila one pure compound (knipholone) was obtained. Its antibacterial activity was also evaluated in combination with ZnCl2 salt and alone.


2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Fernando Carrasco ◽  
Wilfredo Hernández ◽  
Oscar Chupayo ◽  
Celedonio M. Álvarez ◽  
Sandra Oramas-Royo ◽  
...  

Four indole-3-carbaldehyde semicarbazone derivatives, 2-((5-bromo-1H-indol-3-yl)methylene)hydrazinecarboxamide (1), 2-((5-chloro-1H-indol-3-yl)methylene)hydrazinecarboxamide (2), 2-((5-methoxy-1H-indol-3-yl)methylene)hydrazinecarboxamide (3), and 2-((4-nitro-1H-indol-3-yl)methylene)hydrazinecarboxamide (4) were synthesized and characterized by ESI-MS and spectroscopic (FT-IR, 1H NMR, and 13C NMR) techniques. The two-dimensional NMR (in acetone-d6) spectral data revealed that the molecules 1 and 2 in solution are in the cisE isomeric form. This evidence is supported by DFT calculations at the B3LYP/6-311++G(d,p) level of theory where it was shown that the corresponding most stable conformers of the synthesized compounds have a cisE geometrical configuration, in both the gas and liquid (acetone and DMSO) phases. The in vitro antibacterial activity of compounds 1–4 was determined against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Pseudomonas aeruginosa and Escherichia coli) bacteria. Among all the tested semicarbazones, 1 and 2 exhibited similar inhibitory activities against Staphylococcus aureus (MIC = 100 and 150 μg/mL, respectively) and Bacillus subtilis (MIC = 100 and 150 μg/mL, respectively). On the other hand, 3 and 4 were relatively less active against the tested bacterial strains compared with 1, 2, and tetracycline.


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.


Author(s):  
Dushyant Sharma ◽  
Reena Rani ◽  
Monika Chaturvedi ◽  
J. P. Yadav

Objective: Plants offer a novel source for the isolation of a wide variety of medicinal agents. Allium cepa commonly known as onion is very well known medicinal plants and we investigated the antibacterial activity of different extracts and their phytochemical analysis by gas chromatography mass spectrometry (GCMS).Methods: The extracts of A. cepa prepared in six different solvents was analyzed for antibacterial activity against nine American type cell culture (ATCC) reference bacterial strains i.e. Shigella flexneri, Enterococcus faecalis, Staphylococus aureus, Proteus mirabilis, Salmonella typhi, Serratia marcescens, Klebsiella pneumonia, Escherichia coli, Pseudomonas aeruginosa by using the agar well diffusion method. GCMS analysis also has been carried out for their phytochemical analysis.Results: The results obtained from agar well diffusion assay showed the zone of inhibition range from 10±0.76 to 26±0.76 mm for different extracts. The methanol extract was found most potent against K. pneumonia and S. marcescens with the zone of inhibition of 26±0.76 mm for both strains. Minimum inhibitory concentration (MIC) values were in the range of 1.87 to 7.5 mg/ml and the MIC values for K. pneumonia and S. marcescens was 1.87 mg/ml. A total of 43 compounds were identified by GCMS analysis. Out of them dodecanoic acid was found common in all extracts.Conclusion: It is concluded that Allium cepa have good antibacterial activity so it can be used for the treatment of various infectious diseases.


2020 ◽  
Vol 17 ◽  
Author(s):  
Kiana Faraji Sina ◽  
Asieh Yahyazadeh ◽  
Nosrat Ollah Mahmoodi

: 2, 3-Dihydroquinazolinones are of popular compounds with the diversification of biological and pharmacological activities. Among many discovered methods, there are efficient and convenient methods used for the synthesis of 2, 3- dihydroquinazoline-4 (1H)-one and some new bis 2, 3-dihydroquinazoline-4 (1H)-one derivatives which are reported in this study. The mentioned methods include the two-component condensation of one molecule of anthranilamide and one molecule of DOI: pyrazole carbaldehyde using montmorillonite-K10 as a catalyst for the preparation of 2, 3 dihydroquinazoline4 (1H)-ones. Also, one-pot pseudo-five-component reaction (5MCRs) of two molecules of isatoic anhydride, two molecules of pyrazole carbaldehydes and one molecule of ethan-1, 2-diamine in the presence of the recoverable catalyst (montmorillonite-K10) for the synthesis of bis 2, 3-dihydroquinazoline-4 (1H)-ones. Despite the short times of reactions, high yields of products were obtained, which were validated using FT-IR, 1HNMR, 13CNMR, and elemental analysis. Moreover, the compounds were screened for their antimicrobial activities against two-gram-positive bacterial strains: Staphylococcus aureus and Micrococcus Luteus; and against two-gram-negative bacterial strains, as well: Escherichia coli and Pseudomonas aeruginosa, which all were utilized for antibacterial investigations. The results showed moderate or significant antibacterial activities.


2021 ◽  
Vol 11 (4) ◽  
pp. 12178-12185

In this study, some thiazole-based pyrrolidine derivatives were synthesized, characterized by FT-IR and 1H NMR spectroscopic techniques, and evaluated as potential antibacterial agents. Their antibacterial activities were evaluated by broth microdilution method and expressed as minimum inhibitory concentration; against Escherichia coli, Salmonella typhimurium, Bacillus cereus, and Staphylococcus aureus. Cytotoxicity studies of synthesized compounds were also conducted to minimize the toxic effects on healthy mammalian cells. From synthesized compounds, 4-F-phenyl derivative compound (11) has been found to inhibit Gram-positive bacteria with minimum toxicity selectively.


2019 ◽  
Vol 8 (1) ◽  
pp. 302-308 ◽  
Author(s):  
Afsaneh Vahidi ◽  
Hamideh Vaghari ◽  
Yahya Najian ◽  
Mohammad Javad Najian ◽  
Hoda Jafarizadeh-Malmiri

Abstract Zinc oxide nanoparticles (ZnO NPs) were green synthesized using Pelargonum zonale leaf extract under three different heating methods, and their characteristics were evaluated using X-ray diffractometry (XRD), Fourier-transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), 2,2-diphenyl-2-picrylhydrazyl (DPPH) assay and antibacterial well diffusion method. The FT-IR analysis indicated that the Pelargonium leaf extract contained hydroxyl and amide I groups which were related to the proteins, carbohydrate, tannins and phenolic compounds of the extract and had an essential role in the reduction of the zinc ions and synthesis of the ZnO NPs. The obtained results revealed that the synthesized spherical individual ZnO NPs as well as the number of aggregates using microwave irradiation, autoclave and conventional heating (heater-stirrer) methods had average crystalline size of 51, 60 and 61 nm. Furthermore, antioxidant activities of the fabricated ZnO NPs were 7.8, 4.1 and 5.5% by using conventional heating, autoclave and microwave irradiation, respectively. The obtained results indicated that all the formed ZnO NPs had bactericidal effects against to the both Gram negative and Gram positive bacteria strains. However, the synthesized ZnO NPs using conventional heating method had the highest antibacterial activities toward both studied bacteria strains.


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