scholarly journals Synthesis, Characterization, and Antibacterial Activity of Diethyl 1-((4-Methyl-2-phenyl-4,5-dihydrooxazol-4-yl)methyl)-1H-1,2,3-triazole-4,5-dicarboxylate

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
S. Boukhssas ◽  
Y. Aouine ◽  
H. Faraj ◽  
A. Alami ◽  
A. El Hallaoui ◽  
...  

The compound, diethyl 1-((4-methyl-2-phenyl-4,5-dihydrooxazol-4-yl)methyl)-1H-1,2,3-triazole-4,5-dicarboxylate 2, was synthesized in high yield, through 1,3-dipolar cycloaddition reaction of 4-(azidomethyl)-4-methyl-2-phenyl-4,5-dihydrooxazole and diethyl but-2-ynedioate in the absence of a solvent. The structure of the synthesized compound was established on the basis of NMR spectroscopy (1H, 13C), X-ray crystallography, and MS data. The prepared compound was also tested in vitro for its antibacterial activity against Gram-positive bacteria (Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli). The calculation of MBC/MIC ratio showed that this triazole derivative 2 had a bactericidal effect on the two strains tested.

2018 ◽  
Vol 7 (4) ◽  
pp. 267-271
Author(s):  
Oumaima Karai ◽  
Younas Aouine ◽  
Hassane Faraj ◽  
Alami Anouar ◽  
Mohammed Rachid Kabbour ◽  
...  

The present work covers the recent synthetic of methyl (2R)-2-benzamido-2-{[(1R)-2-methoxy-2-oxo-1-phenylethyl]amino}acetate, via N-alkylation of methyl a-azido glycinate N-benzoylated with methyl 2-amino-2-phenylacetate in methylene chloride and in presence of triethylamine as basic catalyst. The structure of the prepared compound was determined by spectroscopic methods: 1H-NMR, 13C-NMR, MS data, elemental analysis and confirmed by X-Ray diffraction. This compound was screened in vitro for its antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa and Salmonella enteric). The MIC values confirmed that the title compound had a bactericidal effect against the strains tested.


2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
D. P. Mohapatra ◽  
V. Thakur ◽  
S. K. Brar

In vitro antibacterial activity of methanol, ethanol, and ethyl acetate extracts of raw and processed honey was tested against Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Enterococcus faecalis, and Micrococcus luteus) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi). Both types of honey showed antibacterial activity against tested organisms with the zone of inhibition (ZOI) ranging from 6.94 to 37.94 mm, while E. coli, S. typhi, and P. aeruginosa showed that sensibility towards all the extracts with ZOI ranges between 13.09 to 37.94 mm. The methanol extract showed more potent activity than other organic extracts. Gram-negative bacteria were found to be more susceptible as compared to Gram-positive bacteria except E. faecalis. The broth microdilution assay gave minimum inhibitory concentrations (MIC) value of 625 μg/mL, while the minimum bactericidal concentration (MBC) ranges between 625 μg/mL 2500 μg/mL. The study showed that honey has antibacterial activity (bacteriostatic and bactericidal effect), similar to antibiotics, against test organisms and provides alternative therapy against certain bacteria.


2010 ◽  
Vol 63 (11) ◽  
pp. 1550 ◽  
Author(s):  
Nawong Boonnak ◽  
Achjana Khamthip ◽  
Chatchanok Karalai ◽  
Suchada Chantrapromma ◽  
Chanita Ponglimanont ◽  
...  

Three new xanthones, pruniflorone M-O (1–3), and a new xanthonolignoid, 3-methoxy-5′-demethoxycadensin G (4), were isolated from the green fruits of Cratoxylum formosum ssp. pruniflorum along with three known xanthones (5–7) and a known flavonoid (8). Their structures were elucidated by spectroscopic methods and the structure of 1 was also determined by X-ray crystallography. Compounds 2 and 7 showed potent nitric oxide inhibitory activity with IC50 values of 4.4 and 4.3 μM, respectively. Moreover, 7 also showed strong antibacterial activity against both Gram-positive and Gram-negative bacteria with an MIC value of 4.67 μg mL–1.


2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
Mohammed Khaled bin Break ◽  
M. Ibrahim M. Tahir ◽  
Karen A. Crouse ◽  
Teng-Jin Khoo

Two bidentate Schiff base ligands having nitrogen sulphur donor sequence were derived from the condensation of S-benzyldithiocarbazate (SBDTC) with 2-chloroacetophenone and 4-chloroacetophenone to give S-benzyl-β-N-(2-chlorophenyl)methylenedithiocarbazate (NS2) and S-benzyl-β-N-(4-chlorophenyl)methylenedithiocarbazate (NS4) isomers. Each of the ligands was then chelated with Cd2+, Zn2+, Cu2+, and Ni2+. The compounds were characterized via IR spectroscopy and melting point while the structure of NS4 was revealed via X-ray crystallography. Finally, the compounds were screened for antimicrobial activity to investigate the effect that is brought by the introduction of the chlorine atom to the benzene ring. X-ray crystallographic analysis showed that the structure of NS4 is planar with a phenyl ring that is nearly perpendicular to the rest of the molecules. The qualitative antimicrobial assay results showed that NS4 and its complexes lacked antifungal activity while Gram-positive bacteria were generally inhibited more strongly than Gram-negative bacteria. Furthermore, NS4 metal complexes were inhibited more strongly than the ligand while the opposite was seen with NS2 ligand and its complexes due to the partial solubility in dimethyl sulfoxide (DMSO). It was concluded that generally NS2 derivatives have higher bioactivity than that of NS4 derivatives and that the Cd complexes of both ligands have pronounced activity specifically onK. rhizophila.


2013 ◽  
Vol 78 (9) ◽  
pp. 1323-1333 ◽  
Author(s):  
Garima Matela ◽  
Robina Aman ◽  
Chetan Sharma ◽  
Smita Chaudhary

A new series of diisopropyloxytin- and triorganotin(IV) complexes of H2hbgl (1) of the general formula Sn(OPri)2(hbgl) (2), Sn(OPri)2(Hhbgl)2 (3), Ph3Sn(Hhbgl) (4), Bu3Sn(Hhbgl) (5) and Me3Sn(Hhbgl) (6), [where H2hbgl= a ligand of thymol derivative namely, N-(2-hydroxy-3-isopropyl-6-methyl benzyl)Glycine] were synthesized by reacting tin- and triorganotin(IV) chloride with the ligand, with the aid of sodium iso-propoxide in appropriate stiochiometric ratios (1:1 and 1:2). These complexes were characterized by elemental analysis, IR, 1H nuclear magnetic resonance. The spectral data suggest that the carboxylate group, in complexes 2-5, was bonded in a bidentate manner, while a unidentate bonding was observed in complex 6. All five complexes were tested in vitro for their antibacterial activity against Gram-positive bacteria namely, Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 121 and two Gram-negative bacteria namely, Escherichia coli MTCC 1652 and Pseudomonas aeruginosa MTCC 741. All the five complexes were also tested against three pathogenic fungal strains namely, Aspergillus niger, A. flavus and Penicillium sp.


2018 ◽  
Vol 16 (1) ◽  
pp. 1077-1088
Author(s):  
L. Jyothish Kumar ◽  
S. Sarveswari ◽  
V. Vijayakumar

AbstractA series of 3,4-dihydro-9-arylacridin-1(2H)-ones was synthesized and enaminone function was introduced at the C-2 position using DMFDMA catalyst which in turn successfully converted into pyrazole, isoxazol, 1-phenyl-1H-pyrazole by treating it with reagents such as hydrazine, hydroxylamine and phenylhydrazine. These newly synthesized compounds were evaluated for their antibacterial activity against a series of Gram-Positive bacteria including Staphylococcusaureus, Bacilluscereus, StaphylococcusaureusMLS16 and Gram-Negative bacteria including Klebsiellaplanticol, Escherichiacoliand Pseudomonasaeruginosaand also against fungal strains including Candidaalbicans, Candidaparapsilosis, Candidaglabrata, Candidaaaseri, Aspergillusnigerand Issatchenkiahanoiensis. The compounds3aand6aexhibited considerable antifungal activity (MIC value 0.007 and 0.006 μM) against Candidaalbicansand Aspergillusnigerrespectively. The compound4ashowed excellent antibacterial activity towards EscherichiaColi(MIC = 0.003 μM) and the compound5afound to show prominent DPPH radical scavenging activity with EC50value 16.85±1.5μg mL−1.


Polyhedron ◽  
2017 ◽  
Vol 134 ◽  
pp. 230-237 ◽  
Author(s):  
Pradip Bera ◽  
Paula Brandão ◽  
Gopinath Mondal ◽  
Harekrishna Jana ◽  
Abhimanyu Jana ◽  
...  

2007 ◽  
Vol 53 (1) ◽  
pp. 75-81 ◽  
Author(s):  
M Shahid ◽  
Anwar Shahzad ◽  
Abida Malik ◽  
M Anis

Leaves, stem, and flowers of Saraca asoca, an endangered medicinal plant in India, and young explants cultivated on Murashige & Skoog's medium containing 6-benzylaminopurine were analyzed for antibacterial potential. Alcoholic and aqueous extracts from parent explants and their in vitro raised calli were tested by an agar well diffusion method. Minimal inhibitory concentrations (MICs) of the extracts were determined by broth microdilution method. Aqueous extracts showed antibacterial activity against limited bacterial species, whereas alcoholic extracts were active against a wider range of bacteria. Although the alcoholic extracts of all the explants and calli showed antibacterial activity, the extracts derived from flowers and their calli showed better results. Extracts derived from calli showed comparable results to the extracts from explants. Overall, the MICs of the extracts ranged from 0.039 to 1.25 mg/mL. MICs against Gram-positive bacteria ranged from 0.078 to 1.25 mg/mL, whereas they ranged between 0.039 and 0.625 mg/mL against Gram-negative bacteria. A MIC distribution plot showed that Gram-negative bacteria were more susceptible to the extracts than Gram-positive bacteria. It is concluded that extracts of S. asoca contain antibacterial agent, and as the calli gave good results, in vitro cultivation of the explants may be used to obtain antibacterial compounds. This is the first report on antibacterial activity of S. asoca, especially through in vitro raised calli.Key words: Saraca asoca, antibacterial activity, in vitro, callus, minimal inhibitory concentration.


2014 ◽  
Vol 881-883 ◽  
pp. 484-487 ◽  
Author(s):  
Lin Yang ◽  
Jing Long ◽  
Wei Juan Li ◽  
Ai Mei Yang ◽  
Zhong Duo Yang ◽  
...  

In this study, 23 endophytic fungus were isolated from Anemone tomentosa. The antibacterial activity of the endophytic fungi were tested and analyzed by filter paper method. The results showed that the endophytic fungi from Anemone tomentosa had broad antibiogram and strong inhibited Gram-positive bacteria and Gram-negative bacteria, especially the mycelia extract of root-1, the ethyl acetate and the n-BuOH extracts of root-8. So the endophytic fungi from Anemone tomentosa could be an important resource for developing antimicrobial products.


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