scholarly journals Microwave Assisted Improved Method for the Synthesis of Pyrazole Containing 2,4,-Disubstituted Oxazole-5-one and their Antimicrobial Activity

2008 ◽  
Vol 5 (1) ◽  
pp. 120-129 ◽  
Author(s):  
N. D. Argade ◽  
B. K. Kalrale ◽  
C. H. Gill
Keyword(s):  
Conventional Method ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Microwave Assisted Synthesis ◽  
Antifungal Activities ◽  
Microwave Assisted ◽  
Antibacterial And Antifungal Activities ◽  
Microwave Assistance ◽  
Antibacterial And Antifungal

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.

scholarly journals SYNTHESIS, CHARACTERIZATION AND IN VITRO STUDY OF ANTIBACTERIAL, ANTIFUNGAL ACTIVITIES OF SOME NOVEL DIHYDROPYRIMIDINTHIONE DERIVATIVES

2014 ◽  
Vol 44 (4) ◽  
pp. 289-293
Author(s):  
S. BALUJA ◽  
S. CHANDA ◽  
R. BHALODIA ◽  
R. TALAVIYA
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
In Vitro Study ◽  
Dimethyl Formamide ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Dihydropyrimidinthione is an important class of heterocyclic compounds which exhibits wide spectrum of biological activities. In the present study, some bio-active dihydropyrimidinthione derivatives have been synthesized and their characterization was done by IR, NMR and mass spectral data. The antibacterial and antifungal activities of synthesized compounds have also been studied in N,N-dimethyl formamide and Dimethyl sulfoxide.

scholarly journals Microwave assisted synthesis of substituted 4-chloro-8-methyl-2-(1,3-diphenyl-1H-pyrazol-4-yl)-1,5-dioxa-2H-phenanthren-6-ones and their antimicrobial activity

2017 ◽  
Vol 82 (2) ◽  
pp. 117-125 ◽  
Author(s):  
Dongamanti Ashok ◽  
Reddy Vanaja ◽  
Mdderla Sarasija ◽  
Vijaya Lakshmi
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Microwave Assisted Synthesis ◽  
Vilsmeier Reaction ◽  
Microwave Assisted ◽  
Antibacterial And Antifungal Activities ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
Microwave Assisted Method

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.

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
Keyword(s):  
Escherichia Coli ◽  
Candida Albicans ◽  
Staphylococcus Epidermidis ◽  
Microwave Assisted Synthesis ◽  
Antifungal Activities ◽  
Microwave Assisted ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Microwave Assisted Method

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.

scholarly journals An efficient, microwave-assisted, one-pot synthesis of novel 5,6,7,8-tetrahydroquinoline-3-carbonitriles

2011 ◽  
Vol 76 (6) ◽  
pp. 823-830 ◽  
Author(s):  
Dipti Dodiya ◽  
Haresh Ram ◽  
Amit Trivedi ◽  
Viresh Shah
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Microwave Assisted Synthesis ◽  
Spectroscopic Techniques ◽  
One Pot ◽  
Antifungal Activities ◽  
Microwave Assisted ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Antibacterial And Antifungal

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.

scholarly journals Microwave Assisted Synthesis of Novel 1,2,3,4-Tetrahydrocarbazolyl thiazolidin-4-ones and Azetidin-2-ones and its Biological Behavior

2009 ◽  
Vol 6 (s1) ◽  
pp. S374-S380 ◽  
Author(s):  
T. Surendiran ◽  
S. Balasubramanian ◽  
Sivaraj D.
Keyword(s):  
Elemental Analysis ◽  
Mass Spectra ◽  
Thioglycolic Acid ◽  
Biological Behavior ◽  
Microwave Assisted Synthesis ◽  
Antifungal Activities ◽  
Microwave Assisted ◽  
Antibacterial And Antifungal Activities ◽  
New Family ◽  
Antibacterial And Antifungal

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.

Synthesis of a Series of Novel 2-Amino-5-Substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole Derivatives as Potential Anticancer, Antifungal and Antibacterial Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Em Canh Pham ◽  
Tuyen Ngoc Truong ◽  
Nguyen Hanh Dong ◽  
Duy Duc Vo ◽  
Tuoi Thi Hong Do
Keyword(s):  
Cell Line ◽  
Biological Activities ◽  
Chemical Properties ◽  
Diffusion Method ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

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