scholarly journals Microwave-Assisted Synthesis of Acetophenone (per-O-acetylated-β-D-glucopyranosyl)thiosemicarbazones

2010 ◽  
Vol 7 (3) ◽  
pp. 899-907 ◽  
Author(s):  
Nguyen Dinh Thanh ◽  
Nguyen Thi Kim Giang ◽  
Le The Hoai

Thirteen new substituted acetophenone (2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-thiosemicarbazones (3) were synthesized by reaction of 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl thiosemicarbazide (1) and substituted acetophenones (2). The reaction was performed using microwave-assisted method. The compounds (3) have remarkable antibacterial and antifungal activities againstEscherichia coli, Staphylococcus epidermidisandCandida albicans.

2008 ◽  
Vol 5 (1) ◽  
pp. 120-129 ◽  
Author(s):  
N. D. Argade ◽  
B. K. Kalrale ◽  
C. H. Gill

Disubstituted oxazol-5-one and pyrazoles are known to exhibit various biological activities. Therefore, in this work, we designed pyrazole containing 2,4-disubstituted oxazol-5-one(3a-g)as a new class of antimicrobial agents. Synthesis of titled compounds was carried out by two different methods. In the first method (conventional Method A), disubstituted oxazol-5-one(3a-g)was prepared by reacting 1-phenyl-3-p-tolyl-1H-pyrazole-4-carbaldehyde(1a-g)with hippuric acid(2)and sodium acetate, in an acetic anhydride for 2.5 - 4 h. In the second method (Method B), the above reaction was carried out under microwave assistance. Compared to the conventional method, the microwave-assisted synthesis of 3,4,5-trisubstituted imidazoles demonstrate several advantages, in terms of reaction time and overall yield. All the test compounds were evaluated forin vitroantibacterial and antifungal activities. In general, compounds with electron withdrawing groups showed good antibacterial and antifungal activities. Among the compound tested, compound(3d)showed highest activity.


2011 ◽  
Vol 76 (6) ◽  
pp. 823-830 ◽  
Author(s):  
Dipti Dodiya ◽  
Haresh Ram ◽  
Amit Trivedi ◽  
Viresh Shah

An efficient, microwave-assisted synthesis of novel 2-alkoxy- 5,6,7,8-tetrahydroquinoline-3-carbonitriles, which have not hitherto been reported, via reactions of cyclohexanone and arylidene malononitriles in the corresponding alcohols in presence of sodium is described. All the newly synthesized compounds were characterized by the IR, 1H-NMR, 13C-NMR and mass spectroscopic techniques and by elemental analyses. The newly synthesized compounds were evaluated for their antibacterial and antifungal activities.


2017 ◽  
Vol 82 (2) ◽  
pp. 117-125 ◽  
Author(s):  
Dongamanti Ashok ◽  
Reddy Vanaja ◽  
Mdderla Sarasija ◽  
Vijaya Lakshmi

Due to the potential antimicrobial activity of pyranochromenones and pyrazolines moieties, hybrid compounds containing both, substituted 4-Chloro-8-methyl-2-(1,3-diphenyl- -1H-pyrazol-4-yl)-1,5-dioxa-2H-phenanthren-6-ones (4a-g), have been synthesized from substituted (E)-1-(7-Hydroxy-4-methyl-8-coumarinyl)-3-(1,3-diphenyl -1H-pyrazol-4-yl)-2-propen-1-ones (3a-g) in good yield using the Vilsmeier reaction, by microwave-assisted method. The structures of all the compounds have been established on the basis of analytical and spectral data. All the synthesized compounds were tested in vitro for their antibacterial and antifungal activities. Some of the compounds have shown very good activity compared to standard drugs against all pathogenic bacteria and fungi.


2009 ◽  
Vol 6 (s1) ◽  
pp. S374-S380 ◽  
Author(s):  
T. Surendiran ◽  
S. Balasubramanian ◽  
Sivaraj D.

A new family of 1,2,3,4 – tetrahydrocarbazolyl thiazolidin-4-ones(4a-e)and 1,2,3,4–tetrahydrocarbazolyl azetidin-2-ones(5a-e)were individually derived usingN-[(α-substituted bezylidenehydrazino) acetyl] -1,2,3,4-tetra-hydrocarbazoles3a-eby cyclization with thioglycolic acid and chloro- acetylchloride respectively. The compounds(3a-e)were prepared by condensation ofN-(hydrazinoacetyl) 1,2,3,4-tetrahydrocarbazole (2) with a series of aldehydes. The compound 2 was obtained by the hydrazinolysis ofN-(chloroacetyl)-1,2,3,4-tetrahydrocarbazole (1). These products were characterized by IR, NMR, MASS spectra and by elemental analysis. All the titled compounds(4a-e)and5(a-e)were screened for antibacterial and antifungal activities.


2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).


2019 ◽  
Vol 74 (6) ◽  
pp. 473-478 ◽  
Author(s):  
Abd El-Galil E. Amr ◽  
Ahmed M. Naglah ◽  
Nermien M. Sabry ◽  
Alhussein A. Ibrahim ◽  
Elsayed A. Elsayed ◽  
...  

AbstractInterest in the synthesis of heterocyclic organic molecules with peptide moieties has gained attention due to their potential biological activities. The current work aimed at synthesizing new macrocyclic tripeptide imides and evaluating their possible antimicrobial activities. A series of 11 derivatives were prepared from dimethyl 3,5-pyridinevalinyl ester either by NaOH or NH2NH2 treatment, followed by cyclization and further reaction with NaOH or NH2NH2. The majority of synthesized derivatives showed promising antibacterial and antifungal activities in comparison to standard known antibiotics. Compounds 5a and 7b showed the most potential antibacterial against Staphylococcus aureus and antifungal activities against Candida albicans, respectively.


Nanomaterials ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 638 ◽  
Author(s):  
Majid Sharifi-Rad ◽  
Pawel Pohl

In this study, very simple and fast one-step synthesis of biogenic silver chloride nanoparticles (AgCl-NPs) using a Pulicaria vulgaris Gaertn. aerial part extract from an aqueous solution of silver nitrate at room temperature is proposed. The proceedings of the reaction were investigated by UV–Vis spectroscopy. AgCl-NPs were characterized using X-ray diffraction spectroscopy (XRD), Fourier-transform infrared spectroscopy (FTIR), and transmission electron microscopy (TEM). Antibacterial and antifungal activities of these nanoparticles were evaluated by disk diffusion and microdilution methods against Staphylococcus aureus, Escherichia coli, Candida albicans, and C. glabrata. In addition, the antioxidant activity of the synthesized AgCl-NPs was determined by the DPPH radical scavenging assay. The antimicrobial test confirmed the bactericidal activity of biosynthesized AgCl-NPs against Gram-positive and Gram-negative bacteria. They also exhibited good antifungal activities with minimum inhibitory concentration (MIC) values ranging from 40 to 60 µg/mL against Candida glabrata and Candida albicans, respectively. In addition, biosynthesized AgCl-NPs were established to have remarkable antioxidant activity. All this pointed out that the proposed new biosynthesis approach resulted in production of AgCl-NPs with convenient biomedical applications.


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